Page last updated: 2024-08-07 17:16:25
Reverse transcriptase/RNaseH
[no definition available]
Synonyms
Research
Bioassay Publications (374)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 2 (0.53) | 18.7374 |
| 1990's | 74 (19.79) | 18.2507 |
| 2000's | 114 (30.48) | 29.6817 |
| 2010's | 148 (39.57) | 24.3611 |
| 2020's | 36 (9.63) | 2.80 |
Compounds (158)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| gallic acid | Human immunodeficiency virus 1 | IC50 | 100.0000 | 1 | 1 |
| ag-1549 | Human immunodeficiency virus 1 | IC50 | 0.0587 | 3 | 3 |
| ellipticine | Human immunodeficiency virus 1 | IC50 | 182.0000 | 1 | 1 |
| foscarnet | Human immunodeficiency virus 1 | IC50 | 11.3444 | 9 | 9 |
| ethidium | Human immunodeficiency virus 1 | IC50 | 2.0333 | 3 | 3 |
| nevirapine | Human immunodeficiency virus 1 | IC50 | 32.3710 | 233 | 236 |
| nevirapine | Human immunodeficiency virus 1 | Ki | 348.4432 | 37 | 37 |
| suramin | Human immunodeficiency virus 1 | IC50 | 12.2000 | 2 | 2 |
| thiabendazole | Human immunodeficiency virus 1 | IC50 | 14.6000 | 1 | 1 |
| delavirdine | Human immunodeficiency virus 1 | IC50 | 3.2663 | 24 | 24 |
| primaquine phosphate | Human immunodeficiency virus 1 | IC50 | 100.0000 | 1 | 1 |
| alizarin | Human immunodeficiency virus 1 | IC50 | 100.0000 | 1 | 1 |
| 5-methylpyrazole-3-carboxylic acid | Human immunodeficiency virus 1 | IC50 | 100.0000 | 1 | 1 |
| quinoline-4-carboxylic acid | Human immunodeficiency virus 1 | IC50 | 9,600.0000 | 1 | 1 |
| ethidium bromide | Human immunodeficiency virus 1 | IC50 | 2.0000 | 1 | 1 |
| stavudine | Human immunodeficiency virus 1 | IC50 | 4.8300 | 2 | 2 |
| zalcitabine | Human immunodeficiency virus 1 | Ki | 0.0510 | 1 | 1 |
| daunorubicin | Human immunodeficiency virus 1 | IC50 | 139.0000 | 1 | 1 |
| alovudine | Human immunodeficiency virus 1 | IC50 | 0.0500 | 1 | 1 |
| zidovudine | Human immunodeficiency virus 1 | IC50 | 17.7391 | 22 | 22 |
| triciribine phosphate | Human immunodeficiency virus 1 | IC50 | 0.0400 | 2 | 2 |
| foscarnet sodium | Human immunodeficiency virus 1 | IC50 | 9.8150 | 2 | 2 |
| l 697639 | Human immunodeficiency virus 1 | IC50 | 0.0200 | 2 | 2 |
| atevirdine | Human immunodeficiency virus 1 | IC50 | 4.3280 | 5 | 5 |
| acridine orange | Human immunodeficiency virus 1 | IC50 | 200.0000 | 1 | 1 |
| efavirenz | Human immunodeficiency virus 1 | IC50 | 1.3653 | 147 | 149 |
| efavirenz | Human immunodeficiency virus 1 | Ki | 0.2939 | 33 | 34 |
| thymidine 5'-triphosphate | Human immunodeficiency virus 1 | Ki | 0.0610 | 1 | 1 |
| calanolide a | Human immunodeficiency virus 1 | IC50 | 0.6600 | 2 | 2 |
| nsc 624231 | Human immunodeficiency virus 1 | IC50 | 15.9244 | 2 | 2 |
| 1-((2-hydroxyethoxy)methyl)-6-(phenylthio)thymine | Human immunodeficiency virus 1 | IC50 | 139.6950 | 8 | 8 |
| 5-ethyl-1-ethoxymethyl-6-(phenylthio)uracil | Human immunodeficiency virus 1 | IC50 | 0.0320 | 1 | 1 |
| l 693593 | Human immunodeficiency virus 1 | IC50 | 3.7000 | 3 | 3 |
| l-697661 | Human immunodeficiency virus 1 | IC50 | 3.2209 | 42 | 42 |
| tsao-t | Human immunodeficiency virus 1 | IC50 | 2.9667 | 3 | 3 |
| 1-(2',5'-bis-o-(tert-butyldimethylsilylribofuranosyl)-3-n-methylthymine)-3'-spiro-5''-(4''-amino-1'',2''-oxathiole-2'',2''-dioxide) | Human immunodeficiency virus 1 | IC50 | 22.5000 | 5 | 5 |
| emivirine | Human immunodeficiency virus 1 | IC50 | 0.3142 | 9 | 9 |
| epigallocatechin gallate | Human immunodeficiency virus 1 | IC50 | 0.7300 | 1 | 1 |
| 2',3'-dideoxythymidine | Human immunodeficiency virus 1 | IC50 | 0.0850 | 2 | 2 |
| 2',3'-dideoxyadenosine triphosphate | Human immunodeficiency virus 1 | Ki | 0.3950 | 6 | 6 |
| stavudine triphosphate | Human immunodeficiency virus 1 | IC50 | 4.4753 | 3 | 3 |
| stavudine triphosphate | Human immunodeficiency virus 1 | Ki | 0.5029 | 9 | 9 |
| triciribine | Human immunodeficiency virus 1 | IC50 | 0.0350 | 3 | 4 |
| zidovudine triphosphate | Human immunodeficiency virus 1 | IC50 | 0.9835 | 11 | 11 |
| zidovudine triphosphate | Human immunodeficiency virus 1 | Ki | 0.0597 | 3 | 3 |
| 2',3'-dideoxyuridine-5'-triphosphate | Human immunodeficiency virus 1 | Ki | 0.5450 | 1 | 1 |
| epicatechin | Human immunodeficiency virus 1 | IC50 | 100.0000 | 1 | 1 |
| u 88204 | Human immunodeficiency virus 1 | IC50 | 1.2000 | 1 | 1 |
| inophyllum b | Human immunodeficiency virus 1 | IC50 | 0.2027 | 3 | 3 |
| beta-thujaplicinol | Human immunodeficiency virus 1 | IC50 | 0.7264 | 11 | 11 |
| quinoxaline-2-carboxylic acid | Human immunodeficiency virus 1 | IC50 | 320.0000 | 1 | 1 |
| propidium iodide | Human immunodeficiency virus 1 | IC50 | 3.0000 | 1 | 1 |
| epicatechin gallate | Human immunodeficiency virus 1 | IC50 | 0.7600 | 1 | 1 |
| 3-phenyl-1H-pyrazole-5-carboxylic acid | Human immunodeficiency virus 1 | IC50 | 100.0000 | 1 | 1 |
| 1-(2',6'-difluorophenyl)-1h,3h-thiazolo(3,4-a)benzimidazole | Human immunodeficiency virus 1 | IC50 | 12.5350 | 2 | 2 |
| r 79882 | Human immunodeficiency virus 1 | IC50 | 3.3200 | 1 | 1 |
| l 696040 | Human immunodeficiency virus 1 | IC50 | 0.1678 | 5 | 5 |
| atazanavir | Human immunodeficiency virus 1 | IC50 | 0.0260 | 1 | 1 |
| gw420867x | Human immunodeficiency virus 1 | IC50 | 0.1120 | 2 | 2 |
| maprounic acid | Human immunodeficiency virus 1 | IC50 | 24.9000 | 1 | 1 |
| acetyl aleuritolic acid | Human immunodeficiency virus 1 | IC50 | 136.0000 | 1 | 1 |
| 3'-fluorothymidine-5'-triphosphate | Human immunodeficiency virus 1 | Ki | 0.0710 | 1 | 1 |
| etravirine | Human immunodeficiency virus 1 | IC50 | 0.2711 | 97 | 99 |
| dapivirine | Human immunodeficiency virus 1 | IC50 | 0.9303 | 18 | 18 |
| adam ii | Human immunodeficiency virus 1 | IC50 | 0.7000 | 8 | 8 |
| tryptophanamide | Human immunodeficiency virus 1 | IC50 | 12,800.0000 | 2 | 2 |
| abacavir | Human immunodeficiency virus 1 | IC50 | 0.1300 | 1 | 1 |
| delavirdine mesylate | Human immunodeficiency virus 1 | IC50 | 19.1375 | 8 | 11 |
| tnk-651 | Human immunodeficiency virus 1 | IC50 | 0.0340 | 5 | 5 |
| 9-(2-(phosphonomethoxy)ethyl)adenine diphosphate | Human immunodeficiency virus 1 | IC50 | 30.1500 | 2 | 2 |
| TTP | Human immunodeficiency virus 1 | IC50 | 200.0000 | 1 | 1 |
| 12-hydroxynevirapine | Human immunodeficiency virus 1 | IC50 | 3.0000 | 3 | 3 |
| lamivudine triphosphate | Human immunodeficiency virus 1 | IC50 | 5.0075 | 2 | 2 |
| lamivudine triphosphate | Human immunodeficiency virus 1 | Ki | 0.1880 | 1 | 1 |
| l 737126 | Human immunodeficiency virus 1 | IC50 | 1.3030 | 4 | 4 |
| dactinomycin | Human immunodeficiency virus 1 | IC50 | 270.0000 | 1 | 1 |
| 5-(1,1-dioxido-1,2-thiazinan-2-yl)-n-(4-fluorobenzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamide | Human immunodeficiency virus 1 | IC50 | 0.0050 | 1 | 1 |
| retrojusticidin b | Human immunodeficiency virus 1 | IC50 | 5.5000 | 1 | 1 |
| costatolide | Human immunodeficiency virus 1 | IC50 | 0.8450 | 2 | 2 |
| tenofovir | Human immunodeficiency virus 1 | IC50 | 0.3800 | 3 | 3 |
| dpc 961 | Human immunodeficiency virus 1 | IC50 | 0.0474 | 5 | 5 |
| dpc 963 | Human immunodeficiency virus 1 | IC50 | 0.0740 | 1 | 1 |
| 3-dimethylamino-4-(3,5-dimethylbenzyl)-5-ethyl-6-methylpyridin-2(1h)-one | Human immunodeficiency virus 1 | IC50 | 0.0140 | 2 | 2 |
| iqp-0528 | Human immunodeficiency virus 1 | IC50 | 2.3335 | 2 | 2 |
| 6-chloro-1,4-dihydro-4-oxo-1-(beta-d-ribofuranosyl)quinoline-3-carboxylic acid | Human immunodeficiency virus 1 | Ki | 0.5000 | 1 | 1 |
| gw 678248 | Human immunodeficiency virus 1 | IC50 | 0.0023 | 5 | 5 |
| 8-hydroxyefavirenz | Human immunodeficiency virus 1 | IC50 | 2.3410 | 1 | 1 |
| 4-phenyl-4-oxo-2-hydroxybuten-2-oic acid | Human immunodeficiency virus 1 | IC50 | 54.0000 | 1 | 1 |
| 2-hydroxy-4h-isoquinoline-1,3-dione | Human immunodeficiency virus 1 | IC50 | 8.7075 | 8 | 8 |
| 2-hydroxy-5-[[(5-methyl-2-furanyl)-oxomethyl]amino]benzoic acid | Human immunodeficiency virus 1 | IC50 | 100.0000 | 2 | 2 |
| 3-hydroxyquinolin-2(1h)-one | Human immunodeficiency virus 1 | IC50 | 100.0000 | 1 | 1 |
| nbd 556 | Human immunodeficiency virus 1 | IC50 | 250.0000 | 2 | 2 |
| nsc 727447 | Human immunodeficiency virus 1 | IC50 | 28.1000 | 1 | 1 |
| r 82150 | Human immunodeficiency virus 1 | IC50 | 8.8974 | 5 | 5 |
| r-82913 | Human immunodeficiency virus 1 | IC50 | 11.6333 | 3 | 3 |
| r 86183 | Human immunodeficiency virus 1 | IC50 | 2.1525 | 2 | 2 |
| hi 236 | Human immunodeficiency virus 1 | IC50 | 0.0665 | 4 | 4 |
| trovirdine | Human immunodeficiency virus 1 | IC50 | 1.1546 | 14 | 14 |
| trovirdine | Human immunodeficiency virus 1 | Ki | 0.6000 | 1 | 1 |
| ly 73497 | Human immunodeficiency virus 1 | IC50 | 0.9000 | 3 | 3 |
| jtk-303 | Human immunodeficiency virus 1 | IC50 | 91.0000 | 2 | 2 |
| apigenin | Human immunodeficiency virus 1 | IC50 | 443.0000 | 1 | 1 |
| agathisflavone | Human immunodeficiency virus 1 | IC50 | 100.0000 | 1 | 1 |
| amentoflavone | Human immunodeficiency virus 1 | IC50 | 119.0000 | 1 | 1 |
| hinokiflavone | Human immunodeficiency virus 1 | IC50 | 62.0000 | 1 | 1 |
| robustaflavone | Human immunodeficiency virus 1 | IC50 | 65.0000 | 1 | 1 |
| rosmarinic acid | Human immunodeficiency virus 1 | IC50 | 100.0000 | 1 | 1 |
| pecilocin | Human immunodeficiency virus 1 | IC50 | 200.0000 | 1 | 1 |
| cyclosporine | Human immunodeficiency virus 1 | IC50 | 0.4550 | 1 | 1 |
| dpc 083 | Human immunodeficiency virus 1 | IC50 | 0.0230 | 2 | 2 |
| 2-pyridinecarboxaldehyde-1-oxide-3,4-dimethoxybenzene sulfonylhydrazone | Human immunodeficiency virus 1 | IC50 | 100.0000 | 2 | 2 |
| s 1360 | Human immunodeficiency virus 1 | IC50 | 0.0200 | 1 | 1 |
| rilpivirine | Human immunodeficiency virus 1 | IC50 | 0.5721 | 19 | 20 |
| scy-635 | Human immunodeficiency virus 1 | IC50 | 0.0450 | 1 | 1 |
| 6-(1-(4-fluorophenyl)methyl-1h-pyrrol-2-yl)-2,4-dioxo-5-hexenoic acid ethyl ester | Human immunodeficiency virus 1 | IC50 | 10.1833 | 6 | 6 |
| synadenol | Human immunodeficiency virus 1 | IC50 | 57.0000 | 2 | 2 |
| nigranoic acid | Human immunodeficiency virus 1 | IC50 | 159.4000 | 1 | 1 |
| vrx-480773 | Human immunodeficiency virus 1 | IC50 | 0.0040 | 2 | 2 |
| halocynthiaxanthin | Human immunodeficiency virus 1 | IC50 | 7.2000 | 1 | 1 |
| ethidium homodimer | Human immunodeficiency virus 1 | IC50 | 3.6036 | 3 | 3 |
| gs-9148 | Human immunodeficiency virus 1 | IC50 | 1.9000 | 2 | 2 |
| mk 4965 | Human immunodeficiency virus 1 | IC50 | 0.0052 | 9 | 9 |
| mk 4965 | Human immunodeficiency virus 1 | Ki | 0.0004 | 5 | 5 |
| sch 725680 | Human immunodeficiency virus 1 | IC50 | 200.0000 | 1 | 1 |
| uk 453,061 | Human immunodeficiency virus 1 | IC50 | 0.1665 | 2 | 2 |
| uk 453,061 | Human immunodeficiency virus 1 | Ki | 0.1170 | 1 | 1 |
| nicousamide | Human immunodeficiency virus 1 | IC50 | 9.9000 | 1 | 1 |
| naproxen sodium | Human immunodeficiency virus 1 | IC50 | 6,700.0000 | 1 | 1 |
| raltegravir | Human immunodeficiency virus 1 | IC50 | 40.0000 | 6 | 6 |
| dolutegravir | Human immunodeficiency virus 1 | IC50 | 10.0000 | 3 | 3 |
| pinophilin b | Human immunodeficiency virus 1 | IC50 | 200.0000 | 1 | 1 |
| doravirine | Human immunodeficiency virus 1 | IC50 | 0.0315 | 2 | 2 |
| didanosine | Human immunodeficiency virus 1 | IC50 | 6.2600 | 2 | 2 |
| 2-hydroxy-1-naphthylaldehyde isonicotinoyl hydrazone | Human immunodeficiency virus 1 | IC50 | 100.0000 | 1 | 1 |
| 2-(methylthio)-6-(phenylmethyl)-1H-pyrimidin-4-one | Human immunodeficiency virus 1 | IC50 | 10.0000 | 1 | 1 |
| carbovir triphosphate | Human immunodeficiency virus 1 | IC50 | 1.1450 | 4 | 4 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| foscarnet | Human immunodeficiency virus 1 | Kd | 7.1500 | 2 | 2 |
| 6-(3,5-dimethylbenzyl)-1-(ethoxymethyl)-5-isopropyluracil | Human immunodeficiency virus 1 | EC50 | 0.0006 | 1 | 1 |
| loviride | Human immunodeficiency virus 1 | EC50 | 0.0130 | 1 | 1 |
| nevirapine | Human immunodeficiency virus 1 | EC50 | 5.9505 | 37 | 37 |
| 1-(ethoxymethyl)-5-isopropyl-6-(phenylsulfanyl)uracil | Human immunodeficiency virus 1 | EC50 | 0.0120 | 2 | 2 |
| delavirdine | Human immunodeficiency virus 1 | EC50 | 11.0253 | 3 | 3 |
| deoxycytidine | Human immunodeficiency virus 1 | Kd | 2.0500 | 2 | 2 |
| 2'-deoxyadenosine triphosphate | Human immunodeficiency virus 1 | Kd | 4.9286 | 7 | 7 |
| stavudine | Human immunodeficiency virus 1 | EC50 | 0.3333 | 3 | 3 |
| zalcitabine | Human immunodeficiency virus 1 | EC50 | 0.0310 | 1 | 1 |
| zidovudine | Human immunodeficiency virus 1 | EC50 | 1.0897 | 23 | 23 |
| zidovudine | Human immunodeficiency virus 1 | Kd | 0.0054 | 1 | 1 |
| lamivudine | Human immunodeficiency virus 1 | EC50 | 25.0210 | 2 | 2 |
| efavirenz | Human immunodeficiency virus 1 | EC50 | 0.0900 | 33 | 33 |
| thymidine 5'-triphosphate | Human immunodeficiency virus 1 | Kd | 34.5089 | 9 | 9 |
| calanolide a | Human immunodeficiency virus 1 | EC50 | 0.6450 | 1 | 2 |
| 1-((2-hydroxyethoxy)methyl)-6-(phenylthio)thymine | Human immunodeficiency virus 1 | EC50 | 7.0000 | 1 | 1 |
| 5-ethyl-1-ethoxymethyl-6-(phenylthio)uracil | Human immunodeficiency virus 1 | EC50 | 0.0190 | 2 | 2 |
| l-697661 | Human immunodeficiency virus 1 | EC50 | 0.0070 | 1 | 1 |
| 1-(2',5'-bis-o-(tert-butyldimethylsilylribofuranosyl)-3-n-methylthymine)-3'-spiro-5''-(4''-amino-1'',2''-oxathiole-2'',2''-dioxide) | Human immunodeficiency virus 1 | EC50 | 0.0500 | 2 | 2 |
| emivirine | Human immunodeficiency virus 1 | EC50 | 0.0076 | 4 | 4 |
| 2'-deoxycytidine 5'-triphosphate | Human immunodeficiency virus 1 | Kd | 1.7900 | 5 | 5 |
| 2',3'-dideoxyadenosine triphosphate | Human immunodeficiency virus 1 | Kd | 5.3000 | 1 | 1 |
| stavudine triphosphate | Human immunodeficiency virus 1 | Kd | 185.7600 | 5 | 5 |
| 2',3'-dideoxyadenosine 5'-phosphate | Human immunodeficiency virus 1 | Kd | 0.1000 | 1 | 1 |
| 3'-azido-3'-deoxythymidine 5'phosphate | Human immunodeficiency virus 1 | Kd | 4.1891 | 6 | 6 |
| zidovudine triphosphate | Human immunodeficiency virus 1 | Kd | 18.0771 | 7 | 7 |
| 5-ethyl-1-benzyloxymethyl-6-(phenylthio)uracil | Human immunodeficiency virus 1 | EC50 | 0.0059 | 2 | 2 |
| inophyllum b | Human immunodeficiency virus 1 | EC50 | 0.2253 | 1 | 1 |
| 2',3'-dideoxycytidine 5'-triphosphate | Human immunodeficiency virus 1 | Kd | 2.7000 | 1 | 1 |
| 1-(2',6'-difluorophenyl)-1h,3h-thiazolo(3,4-a)benzimidazole | Human immunodeficiency virus 1 | EC50 | 11.3643 | 14 | 14 |
| 6,6'-bieckol | Human immunodeficiency virus 1 | EC50 | 1.0700 | 1 | 1 |
| etravirine | Human immunodeficiency virus 1 | EC50 | 0.0140 | 19 | 19 |
| abacavir | Human immunodeficiency virus 1 | EC50 | 10.4000 | 2 | 2 |
| 9-(2-(phosphonomethoxy)ethyl)adenine diphosphate | Human immunodeficiency virus 1 | Kd | 7.8000 | 2 | 2 |
| TTP | Human immunodeficiency virus 1 | Kd | 2.5000 | 2 | 2 |
| e-ebu-dm | Human immunodeficiency virus 1 | EC50 | 0.0016 | 1 | 1 |
| lamivudine triphosphate | Human immunodeficiency virus 1 | Kd | 6.5375 | 8 | 8 |
| tenofovir | Human immunodeficiency virus 1 | Kd | 3.2000 | 1 | 1 |
| elvucitabine | Human immunodeficiency virus 1 | EC50 | 0.1600 | 2 | 2 |
| r 82150 | Human immunodeficiency virus 1 | EC50 | 0.0440 | 1 | 1 |
| r-82913 | Human immunodeficiency virus 1 | EC50 | 1.8977 | 3 | 3 |
| r 86183 | Human immunodeficiency virus 1 | EC50 | 0.0051 | 1 | 1 |
| trovirdine | Human immunodeficiency virus 1 | EC50 | 0.0200 | 1 | 1 |
| uc-781 | Human immunodeficiency virus 1 | EC50 | 0.0165 | 2 | 2 |
| 8,8'-bieckol | Human immunodeficiency virus 1 | EC50 | 0.5100 | 1 | 1 |
| tenofovir diphosphate | Human immunodeficiency virus 1 | Kd | 4.3000 | 1 | 1 |
| rilpivirine | Human immunodeficiency virus 1 | EC50 | 0.0016 | 3 | 3 |
| miv 150 | Human immunodeficiency virus 1 | Kd | 0.0020 | 8 | 8 |
| uk 453,061 | Human immunodeficiency virus 1 | Kd | 0.6240 | 1 | 1 |
| deoxyguanosine triphosphate | Human immunodeficiency virus 1 | Kd | 4.2000 | 2 | 2 |
| carbovir triphosphate | Human immunodeficiency virus 1 | Kd | 4.0000 | 1 | 1 |
Drugs with Other Measurements
Pharmacophore requirements for HIV-1 reverse transcriptase inhibitors that selectively "Freeze" the pre-translocated complex during the polymerization catalytic cycle.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
Modular assembly of purine-like bisphosphonates as inhibitors of HIV-1 reverse transcriptase.Journal of medicinal chemistry, , Sep-11, Volume: 57, Issue:17, 2014
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.The Journal of biological chemistry, , Mar-16, Volume: 282, Issue:11, 2007
The pyrophosphate analogue foscarnet traps the pre-translocational state of HIV-1 reverse transcriptase in a Brownian ratchet model of polymerase translocation.The Journal of biological chemistry, , Feb-02, Volume: 282, Issue:5, 2007
Hybrids of [TSAO-T]-[foscarnet]: The first conjugate of foscarnet with a non-nucleoside reverse transcriptase inhibitor through a labile covalent ester bond.Journal of medicinal chemistry, , Jun-17, Volume: 47, Issue:13, 2004
Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK.Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022
Structure-Based Discovery of Novel NHJournal of medicinal chemistry, , 06-23, Volume: 65, Issue:12, 2022
[no title available]Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.European journal of medicinal chemistry, , Dec-15, Volume: 226, 2021
Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.Journal of medicinal chemistry, , 07-22, Volume: 64, Issue:14, 2021
[no title available]European journal of medicinal chemistry, , Mar-15, Volume: 214, 2021
2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 NNRTIs: Rational Design, Synthesis, Activity Evaluation, and Crystallographic Studies.Journal of medicinal chemistry, , 04-08, Volume: 64, Issue:7, 2021
[no title available]Journal of medicinal chemistry, , 09-23, Volume: 64, Issue:18, 2021
Design of gp120 HIV-1 entry inhibitors by scaffold hopping via isosteric replacements.European journal of medicinal chemistry, , Nov-15, Volume: 224, 2021
Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high FspEuropean journal of medicinal chemistry, , Mar-05, Volume: 213, 2021
Covalent Inhibition of Wild-Type HIV-1 Reverse Transcriptase Using a Fluorosulfate Warhead.ACS medicinal chemistry letters, , Feb-11, Volume: 12, Issue:2, 2021
Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from Journal of medicinal chemistry, , 04-22, Volume: 64, Issue:8, 2021
HIV-1 gp120 Antagonists Also Inhibit HIV-1 Reverse Transcriptase by Bridging the NNRTI and NRTI Sites.Journal of medicinal chemistry, , 11-25, Volume: 64, Issue:22, 2021
Peptides Mimicking the β7/β8 Loop of HIV-1 Reverse Transcriptase p51 as "Hotspot-Targeted" Dimerization Inhibitors.ACS medicinal chemistry letters, , May-14, Volume: 11, Issue:5, 2020
Inhibition of HIV-1 RT activity by a new series of 3-(1,3,4-thiadiazol-2-yl)thiazolidin-4-one derivatives.Bioorganic & medicinal chemistry, , 04-15, Volume: 28, Issue:8, 2020
Fragment hopping-based discovery of novel sulfinylacetamide-diarylpyrimidines (DAPYs) as HIV-1 nonnucleoside reverse transcriptase inhibitors.European journal of medicinal chemistry, , Jan-01, Volume: 185, 2020
Discovery and Characterization of Fluorine-Substituted Diarylpyrimidine Derivatives as Novel HIV-1 NNRTIs with Highly Improved Resistance Profiles and Low Activity for the hERG Ion Channel.Journal of medicinal chemistry, , 02-13, Volume: 63, Issue:3, 2020
New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.European journal of medicinal chemistry, , Dec-15, Volume: 208, 2020
Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles.Journal of medicinal chemistry, , 12-26, Volume: 62, Issue:24, 2019
Design, synthesis and biological evaluation of novel acetamide-substituted doravirine and its prodrugs as potent HIV-1 NNRTIs.Bioorganic & medicinal chemistry, , 02-01, Volume: 27, Issue:3, 2019
The Journey of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) from Lab to Clinic.Journal of medicinal chemistry, , 05-23, Volume: 62, Issue:10, 2019
[no title available]European journal of medicinal chemistry, , Nov-15, Volume: 182, 2019
Aryl Substituted Benzimidazolones as Potent HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors.ACS medicinal chemistry letters, , Feb-14, Volume: 10, Issue:2, 2019
Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.Journal of medicinal chemistry, , 01-24, Volume: 62, Issue:2, 2019
Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors.European journal of medicinal chemistry, , Nov-15, Volume: 182, 2019
Synthesis and biological evaluation of dihydroquinazoline-2-amines as potent non-nucleoside reverse transcriptase inhibitors of wild-type and mutant HIV-1 strains.European journal of medicinal chemistry, , Aug-15, Volume: 176, 2019
[no title available]Journal of medicinal chemistry, , 02-28, Volume: 62, Issue:4, 2019
The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
Design and synthesis of a novel series of non-nucleoside HIV-1 inhibitors bearing pyrimidine and N-substituted aromatic piperazine.Bioorganic & medicinal chemistry letters, , 12-01, Volume: 28, Issue:22, 2018
Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery.ACS medicinal chemistry letters, , Apr-12, Volume: 9, Issue:4, 2018
Discovery of Novel Diarylpyrimidine Derivatives as Potent HIV-1 NNRTIs Targeting the "NNRTI Adjacent" Binding Site.ACS medicinal chemistry letters, , Apr-12, Volume: 9, Issue:4, 2018
Structural optimization of NBioorganic & medicinal chemistry, , 02-01, Volume: 26, Issue:3, 2018
Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1.European journal of medicinal chemistry, , Feb-10, Volume: 145, 2018
Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR.Bioorganic & medicinal chemistry, , 04-15, Volume: 25, Issue:8, 2017
Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives as potent HIV-1 NNRTIs.European journal of medicinal chemistry, , Nov-10, Volume: 140, 2017
Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.Journal of medicinal chemistry, , 05-25, Volume: 60, Issue:10, 2017
Discovery of Thiophene[3,2-ACS medicinal chemistry letters, , Nov-09, Volume: 8, Issue:11, 2017
Searching for novel NBioorganic & medicinal chemistry, , 07-15, Volume: 25, Issue:14, 2017
Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.Journal of medicinal chemistry, , 08-10, Volume: 60, Issue:15, 2017
Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach.Bioorganic & medicinal chemistry, , 09-15, Volume: 24, Issue:18, 2016
Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket.European journal of medicinal chemistry, , Jun-10, Volume: 115, 2016
Discovery and Structure-Based Optimization of 2-Ureidothiophene-3-carboxylic Acids as Dual Bacterial RNA Polymerase and Viral Reverse Transcriptase Inhibitors.Journal of medicinal chemistry, , Aug-11, Volume: 59, Issue:15, 2016
Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket.European journal of medicinal chemistry, , Feb-15, Volume: 109, 2016
Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket.European journal of medicinal chemistry, , Oct-04, Volume: 121, 2016
Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy.Bioorganic & medicinal chemistry, , 07-01, Volume: 24, Issue:13, 2016
1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus.Bioorganic & medicinal chemistry, , 06-01, Volume: 24, Issue:11, 2016
Discovery, characterization, and lead optimization of 7-azaindole non-nucleoside HIV-1 reverse transcriptase inhibitors.Bioorganic & medicinal chemistry letters, , 08-15, Volume: 26, Issue:16, 2016
Design, discovery, modelling, synthesis, and biological evaluation of novel and small, low toxicity s-triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors.Bioorganic & medicinal chemistry, , 06-01, Volume: 24, Issue:11, 2016
Development and in Vitro Evaluation of a Microbicide Gel Formulation for a Novel Non-Nucleoside Reverse Transcriptase Inhibitor Belonging to the N-Dihydroalkyloxybenzyloxopyrimidines (N-DABOs) Family.Journal of medicinal chemistry, , Mar-24, Volume: 59, Issue:6, 2016
Synthesis and biological evaluation of DAPY-DPEs hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase.Bioorganic & medicinal chemistry, , Feb-01, Volume: 23, Issue:3, 2015
Synthesis and biological evaluation of pyridinone analogues as novel potent HIV-1 NNRTIs.Bioorganic & medicinal chemistry, , Jan-01, Volume: 23, Issue:1, 2015
Hybrid chemistry. Part 4: Discovery of etravirine-VRX-480773 hybrids as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.Bioorganic & medicinal chemistry, , Aug-01, Volume: 23, Issue:15, 2015
Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 4: design, synthesis and biological evaluation of novel imidazo[1,2-a]pyrazines.European journal of medicinal chemistry, , Mar-26, Volume: 93, 2015
Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches.European journal of medicinal chemistry, , Mar-06, Volume: 92, 2015
Scaffold hopping: exploration of acetanilide-containing uracil analogues as potential NNRTIs.Bioorganic & medicinal chemistry, , Mar-01, Volume: 23, Issue:5, 2015
Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.European journal of medicinal chemistry, , Sep-18, Volume: 102, 2015
Anti-HIV diarylpyrimidine-quinolone hybrids and their mode of action.Bioorganic & medicinal chemistry, , Jul-01, Volume: 23, Issue:13, 2015
Discovery of piperidin-4-yl-aminopyrimidine derivatives as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.European journal of medicinal chemistry, , Jun-05, Volume: 97, 2015
A novel family of diarylpyrimidines (DAPYs) featuring a diatomic linker: Design, synthesis and anti-HIV activities.Bioorganic & medicinal chemistry, , Oct-15, Volume: 23, Issue:20, 2015
Exploiting the anti-HIV 6-desfluoroquinolones to design multiple ligands.Bioorganic & medicinal chemistry, , Sep-01, Volume: 22, Issue:17, 2014
Arylazolyl(azinyl)thioacetanilides. Part 16: Structure-based bioisosterism design, synthesis and biological evaluation of novel pyrimidinylthioacetanilides as potent HIV-1 inhibitors.Bioorganic & medicinal chemistry, , Oct-01, Volume: 22, Issue:19, 2014
Fused heterocyclic compounds bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 1: design, synthesis and biological evaluation of novel 5,7-disubstituted pyrazolo[1,5-a]pyrimidine derivatives.Bioorganic & medicinal chemistry, , Apr-01, Volume: 22, Issue:7, 2014
Design and synthesis of N₁-aryl-benzimidazoles 2-substituted as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.Bioorganic & medicinal chemistry, , Feb-15, Volume: 22, Issue:4, 2014
Design, synthesis and anti-HIV evaluation of novel diarylnicotinamide derivatives (DANAs) targeting the entrance channel of the NNRTI binding pocket through structure-guided molecular hybridization.European journal of medicinal chemistry, , Nov-24, Volume: 87, 2014
Discovery of 2-pyridone derivatives as potent HIV-1 NNRTIs using molecular hybridization based on crystallographic overlays.Bioorganic & medicinal chemistry, , Mar-15, Volume: 22, Issue:6, 2014
Design, synthesis and preliminary SAR studies of novel N-arylmethyl substituted piperidine-linked aniline derivatives as potent HIV-1 NNRTIs.Bioorganic & medicinal chemistry, , Jan-01, Volume: 22, Issue:1, 2014
Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.Journal of medicinal chemistry, , Dec-11, Volume: 57, Issue:23, 2014
Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes.Journal of medicinal chemistry, , Jun-26, Volume: 57, Issue:12, 2014
Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors.Bioorganic & medicinal chemistry, , Apr-15, Volume: 22, Issue:8, 2014
New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.European journal of medicinal chemistry, , Jun-10, Volume: 80, 2014
Novel piperidinylamino-diarylpyrimidine derivatives with dual structural conformations as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 23, Issue:24, 2013
Design, synthesis and biological evaluation of 3-benzyloxy-linked pyrimidinylphenylamine derivatives as potent HIV-1 NNRTIs.Bioorganic & medicinal chemistry, , Dec-01, Volume: 21, Issue:23, 2013
Phenylspirodrimanes with anti-HIV activity from the sponge-derived fungus Stachybotrys chartarum MXH-X73.Journal of natural products, , Dec-27, Volume: 76, Issue:12, 2013
Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors.European journal of medicinal chemistry, , Volume: 65, 2013
Cytotoxic, antitopoisomerase IIα, and anti-HIV-1 activities of triterpenoids isolated from leaves and twigs of Gardenia carinata.Journal of natural products, , Apr-26, Volume: 76, Issue:4, 2013
Novel pyridinone derivatives as non-nucleoside reverse transcriptase inhibitors (NNRTIs) with high potency against NNRTI-resistant HIV-1 strains.Journal of medicinal chemistry, , May-09, Volume: 56, Issue:9, 2013
Towards new C6-rigid S-DABO HIV-1 reverse transcriptase inhibitors: synthesis, biological investigation and molecular modeling studies.Bioorganic & medicinal chemistry, , Nov-01, Volume: 21, Issue:21, 2013
Design, synthesis and biological evaluation of N2,N4-disubstituted-1,1,3-trioxo-2H,4H-pyrrolo[1,2-b][1,2,4,6]thiatriazine derivatives as HIV-1 NNRTIs.Bioorganic & medicinal chemistry, , Nov-15, Volume: 21, Issue:22, 2013
Synthesis and biological evaluation of pyridazine derivatives as novel HIV-1 NNRTIs.Bioorganic & medicinal chemistry, , Apr-01, Volume: 21, Issue:7, 2013
N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase.Bioorganic & medicinal chemistry, , Mar-01, Volume: 21, Issue:5, 2013
Discovery of novel 2-(3-(2-chlorophenyl)pyrazin-2-ylthio)-N-arylacetamides as potent HIV-1 inhibitors using a structure-based bioisosterism approach.Bioorganic & medicinal chemistry, , Dec-01, Volume: 20, Issue:23, 2012
2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.Journal of medicinal chemistry, , Apr-12, Volume: 55, Issue:7, 2012
Structure-based bioisosterism design, synthesis and biological evaluation of novel 1,2,4-triazin-6-ylthioacetamides as potent HIV-1 NNRTIs.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 22, Issue:23, 2012
New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors.Journal of medicinal chemistry, , Jul-26, Volume: 55, Issue:14, 2012
Design, synthesis, and biological evaluation of 1-[(2-benzyloxyl/alkoxyl)methyl]-5-halo-6-aryluracils as potent HIV-1 non-nucleoside reverse transcriptase inhibitors with an improved drug resistance profile.Journal of medicinal chemistry, , Mar-08, Volume: 55, Issue:5, 2012
Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors.European journal of medicinal chemistry, , Volume: 51, 2012
Imidazo[1,2-a]pyridin-3-amines as potential HIV-1 non-nucleoside reverse transcriptase inhibitors.Bioorganic & medicinal chemistry, , Jul-15, Volume: 19, Issue:14, 2011
Synthesis and biological evaluation of novel 5-alkyl-2-arylthio-6-((3,4-dihydroquinolin-1(2H)-yl)methyl)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.Bioorganic & medicinal chemistry, , Jul-15, Volume: 19, Issue:14, 2011
Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.Journal of medicinal chemistry, , Apr-28, Volume: 54, Issue:8, 2011
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.Bioorganic & medicinal chemistry, , Oct-01, Volume: 19, Issue:19, 2011
Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors.European journal of medicinal chemistry, , Volume: 46, Issue:10, 2011
Enantioselective binding of second generation pyrrolobenzoxazepinones to the catalytic ternary complex of HIV-1 RT wild-type and L100I and K103N drug resistant mutants.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 21, Issue:13, 2011
Novel isatinyl thiosemicarbazones derivatives as potential molecule to combat HIV-TB co-infection.European journal of medicinal chemistry, , Volume: 46, Issue:1, 2011
Synthesis and biological evaluation of novel 2-arylalkylthio-4-amino-6-benzyl pyrimidines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.Bioorganic & medicinal chemistry letters, , May-01, Volume: 20, Issue:9, 2010
The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity.Antimicrobial agents and chemotherapy, , Volume: 54, Issue:6, 2010
Synthesis and biological evaluation of novel C5 halogen-functionalized S-DABO as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.Bioorganic & medicinal chemistry, , May-01, Volume: 18, Issue:9, 2010
Tricyclononene carboxamide derivatives as novel anti-HIV-1 agents.European journal of medicinal chemistry, , Volume: 45, Issue:9, 2010
Biomimetic synthesis and anti-HIV activity of dimeric phloroglucinols.Bioorganic & medicinal chemistry, , Mar-01, Volume: 18, Issue:5, 2010
Novel 1,3-dihydro-benzimidazol-2-ones and their analogues as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.Bioorganic & medicinal chemistry, , Feb-15, Volume: 18, Issue:4, 2010
Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants.Journal of medicinal chemistry, , Feb-12, Volume: 52, Issue:3, 2009
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.Antimicrobial agents and chemotherapy, , Volume: 53, Issue:6, 2009
Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.Antimicrobial agents and chemotherapy, , Volume: 53, Issue:11, 2009
Design, synthesis, and structure-activity relationships of 1,3-dihydrobenzimidazol-2-one analogues as anti-HIV agents.Bioorganic & medicinal chemistry, , Aug-15, Volume: 17, Issue:16, 2009
Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations.Journal of medicinal chemistry, , Feb-26, Volume: 52, Issue:4, 2009
Investigation of the alkenyldiarylmethane non-nucleoside reverse transcriptase inhibitors as potential cAMP phosphodiesterase-4B2 inhibitors.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 18, Issue:4, 2008
5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile.Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
Inhibition of tubulin polymerization by select alkenyldiarylmethanes.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 18, Issue:2, 2008
Virtual screening, identification, and biochemical characterization of novel inhibitors of the reverse transcriptase of human immunodeficiency virus type-1.Journal of medicinal chemistry, , Sep-25, Volume: 51, Issue:18, 2008
Novel N1-substituted 1,3-dihydro-2H-benzimidazol-2-ones as potent non-nucleoside reverse transcriptase inhibitors.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 17, Issue:7, 2007
Synthesis and anti-HIV studies of 2-adamantyl-substituted thiazolidin-4-ones.European journal of medicinal chemistry, , Volume: 42, Issue:7, 2007
De novo parallel design, synthesis and evaluation of inhibitors against the reverse transcriptase of human immunodeficiency virus type-1 and drug-resistant variants.Journal of medicinal chemistry, , May-17, Volume: 50, Issue:10, 2007
Development of a new methodology for screening of human immunodeficiency virus type 1 microbicides based on real-time PCR quantification.Antimicrobial agents and chemotherapy, , Volume: 51, Issue:2, 2007
The design and synthesis of N-1-alkylated-5-aminoarylalkylsubstituted-6-methyluracils as potential non-nucleoside HIV-1 RT inhibitors.Bioorganic & medicinal chemistry, , Dec-01, Volume: 15, Issue:23, 2007
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.The Journal of biological chemistry, , Mar-16, Volume: 282, Issue:11, 2007
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.Journal of medicinal chemistry, , Nov-01, Volume: 50, Issue:22, 2007
Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity.Journal of medicinal chemistry, , Oct-04, Volume: 50, Issue:20, 2007
Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 16, Issue:13, 2006
New HIV-1 reverse transcriptase inhibitors based on a tricyclic benzothiophene scaffold: synthesis, resolution, and inhibitory activity.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 16, Issue:11, 2006
Specific targeting highly conserved residues in the HIV-1 reverse transcriptase primer grip region. Design, synthesis, and biological evaluation of novel, potent, and broad spectrum NNRTIs with antiviral activity.Journal of medicinal chemistry, , Nov-17, Volume: 48, Issue:23, 2005
Parallel solution-phase and microwave-assisted synthesis of new S-DABO derivatives endowed with subnanomolar anti-HIV-1 activity.Journal of medicinal chemistry, , Dec-15, Volume: 48, Issue:25, 2005
Novel 1-[2-(diarylmethoxy)ethyl]-2-methyl-5-nitroimidazoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. A structure-activity relationship investigation.Journal of medicinal chemistry, , Jun-30, Volume: 48, Issue:13, 2005
Human immunodeficiency virus-reverse transcriptase inhibition and hepatitis C virus RNA-dependent RNA polymerase inhibition activities of fullerene derivatives.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 15, Issue:4, 2005
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.Journal of medicinal chemistry, , Feb-26, Volume: 47, Issue:5, 2004
Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 1.Journal of medicinal chemistry, , Nov-18, Volume: 47, Issue:24, 2004
5-Alkyl-2-[(aryl and alkyloxylcarbonylmethyl)thio]-6-(1-naphthylmethyl) pyrimidin-4(3H)-ones as an unique HIV reverse transcriptase inhibitors of S-DABO series.Bioorganic & medicinal chemistry letters, , Jun-21, Volume: 14, Issue:12, 2004
Design, synthesis, SAR, and molecular modeling studies of acylthiocarbamates: a novel series of potent non-nucleoside HIV-1 reverse transcriptase inhibitors structurally related to phenethylthiazolylthiourea derivatives.Journal of medicinal chemistry, , Feb-27, Volume: 46, Issue:5, 2003
Prediction of activity for nonnucleoside inhibitors with HIV-1 reverse transcriptase based on Monte Carlo simulations.Journal of medicinal chemistry, , Jul-04, Volume: 45, Issue:14, 2002
Estimation of binding affinities for HEPT and nevirapine analogues with HIV-1 reverse transcriptase via Monte Carlo simulations.Journal of medicinal chemistry, , Jan-18, Volume: 44, Issue:2, 2001
Structure-based design, synthesis, and biological evaluation of conformationally restricted novel 2-alkylthio-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.Journal of medicinal chemistry, , Aug-02, Volume: 44, Issue:16, 2001
Anti-HIV activity of aromatic and heterocyclic thiazolyl thiourea compounds.Bioorganic & medicinal chemistry letters, , Feb-26, Volume: 11, Issue:4, 2001
Antiviral drug design: computational analyses of the effects of the L100I mutation for HIV-RT on the binding of NNRTIs.Bioorganic & medicinal chemistry letters, , Nov-05, Volume: 11, Issue:21, 2001
Quinoxalinylethylpyridylthioureas (QXPTs) as potent non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors. Further SAR studies and identification of a novel orally bioavailable hydrazine-based antiviral agent.Journal of medicinal chemistry, , Feb-01, Volume: 44, Issue:3, 2001
Stereochemistry of halopyridyl and thiazolyl thiourea compounds is a major determinant of their potency as nonnucleoside inhibitors of HIV-1 reverse transcriptase.Bioorganic & medicinal chemistry letters, , Sep-18, Volume: 10, Issue:18, 2000
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.Journal of medicinal chemistry, , May-18, Volume: 43, Issue:10, 2000
Novel 2,2-dioxide-4,4-disubstituted-1,3-H-2,1,3-benzothiadiazines as non-nucleoside reverse transcriptase inhibitors.Bioorganic & medicinal chemistry letters, , Jan-17, Volume: 10, Issue:2, 2000
Synthesis and antiviral activity of 4-benzyl pyridinone derivatives as potent and selective non-nucleoside human immunodeficiency virus type 1 reverse transcriptase inhibitors.Journal of medicinal chemistry, , Oct-19, Volume: 43, Issue:21, 2000
Novel 1,5-diphenylpyrazole nonnucleoside HIV-1 reverse transcriptase inhibitors with enhanced activity versus the delavirdine-resistant P236L mutant: lead identification and SAR of 3- and 4-substituted derivatives.Journal of medicinal chemistry, , Mar-09, Volume: 43, Issue:5, 2000
N-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea and N'-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-chloropyridyl)]-thiourea as potent inhibitors of multidrug-resistant human immunodeficiency virus-1.Bioorganic & medicinal chemistry letters, , Sep-20, Volume: 9, Issue:18, 1999
N'-[2-(2-thiophene)ethyl]-N'-[2-(5-bromopyridyl)] thiourea as a potent inhibitor of NNI-resistant and multidrug-resistant human immunodeficiency virus-1.Bioorganic & medicinal chemistry letters, , Dec-20, Volume: 9, Issue:24, 1999
5-Alkyl-2-(alkylthio)-6-(2,6-dihalophenylmethyl)-3, 4-dihydropyrimidin-4(3H)-ones: novel potent and selective dihydro-alkoxy-benzyl-oxopyrimidine derivatives.Journal of medicinal chemistry, , Feb-25, Volume: 42, Issue:4, 1999
Rational design of N-[2-(2,5-dimethoxyphenylethyl)]-N'-[2-(5-bromopyridyl)]-thiourea (HI-236) as a potent non-nucleoside inhibitor of drug-resistant human immunodeficiency virus.Bioorganic & medicinal chemistry letters, , Jun-07, Volume: 9, Issue:11, 1999
Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues.Journal of medicinal chemistry, , Oct-07, Volume: 42, Issue:20, 1999
Pyrrolobenzoxazepinone derivatives as non-nucleoside HIV-1 RT inhibitors: further structure-activity relationship studies and identification of more potent broad-spectrum HIV-1 RT inhibitors with antiviral activity.Journal of medicinal chemistry, , Oct-21, Volume: 42, Issue:21, 1999
Synthesis and anti-HIV activities of urea-PETT analogs belonging to a new class of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.Bioorganic & medicinal chemistry letters, , Jun-16, Volume: 8, Issue:12, 1998
Novel nonnucleoside inhibitors of HIV-1 reverse transcriptase. 7. 8-Arylethyldipyridodiazepinones as potent broad-spectrum inhibitors of wild-type and mutant enzymes.Journal of medicinal chemistry, , Jul-30, Volume: 41, Issue:16, 1998
Novel nonnucleoside inhibitors of HIV-1 reverse transcriptase. 8. 8-Aryloxymethyl- and 8-arylthiomethyldipyridodiazepinones.Journal of medicinal chemistry, , Jul-30, Volume: 41, Issue:16, 1998
A dipyrido [2,3-b:3',2'-f]azepine analog of the HIV-1 reverse transcriptase inhibitor nevirapine.Bioorganic & medicinal chemistry letters, , Aug-18, Volume: 8, Issue:16, 1998
Dihydro(alkylthio)(naphthylmethyl)oxopyrimidines: novel non-nucleoside reverse transcriptase inhibitors of the S-DABO series.Journal of medicinal chemistry, , May-09, Volume: 40, Issue:10, 1997
Pyrrolobenzothiazepinones and pyrrolobenzoxazepinones: novel and specific non-nucleoside HIV-1 reverse transcriptase inhibitors with antiviral activity.Journal of medicinal chemistry, , Jul-05, Volume: 39, Issue:14, 1996
Phenethylthiazolylthiourea (PETT) compounds as a new class of HIV-1 reverse transcriptase inhibitors. 2. Synthesis and further structure-activity relationship studies of PETT analogs.Journal of medicinal chemistry, , Oct-11, Volume: 39, Issue:21, 1996
All-atom models for the non-nucleoside binding site of HIV-1 reverse transcriptase complexed with inhibitors: a 3D QSAR approach.Journal of medicinal chemistry, , Apr-12, Volume: 39, Issue:8, 1996
2-Sulfonyl-4-chloroanilino moiety: a potent pharmacophore for the anti-human immunodeficiency virus type 1 activity of pyrrolyl aryl sulfones.Journal of medicinal chemistry, , Jan-19, Volume: 39, Issue:2, 1996
Targeting delavirdine/atevirdine resistant HIV-1: identification of (alkylamino)piperidine-containing bis(heteroaryl)piperazines as broad spectrum HIV-1 reverse transcriptase inhibitors.Journal of medicinal chemistry, , Sep-13, Volume: 39, Issue:19, 1996
Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 3. Dipyrido[2,3-b:2',3'-e]diazepinones.Journal of medicinal chemistry, , Apr-14, Volume: 38, Issue:8, 1995
Novel non-nucleoside inhibitors of human immunodeficiency virus type 1 reverse transcriptase. 5. 4-Substituted and 2,4-disubstituted analogs of nevirapine.Journal of medicinal chemistry, , Nov-24, Volume: 38, Issue:24, 1995
Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors. 1. Synthesis and basic structure-activity relationship studies of PETT analogs.Journal of medicinal chemistry, , Dec-08, Volume: 38, Issue:25, 1995
Novel non-nucleoside inhibitors of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase. 4. 2-Substituted dipyridodiazepinones as potent inhibitors of both wild-type and cysteine-181 HIV-1 reverse transcriptase enzymes.Journal of medicinal chemistry, , Nov-24, Volume: 38, Issue:24, 1995
Synthesis of a series of 4-(arylethynyl)-6-chloro-4-cyclopropyl-3,4-dihydroquinazolin-2(1H)-ones as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.Journal of medicinal chemistry, , Jul-22, Volume: 37, Issue:15, 1994
Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-carbonyl]-4-[3- [(1-methylethyl)amino]-pyridinyl]piJournal of medicinal chemistry, , May-14, Volume: 36, Issue:10, 1993
Non-nucleoside inhibitors of HIV-1 reverse transcriptase: molecular modeling and X-ray structure investigations.Journal of medicinal chemistry, , Mar-19, Volume: 36, Issue:6, 1993
Selective non-nucleoside HIV-1 reverse transcriptase inhibitors. New 2,3-dihydrothiazolo[2,3-a]isoindol-5(9bH)-ones and related compounds with anti-HIV-1 activity.Journal of medicinal chemistry, , Aug-20, Volume: 36, Issue:17, 1993
Synthesis and evaluation of 2-pyridinone derivatives as specific HIV-1 reverse transcriptase inhibitors. 3. Pyridyl and phenyl analogs of 3-aminopyridin-2(1H)-one.Journal of medicinal chemistry, , Jan-22, Volume: 36, Issue:2, 1993
Synthesis and anti-HIV-1 activity of a series of imidazo[1,5-b]pyridazines.Journal of medicinal chemistry, , Nov-26, Volume: 36, Issue:24, 1993
Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 1. Tricyclic pyridobenzo- and dipyridodiazepinones.Journal of medicinal chemistry, , Volume: 34, Issue:7, 1991
Design, synthesis, structure-activity relationships, and molecular modeling studies of 2,3-diaryl-1,3-thiazolidin-4-ones as potent anti-HIV agents.Journal of medicinal chemistry, , Nov-21, Volume: 45, Issue:24, 2002
Prediction of activity for nonnucleoside inhibitors with HIV-1 reverse transcriptase based on Monte Carlo simulations.Journal of medicinal chemistry, , Jul-04, Volume: 45, Issue:14, 2002
Estimation of binding affinities for HEPT and nevirapine analogues with HIV-1 reverse transcriptase via Monte Carlo simulations.Journal of medicinal chemistry, , Jan-18, Volume: 44, Issue:2, 2001
A 3D QSAR study of a series of HEPT analogues: the influence of conformational mobility on HIV-1 reverse transcriptase inhibition.Journal of medicinal chemistry, , Dec-19, Volume: 40, Issue:26, 1997
The Journey of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) from Lab to Clinic.Journal of medicinal chemistry, , 05-23, Volume: 62, Issue:10, 2019
Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR.Bioorganic & medicinal chemistry, , 04-15, Volume: 25, Issue:8, 2017
Advances in rationally designed dual inhibitors of HIV-1 reverse transcriptase and integrase.Bioorganic & medicinal chemistry, , 11-01, Volume: 24, Issue:21, 2016
Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors.European journal of medicinal chemistry, , Volume: 65, 2013
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.Journal of medicinal chemistry, , Feb-26, Volume: 47, Issue:5, 2004
Synthesis, biological evaluation, and binding mode of novel 1-[2-(diarylmethoxy)ethyl]-2-methyl-5-nitroimidazoles targeted at the HIV-1 reverse transcriptase.Journal of medicinal chemistry, , Apr-11, Volume: 45, Issue:8, 2002
Stereochemistry of halopyridyl and thiazolyl thiourea compounds is a major determinant of their potency as nonnucleoside inhibitors of HIV-1 reverse transcriptase.Bioorganic & medicinal chemistry letters, , Sep-18, Volume: 10, Issue:18, 2000
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.Journal of medicinal chemistry, , May-18, Volume: 43, Issue:10, 2000
N-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea and N'-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-chloropyridyl)]-thiourea as potent inhibitors of multidrug-resistant human immunodeficiency virus-1.Bioorganic & medicinal chemistry letters, , Sep-20, Volume: 9, Issue:18, 1999
N'-[2-(2-thiophene)ethyl]-N'-[2-(5-bromopyridyl)] thiourea as a potent inhibitor of NNI-resistant and multidrug-resistant human immunodeficiency virus-1.Bioorganic & medicinal chemistry letters, , Dec-20, Volume: 9, Issue:24, 1999
Rational design of N-[2-(2,5-dimethoxyphenylethyl)]-N'-[2-(5-bromopyridyl)]-thiourea (HI-236) as a potent non-nucleoside inhibitor of drug-resistant human immunodeficiency virus.Bioorganic & medicinal chemistry letters, , Jun-07, Volume: 9, Issue:11, 1999
Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues.Journal of medicinal chemistry, , Oct-07, Volume: 42, Issue:20, 1999
Synthesis and structure-activity relationships of the (alkylamino)piperidine-containing BHAP class of non-nucleoside reverse transcriptase inhibitors: effect of 3-alkylpyridine ring substitution.Journal of medicinal chemistry, , Oct-07, Volume: 42, Issue:20, 1999
Pyrimidine thioethers: a novel class of HIV-1 reverse transcriptase inhibitors with activity against BHAP-resistant HIV.Journal of medicinal chemistry, , Sep-24, Volume: 41, Issue:20, 1998
(-)-6-Chloro-2-[(1-furo[2, 3-c]pyridin-5-ylethyl)thio]-4-pyrimidinamine, PNU-142721, a new broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitor.Journal of medicinal chemistry, , Apr-23, Volume: 41, Issue:9, 1998
Synthesis and bioactivity of novel bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships and increased metabolic stability of novel substituted pyridine analogs.Journal of medicinal chemistry, , Dec-20, Volume: 39, Issue:26, 1996
Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-carbonyl]-4-[3- [(1-methylethyl)amino]-pyridinyl]piJournal of medicinal chemistry, , May-14, Volume: 36, Issue:10, 1993
Pre-steady state kinetic analysis of cyclobutyl derivatives of 2'-deoxyadenosine 5'-triphosphate as inhibitors of HIV-1 reverse transcriptase.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 22, Issue:12, 2012
Synopsis of some recent tactical application of bioisosteres in drug design.Journal of medicinal chemistry, , Apr-28, Volume: 54, Issue:8, 2011
Synthesis, antiviral activity, cytotoxicity and cellular pharmacology of l-3'-azido-2',3'-dideoxypurine nucleosides.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
Anti-human immunodeficiency virus activity, cross-resistance, cytotoxicity, and intracellular pharmacology of the 3'-azido-2',3'-dideoxypurine nucleosides.Antimicrobial agents and chemotherapy, , Volume: 53, Issue:9, 2009
In vitro suppression of K65R reverse transcriptase-mediated tenofovir- and adefovir-5'-diphosphate resistance conferred by the boranophosphonate derivatives.Antimicrobial agents and chemotherapy, , Volume: 51, Issue:9, 2007
Inhibition of human immunodeficiency virus reverse transcriptase by synadenol triphosphate and its E-isomer.Journal of medicinal chemistry, , Oct-23, Volume: 46, Issue:22, 2003
[d4U]-spacer-[HI-236] double-drug inhibitors of HIV-1 reverse-transcriptase.Bioorganic & medicinal chemistry, , Jul-01, Volume: 18, Issue:13, 2010
Synthesis, anti-HIV activity, and resistance profile of thymidine phosphonomethoxy nucleosides and their bis-isopropyloxymethylcarbonyl (bisPOC) prodrugs.Bioorganic & medicinal chemistry, , Aug-15, Volume: 15, Issue:16, 2007
The role of 2',3'-unsaturation on the antiviral activity of anti-HIV nucleosides against 3TC-resistant mutant (M184V).Bioorganic & medicinal chemistry letters, , Jun-16, Volume: 13, Issue:12, 2003
1,3-dihydrobenzo[c]furan nucleoside analogues: additional studies of the thymine derivative.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 13, Issue:24, 2003
Synthesis and anti-HIV evaluation of D4T and D4T 5'-monophosphate prodrugs.Journal of medicinal chemistry, , Apr-02, Volume: 36, Issue:7, 1993
Synthesis of 2',3'-dideoxynucleoside 5'-alpha-P-borano-beta,gamma-(difluoromethylene)triphosphates and their inhibition of HIV-1 reverse transcriptase.Journal of medicinal chemistry, , Apr-07, Volume: 48, Issue:7, 2005
Synthesis and evaluation of "AZT-HEPT", "AZT-pyridinone", and "ddC-HEPT" conjugates as inhibitors of HIV reverse transcriptase.Journal of medicinal chemistry, , May-18, Volume: 43, Issue:10, 2000
3',3'-Difluoro-3'-deoxythymidine: comparison of anti-HIV activity to 3'-fluoro-3'-deoxythymidine.Journal of medicinal chemistry, , Sep-04, Volume: 35, Issue:18, 1992
3'-Fluoro-2',3'-dideoxy-5-chlorouridine: most selective anti-HIV-1 agent among a series of new 2'- and 3'-fluorinated 2',3'-dideoxynucleoside analogues.Journal of medicinal chemistry, , Volume: 32, Issue:8, 1989
The Journey of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) from Lab to Clinic.Journal of medicinal chemistry, , 05-23, Volume: 62, Issue:10, 2019
Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery.ACS medicinal chemistry letters, , Apr-12, Volume: 9, Issue:4, 2018
Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR.Bioorganic & medicinal chemistry, , 04-15, Volume: 25, Issue:8, 2017
Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.Journal of medicinal chemistry, , 05-25, Volume: 60, Issue:10, 2017
Synthesis of tetracyclic iminosugars fused benzo[e][1,3]thiazin-4-one and their HIV-RT inhibitory activity.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 26, Issue:7, 2016
Synthesis of bi-/tricyclic azasugars fused thiazinan-4-one and their HIV-RT inhibitory activity.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 24, Issue:15, 2014
Clicking 3'-azidothymidine into novel potent inhibitors of human immunodeficiency virus.Journal of medicinal chemistry, , Nov-14, Volume: 56, Issue:21, 2013
Synthesis and evaluation of coumarin derivatives as potential dual-action HIV-1 protease and reverse transcriptase inhibitors.Bioorganic & medicinal chemistry, , Apr-01, Volume: 21, Issue:7, 2013
Synthetic bicyclic iminosugar derivatives fused thiazolidin-4-one as new potential HIV-RT inhibitors.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 22, Issue:23, 2012
Synthesis and biological activity of novel 5'-arylamino-nucleosides by microwave-assisted one-pot tandem Staudinger/aza-Wittig/reduction.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 21, Issue:1, 2011
The nucleoside analogue D-carba T blocks HIV-1 reverse transcription.Journal of medicinal chemistry, , Sep-10, Volume: 52, Issue:17, 2009
Design, synthesis, and anti-HIV activity of 4'-modified carbocyclic nucleoside phosphonate reverse transcriptase inhibitors.Bioorganic & medicinal chemistry, , Feb-15, Volume: 17, Issue:4, 2009
Synthesis and anti-HIV activity of GS-9148 (2'-Fd4AP), a novel nucleoside phosphonate HIV reverse transcriptase inhibitor.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 18, Issue:3, 2008
Synthesis, anti-HIV activity, and resistance profile of thymidine phosphonomethoxy nucleosides and their bis-isopropyloxymethylcarbonyl (bisPOC) prodrugs.Bioorganic & medicinal chemistry, , Aug-15, Volume: 15, Issue:16, 2007
Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 16, Issue:13, 2006
Identification of a novel family of nucleosides that specifically inhibit HIV-1 reverse transcriptase.Bioorganic & medicinal chemistry letters, , Dec-03, Volume: 11, Issue:23, 2001
Synthesis and evaluation of "AZT-HEPT", "AZT-pyridinone", and "ddC-HEPT" conjugates as inhibitors of HIV reverse transcriptase.Journal of medicinal chemistry, , May-18, Volume: 43, Issue:10, 2000
Antioxidant function of phenethyl-5-bromo-pyridyl thiourea compounds with potent anti-HIV activity.Bioorganic & medicinal chemistry letters, , Jan-03, Volume: 10, Issue:1, 2000
Syntheses of 4'-C-ethynyl-beta-D-arabino- and 4'-C-ethynyl-2'-deoxy-beta-D-ribo-pentofuranosylpyrimidines and -purines and evaluation of their anti-HIV activity.Journal of medicinal chemistry, , Nov-16, Volume: 43, Issue:23, 2000
N'-[2-(2-thiophene)ethyl]-N'-[2-(5-bromopyridyl)] thiourea as a potent inhibitor of NNI-resistant and multidrug-resistant human immunodeficiency virus-1.Bioorganic & medicinal chemistry letters, , Dec-20, Volume: 9, Issue:24, 1999
5-Alkyl-2-[(methylthiomethyl)thio]-6-(benzyl)-pyrimidin-4-(1H)-ones as potent non-nucleoside reverse transcriptase inhibitors of S-DABO series.Bioorganic & medicinal chemistry letters, , Jun-16, Volume: 8, Issue:12, 1998
Design, synthesis, and antiviral evaluations of 1-(substituted benzyl)-2-substituted-5,6-dichlorobenzimidazoles as nonnucleoside analogues of 2,5,6-trichloro-1-(beta-D-ribofuranosyl)benzimidazole.Journal of medicinal chemistry, , Apr-09, Volume: 41, Issue:8, 1998
(Z)- and (E)-2-((hydroxymethyl)cyclopropylidene)methyladenine and -guanine. New nucleoside analogues with a broad-spectrum antiviral activity.Journal of medicinal chemistry, , Jan-01, Volume: 41, Issue:1, 1998
Preparation and anti-HIV activity of N-3-substituted thymidine nucleoside analogs.Journal of medicinal chemistry, , May-09, Volume: 40, Issue:10, 1997
Synthesis and antiproliferative and antiviral activity of 2'-deoxy-2'-fluoroarabinofuranosyl analogs of the nucleoside antibiotics toyocamycin and sangivamycin.Journal of medicinal chemistry, , Sep-29, Volume: 38, Issue:20, 1995
Anti-human immunodeficiency virus and anti-hepatitis-B virus activities and toxicities of the enantiomers of 2'-deoxy-3'-oxa-4'-thiocytidine and their 5-fluoro analogues in vitro.Journal of medicinal chemistry, , Jan-06, Volume: 38, Issue:1, 1995
Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors. 1. Synthesis and basic structure-activity relationship studies of PETT analogs.Journal of medicinal chemistry, , Dec-08, Volume: 38, Issue:25, 1995
Mechanistic evaluation of new plant-derived compounds that inhibit HIV-1 reverse transcriptase.Journal of natural products, , Volume: 58, Issue:7, 1995
Synthesis, in vitro biological stability, and anti-HIV activity of 5-halo-6-alkoxy(or azido)-5,6-dihydro-3'-azido-3'-deoxythymidine diastereomers as potential prodrugs to 3'-azido-3'-deoxythymidine (AZT).Journal of medicinal chemistry, , Dec-09, Volume: 37, Issue:25, 1994
Synthesis and anti-HIV evaluation of D4T and D4T 5'-monophosphate prodrugs.Journal of medicinal chemistry, , Apr-02, Volume: 36, Issue:7, 1993
Synthesis and anti-HIV-1 activity of a series of imidazo[1,5-b]pyridazines.Journal of medicinal chemistry, , Nov-26, Volume: 36, Issue:24, 1993
3',3'-Difluoro-3'-deoxythymidine: comparison of anti-HIV activity to 3'-fluoro-3'-deoxythymidine.Journal of medicinal chemistry, , Sep-04, Volume: 35, Issue:18, 1992
Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 1. Tricyclic pyridobenzo- and dipyridodiazepinones.Journal of medicinal chemistry, , Volume: 34, Issue:7, 1991
Activity of acyclic 6-(phenylselenenyl)pyrimidine nucleosides against human immunodeficiency viruses in primary lymphocytes.Journal of medicinal chemistry, , Volume: 34, Issue:11, 1991
3'-Fluoro-2',3'-dideoxy-5-chlorouridine: most selective anti-HIV-1 agent among a series of new 2'- and 3'-fluorinated 2',3'-dideoxynucleoside analogues.Journal of medicinal chemistry, , Volume: 32, Issue:8, 1989
6-N-Acyltriciribine analogues: structure-activity relationship between acyl carbon chain length and activity against HIV-1.Journal of medicinal chemistry, , Jun-15, Volume: 43, Issue:12, 2000
Deoxy sugar analogues of triciribine: correlation of antiviral and antiproliferative activity with intracellular phosphorylation.Journal of medicinal chemistry, , Jun-15, Volume: 43, Issue:12, 2000
Synthesis and evaluation of 2-pyridinone derivatives as HIV-1-specific reverse transcriptase inhibitors. 2. Analogues of 3-aminopyridin-2(1H)-one.Journal of medicinal chemistry, , Oct-16, Volume: 35, Issue:21, 1992
2-Pyridinone derivatives: a new class of nonnucleoside, HIV-1-specific reverse transcriptase inhibitors.Journal of medicinal chemistry, , Volume: 34, Issue:9, 1991
Synthesis of potent antitumor and antiviral benzofuran derivatives.Bioorganic & medicinal chemistry letters, , May-01, Volume: 19, Issue:9, 2009
Synthesis and bioactivity of novel bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships and increased metabolic stability of novel substituted pyridine analogs.Journal of medicinal chemistry, , Dec-20, Volume: 39, Issue:26, 1996
Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-carbonyl]-4-[3- [(1-methylethyl)amino]-pyridinyl]piJournal of medicinal chemistry, , May-14, Volume: 36, Issue:10, 1993
Selective non-nucleoside HIV-1 reverse transcriptase inhibitors. New 2,3-dihydrothiazolo[2,3-a]isoindol-5(9bH)-ones and related compounds with anti-HIV-1 activity.Journal of medicinal chemistry, , Aug-20, Volume: 36, Issue:17, 1993
Synthesis and evaluation of 2-pyridinone derivatives as specific HIV-1 reverse transcriptase inhibitors. 3. Pyridyl and phenyl analogs of 3-aminopyridin-2(1H)-one.Journal of medicinal chemistry, , Jan-22, Volume: 36, Issue:2, 1993
Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK.Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022
Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features.European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022
Structure-Based Discovery of Novel NHJournal of medicinal chemistry, , 06-23, Volume: 65, Issue:12, 2022
Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.European journal of medicinal chemistry, , Dec-15, Volume: 226, 2021
Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.Journal of medicinal chemistry, , 07-22, Volume: 64, Issue:14, 2021
[no title available]European journal of medicinal chemistry, , Mar-15, Volume: 214, 2021
Novel indolylarylsulfone derivatives as covalent HIV-1 reverse transcriptase inhibitors specifically targeting the drug-resistant mutant Y181C.Bioorganic & medicinal chemistry, , 01-15, Volume: 30, 2021
Design and biological evaluation of cinnamic and phenylpropionic amide derivatives as novel dual inhibitors of HIV-1 protease and reverse transcriptase.European journal of medicinal chemistry, , Aug-05, Volume: 220, 2021
Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high FspEuropean journal of medicinal chemistry, , Mar-05, Volume: 213, 2021
Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from Journal of medicinal chemistry, , 04-22, Volume: 64, Issue:8, 2021
Quinolinonyl Non-Diketo Acid Derivatives as Inhibitors of HIV-1 Ribonuclease H and Polymerase Functions of Reverse Transcriptase.Journal of medicinal chemistry, , 06-24, Volume: 64, Issue:12, 2021
Rational design and Structure-Activity relationship of coumarin derivatives effective on HIV-1 protease and partially on HIV-1 reverse transcriptase.European journal of medicinal chemistry, , Jan-15, Volume: 186, 2020
Fragment hopping-based discovery of novel sulfinylacetamide-diarylpyrimidines (DAPYs) as HIV-1 nonnucleoside reverse transcriptase inhibitors.European journal of medicinal chemistry, , Jan-01, Volume: 185, 2020
New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.European journal of medicinal chemistry, , Dec-15, Volume: 208, 2020
Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles.Journal of medicinal chemistry, , 12-26, Volume: 62, Issue:24, 2019
Design, synthesis and biological evaluation of novel acetamide-substituted doravirine and its prodrugs as potent HIV-1 NNRTIs.Bioorganic & medicinal chemistry, , 02-01, Volume: 27, Issue:3, 2019
[no title available]European journal of medicinal chemistry, , Nov-15, Volume: 182, 2019
Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.Journal of medicinal chemistry, , 01-24, Volume: 62, Issue:2, 2019
Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors.European journal of medicinal chemistry, , Nov-15, Volume: 182, 2019
Synthesis and biological evaluation of dihydroquinazoline-2-amines as potent non-nucleoside reverse transcriptase inhibitors of wild-type and mutant HIV-1 strains.European journal of medicinal chemistry, , Aug-15, Volume: 176, 2019
The Journey of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) from Lab to Clinic.Journal of medicinal chemistry, , 05-23, Volume: 62, Issue:10, 2019
[no title available]Journal of medicinal chemistry, , 02-28, Volume: 62, Issue:4, 2019
Advances in diarylpyrimidines and related analogues as HIV-1 nonnucleoside reverse transcriptase inhibitors.European journal of medicinal chemistry, , Oct-05, Volume: 158, 2018
Design and synthesis of a novel series of non-nucleoside HIV-1 inhibitors bearing pyrimidine and N-substituted aromatic piperazine.Bioorganic & medicinal chemistry letters, , 12-01, Volume: 28, Issue:22, 2018
The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery.ACS medicinal chemistry letters, , Apr-12, Volume: 9, Issue:4, 2018
Discovery of Novel Diarylpyrimidine Derivatives as Potent HIV-1 NNRTIs Targeting the "NNRTI Adjacent" Binding Site.ACS medicinal chemistry letters, , Apr-12, Volume: 9, Issue:4, 2018
Design, synthesis, docking studies and biological screening of 2-thiazolyl substituted -2,3-dihydro-1H-naphtho[1,2-e][1,3]oxazines as potent HIV-1 reverse transcriptase inhibitors.European journal of medicinal chemistry, , Sep-05, Volume: 157, 2018
Structural optimization of NBioorganic & medicinal chemistry, , 02-01, Volume: 26, Issue:3, 2018
Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1.European journal of medicinal chemistry, , Feb-10, Volume: 145, 2018
Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR.Bioorganic & medicinal chemistry, , 04-15, Volume: 25, Issue:8, 2017
Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives as potent HIV-1 NNRTIs.European journal of medicinal chemistry, , Nov-10, Volume: 140, 2017
Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.Journal of medicinal chemistry, , 05-25, Volume: 60, Issue:10, 2017
Searching for novel NBioorganic & medicinal chemistry, , 07-15, Volume: 25, Issue:14, 2017
Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.Journal of medicinal chemistry, , 08-10, Volume: 60, Issue:15, 2017
Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.Journal of medicinal chemistry, , 09-08, Volume: 59, Issue:17, 2016
Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket.European journal of medicinal chemistry, , Oct-04, Volume: 121, 2016
Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy.Bioorganic & medicinal chemistry, , 07-01, Volume: 24, Issue:13, 2016
1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus.Bioorganic & medicinal chemistry, , 06-01, Volume: 24, Issue:11, 2016
Discovery, characterization, and lead optimization of 7-azaindole non-nucleoside HIV-1 reverse transcriptase inhibitors.Bioorganic & medicinal chemistry letters, , 08-15, Volume: 26, Issue:16, 2016
Efavirenz a nonnucleoside reverse transcriptase inhibitor of first-generation: Approaches based on its medicinal chemistry.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Novel (2,6-difluorophenyl)(2-(phenylamino)pyrimidin-4-yl)methanones with restricted conformation as potent non-nucleoside reverse transcriptase inhibitors against HIV-1.European journal of medicinal chemistry, , Oct-21, Volume: 122, 2016
Synthesis and biological evaluation of DAPY-DPEs hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase.Bioorganic & medicinal chemistry, , Feb-01, Volume: 23, Issue:3, 2015
Hybrid chemistry. Part 4: Discovery of etravirine-VRX-480773 hybrids as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.Bioorganic & medicinal chemistry, , Aug-01, Volume: 23, Issue:15, 2015
(3Z)-3-(2-[4-(aryl)-1,3-thiazol-2-yl]hydrazin-1-ylidene)-2,3-dihydro-1H-indol-2-one derivatives as dual inhibitors of HIV-1 reverse transcriptase.European journal of medicinal chemistry, , Mar-26, Volume: 93, 2015
Scaffold hopping: exploration of acetanilide-containing uracil analogues as potential NNRTIs.Bioorganic & medicinal chemistry, , Mar-01, Volume: 23, Issue:5, 2015
Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.European journal of medicinal chemistry, , Sep-18, Volume: 102, 2015
Anti-HIV diarylpyrimidine-quinolone hybrids and their mode of action.Bioorganic & medicinal chemistry, , Jul-01, Volume: 23, Issue:13, 2015
Discovery of piperidin-4-yl-aminopyrimidine derivatives as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.European journal of medicinal chemistry, , Jun-05, Volume: 97, 2015
A novel family of diarylpyrimidines (DAPYs) featuring a diatomic linker: Design, synthesis and anti-HIV activities.Bioorganic & medicinal chemistry, , Oct-15, Volume: 23, Issue:20, 2015
Design and synthesis of N₁-aryl-benzimidazoles 2-substituted as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.Bioorganic & medicinal chemistry, , Feb-15, Volume: 22, Issue:4, 2014
Design, synthesis and anti-HIV evaluation of novel diarylnicotinamide derivatives (DANAs) targeting the entrance channel of the NNRTI binding pocket through structure-guided molecular hybridization.European journal of medicinal chemistry, , Nov-24, Volume: 87, 2014
Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.Journal of medicinal chemistry, , Dec-11, Volume: 57, Issue:23, 2014
Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes.Journal of medicinal chemistry, , Jun-26, Volume: 57, Issue:12, 2014
Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors.Bioorganic & medicinal chemistry, , Apr-15, Volume: 22, Issue:8, 2014
New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.European journal of medicinal chemistry, , Jun-10, Volume: 80, 2014
Novel piperidinylamino-diarylpyrimidine derivatives with dual structural conformations as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 23, Issue:24, 2013
Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors.European journal of medicinal chemistry, , Volume: 65, 2013
Towards new C6-rigid S-DABO HIV-1 reverse transcriptase inhibitors: synthesis, biological investigation and molecular modeling studies.Bioorganic & medicinal chemistry, , Nov-01, Volume: 21, Issue:21, 2013
N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase.Bioorganic & medicinal chemistry, , Mar-01, Volume: 21, Issue:5, 2013
2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.Journal of medicinal chemistry, , Apr-12, Volume: 55, Issue:7, 2012
Identification of HIV-1 reverse transcriptase dual inhibitors by a combined shape-, 2D-fingerprint- and pharmacophore-based virtual screening approach.European journal of medicinal chemistry, , Volume: 50, 2012
New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors.Journal of medicinal chemistry, , Jul-26, Volume: 55, Issue:14, 2012
Novel diarylpyridinones, diarylpyridazinones and diarylphthalazinones as potential HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs).Bioorganic & medicinal chemistry, , Oct-15, Volume: 19, Issue:20, 2011
Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.Journal of medicinal chemistry, , Apr-28, Volume: 54, Issue:8, 2011
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.Bioorganic & medicinal chemistry, , Oct-01, Volume: 19, Issue:19, 2011
Biaryl ethers as potent allosteric inhibitors of reverse transcriptase and its key mutant viruses: aryl substituted pyrazole as a surrogate for the pyrazolopyridine motif.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 20, Issue:15, 2010
The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity.Antimicrobial agents and chemotherapy, , Volume: 54, Issue:6, 2010
Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.Antimicrobial agents and chemotherapy, , Volume: 54, Issue:10, 2010
Novel 1,3-dihydro-benzimidazol-2-ones and their analogues as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.Bioorganic & medicinal chemistry, , Feb-15, Volume: 18, Issue:4, 2010
Parallel synthesis, molecular modelling and further structure-activity relationship studies of new acylthiocarbamates as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.European journal of medicinal chemistry, , Volume: 44, Issue:5, 2009
Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants.Journal of medicinal chemistry, , Feb-12, Volume: 52, Issue:3, 2009
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.Antimicrobial agents and chemotherapy, , Volume: 53, Issue:6, 2009
Novel indazole non-nucleoside reverse transcriptase inhibitors using molecular hybridization based on crystallographic overlays.Journal of medicinal chemistry, , Feb-26, Volume: 52, Issue:4, 2009
Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.Antimicrobial agents and chemotherapy, , Volume: 53, Issue:11, 2009
Design, synthesis, and structure-activity relationships of 1,3-dihydrobenzimidazol-2-one analogues as anti-HIV agents.Bioorganic & medicinal chemistry, , Aug-15, Volume: 17, Issue:16, 2009
Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations.Journal of medicinal chemistry, , Feb-26, Volume: 52, Issue:4, 2009
5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile.Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
Discovery and optimization of pyridazinone non-nucleoside inhibitors of HIV-1 reverse transcriptase.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 18, Issue:15, 2008
Parallel one-pot synthesis and structure-activity relationship study of symmetric formimidoester disulfides as a novel class of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.Bioorganic & medicinal chemistry, , Jun-15, Volume: 16, Issue:12, 2008
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.Journal of medicinal chemistry, , Oct-23, Volume: 51, Issue:20, 2008
Thiocarbamates as non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 2: Parallel synthesis, molecular modelling and structure-activity relationship studies on analogues of O-(2-phenylethyl)-N-phenylthiocarbamate.Bioorganic & medicinal chemistry, , Apr-01, Volume: 16, Issue:7, 2008
Novel N1-substituted 1,3-dihydro-2H-benzimidazol-2-ones as potent non-nucleoside reverse transcriptase inhibitors.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 17, Issue:7, 2007
Development of a new methodology for screening of human immunodeficiency virus type 1 microbicides based on real-time PCR quantification.Antimicrobial agents and chemotherapy, , Volume: 51, Issue:2, 2007
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.The Journal of biological chemistry, , Mar-16, Volume: 282, Issue:11, 2007
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.Journal of medicinal chemistry, , Nov-01, Volume: 50, Issue:22, 2007
Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity.Journal of medicinal chemistry, , Oct-04, Volume: 50, Issue:20, 2007
Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 16, Issue:13, 2006
Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 16, Issue:13, 2006
New HIV-1 reverse transcriptase inhibitors based on a tricyclic benzothiophene scaffold: synthesis, resolution, and inhibitory activity.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 16, Issue:11, 2006
Structure-based design, parallel synthesis, structure-activity relationship, and molecular modeling studies of thiocarbamates, new potent non-nucleoside HIV-1 reverse transcriptase inhibitor isosteres of phenethylthiazolylthiourea derivatives.Journal of medicinal chemistry, , Jun-02, Volume: 48, Issue:11, 2005
Specific targeting highly conserved residues in the HIV-1 reverse transcriptase primer grip region. Design, synthesis, and biological evaluation of novel, potent, and broad spectrum NNRTIs with antiviral activity.Journal of medicinal chemistry, , Nov-17, Volume: 48, Issue:23, 2005
Parallel solution-phase and microwave-assisted synthesis of new S-DABO derivatives endowed with subnanomolar anti-HIV-1 activity.Journal of medicinal chemistry, , Dec-15, Volume: 48, Issue:25, 2005
Novel 1-[2-(diarylmethoxy)ethyl]-2-methyl-5-nitroimidazoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. A structure-activity relationship investigation.Journal of medicinal chemistry, , Jun-30, Volume: 48, Issue:13, 2005
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.Journal of medicinal chemistry, , Feb-26, Volume: 47, Issue:5, 2004
5-Alkyl-2-[(aryl and alkyloxylcarbonylmethyl)thio]-6-(1-naphthylmethyl) pyrimidin-4(3H)-ones as an unique HIV reverse transcriptase inhibitors of S-DABO series.Bioorganic & medicinal chemistry letters, , Jun-21, Volume: 14, Issue:12, 2004
Prediction of activity for nonnucleoside inhibitors with HIV-1 reverse transcriptase based on Monte Carlo simulations.Journal of medicinal chemistry, , Jul-04, Volume: 45, Issue:14, 2002
4,1-Benzoxazepinone analogues of efavirenz (Sustiva) as HIV-1 reverse transcriptase inhibitors.Bioorganic & medicinal chemistry letters, , Jun-04, Volume: 11, Issue:11, 2001
Antiviral drug design: computational analyses of the effects of the L100I mutation for HIV-RT on the binding of NNRTIs.Bioorganic & medicinal chemistry letters, , Nov-05, Volume: 11, Issue:21, 2001
Synthesis and evaluation of efavirenz (Sustiva) analogues as HIV-1 reverse transcriptase inhibitors: replacement of the cyclopropylacetylene side chain.Bioorganic & medicinal chemistry letters, , May-07, Volume: 11, Issue:9, 2001
Synthesis and biological activities of potential metabolites of the non-nucleoside reverse transcriptase inhibitor efavirenz.Bioorganic & medicinal chemistry letters, , Mar-12, Volume: 11, Issue:5, 2001
Trifluoromethyl-containing 3-alkoxymethyl- and 3-aryloxymethyl-2-pyridinones are potent inhibitors of HIV-1 non-nucleoside reverse transcriptase.Bioorganic & medicinal chemistry letters, , Feb-12, Volume: 11, Issue:3, 2001
3,3a-Dihydropyrano[4,3,2-de]quinazolin-2(1H)-ones are potent non-nucleoside reverse transcriptase inhibitors.Bioorganic & medicinal chemistry letters, , Jan-22, Volume: 11, Issue:2, 2001
Quinoxalinylethylpyridylthioureas (QXPTs) as potent non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors. Further SAR studies and identification of a novel orally bioavailable hydrazine-based antiviral agent.Journal of medicinal chemistry, , Feb-01, Volume: 44, Issue:3, 2001
Synthesis and evaluation of novel quinolinones as HIV-1 reverse transcriptase inhibitors.Bioorganic & medicinal chemistry letters, , Jul-23, Volume: 11, Issue:14, 2001
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.Journal of medicinal chemistry, , May-18, Volume: 43, Issue:10, 2000
Novel 2,2-dioxide-4,4-disubstituted-1,3-H-2,1,3-benzothiadiazines as non-nucleoside reverse transcriptase inhibitors.Bioorganic & medicinal chemistry letters, , Jan-17, Volume: 10, Issue:2, 2000
Synthesis and evaluation of quinoxalinones as HIV-1 reverse transcriptase inhibitors.Bioorganic & medicinal chemistry letters, , Aug-07, Volume: 10, Issue:15, 2000
Synthesis and evaluation of analogs of Efavirenz (SUSTIVA) as HIV-1 reverse transcriptase inhibitors.Bioorganic & medicinal chemistry letters, , Oct-04, Volume: 9, Issue:19, 1999
Synthesis and evaluation of benzoxazinones as HIV-1 reverse transcriptase inhibitors. Analogs of Efavirenz (SUSTIVA).Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 9, Issue:22, 1999
Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues.Journal of medicinal chemistry, , Oct-07, Volume: 42, Issue:20, 1999
Synopsis of some recent tactical application of bioisosteres in drug design.Journal of medicinal chemistry, , Apr-28, Volume: 54, Issue:8, 2011
Anti-human immunodeficiency virus activity, cross-resistance, cytotoxicity, and intracellular pharmacology of the 3'-azido-2',3'-dideoxypurine nucleosides.Antimicrobial agents and chemotherapy, , Volume: 53, Issue:9, 2009
Impact of novel human immunodeficiency virus type 1 reverse transcriptase mutations P119S and T165A on 4'-ethynylthymidine analog resistance profile.Antimicrobial agents and chemotherapy, , Volume: 53, Issue:11, 2009
Mechanisms by which the G333D mutation in human immunodeficiency virus type 1 Reverse transcriptase facilitates dual resistance to zidovudine and lamivudine.Antimicrobial agents and chemotherapy, , Volume: 52, Issue:1, 2008
Mechanism of inhibition of human immunodeficiency virus type 1 reverse transcriptase by a stavudine analogue, 4'-ethynyl stavudine triphosphate.Antimicrobial agents and chemotherapy, , Volume: 52, Issue:6, 2008
Anti-HIV activity of (-)-(2R,4R)-1- (2-hydroxymethyl-1,3-dioxolan-4-yl)-thymine against drug-resistant HIV-1 mutants and studies of its molecular mechanism.Journal of medicinal chemistry, , Jun-16, Volume: 48, Issue:12, 2005
Synthesis of 2',3'-dideoxynucleoside 5'-alpha-P-borano-beta,gamma-(difluoromethylene)triphosphates and their inhibition of HIV-1 reverse transcriptase.Journal of medicinal chemistry, , Apr-07, Volume: 48, Issue:7, 2005
Structural analogues of the calanolide anti-HIV agents. Modification of the trans-10,11-dimethyldihydropyran-12-ol ring (ring C).Journal of medicinal chemistry, , Mar-14, Volume: 40, Issue:6, 1997
Specific inhibition of human immunodeficiency virus type 1 reverse transcriptase mediated by soulattrolide, a coumarin isolated from the latex of calophyllum teysmannii.Journal of natural products, , Volume: 59, Issue:9, 1996
Mechanistic evaluation of new plant-derived compounds that inhibit HIV-1 reverse transcriptase.Journal of natural products, , Volume: 58, Issue:7, 1995
Comparison of ligand-based and structure-based 3D-QSAR approaches: a case study on (aryl-)bridged 2-aminobenzonitriles inhibiting HIV-1 reverse transcriptase.Journal of medicinal chemistry, , Jun-02, Volume: 48, Issue:11, 2005
2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1.Journal of medicinal chemistry, , Jun-07, Volume: 44, Issue:12, 2001
Computer-aided design, synthesis, and anti-HIV-1 activity in vitro of 2-alkylamino-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as novel potent non-nucleoside reverse transcriptase inhibitors, also active against the Y181C variaJournal of medicinal chemistry, , Feb-12, Volume: 47, Issue:4, 2004
5-Alkyl-2-[(aryl and alkyloxylcarbonylmethyl)thio]-6-(1-naphthylmethyl) pyrimidin-4(3H)-ones as an unique HIV reverse transcriptase inhibitors of S-DABO series.Bioorganic & medicinal chemistry letters, , Jun-21, Volume: 14, Issue:12, 2004
Prediction of activity for nonnucleoside inhibitors with HIV-1 reverse transcriptase based on Monte Carlo simulations.Journal of medicinal chemistry, , Jul-04, Volume: 45, Issue:14, 2002
Estimation of binding affinities for HEPT and nevirapine analogues with HIV-1 reverse transcriptase via Monte Carlo simulations.Journal of medicinal chemistry, , Jan-18, Volume: 44, Issue:2, 2001
Complexes of HIV-1 reverse transcriptase with inhibitors of the HEPT series reveal conformational changes relevant to the design of potent non-nucleoside inhibitors.Journal of medicinal chemistry, , Apr-12, Volume: 39, Issue:8, 1996
A new series of pyridinone derivatives as potent non-nucleoside human immunodeficiency virus type 1 specific reverse transcriptase inhibitors.Journal of medicinal chemistry, , Nov-10, Volume: 38, Issue:23, 1995
Activity of acyclic 6-(phenylselenenyl)pyrimidine nucleosides against human immunodeficiency viruses in primary lymphocytes.Journal of medicinal chemistry, , Volume: 34, Issue:11, 1991
A novel lead for specific anti-HIV-1 agents: 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine.Journal of medicinal chemistry, , Volume: 32, Issue:12, 1989
Prediction of activity for nonnucleoside inhibitors with HIV-1 reverse transcriptase based on Monte Carlo simulations.Journal of medicinal chemistry, , Jul-04, Volume: 45, Issue:14, 2002
Estimation of binding affinities for HEPT and nevirapine analogues with HIV-1 reverse transcriptase via Monte Carlo simulations.Journal of medicinal chemistry, , Jan-18, Volume: 44, Issue:2, 2001
A 3D QSAR study of a series of HEPT analogues: the influence of conformational mobility on HIV-1 reverse transcriptase inhibition.Journal of medicinal chemistry, , Dec-19, Volume: 40, Issue:26, 1997
Synthesis and evaluation of 2-pyridinone derivatives as specific HIV-1 reverse transcriptase inhibitors. 3. Pyridyl and phenyl analogs of 3-aminopyridin-2(1H)-one.Journal of medicinal chemistry, , Jan-22, Volume: 36, Issue:2, 1993
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Synthesis and evaluation of 2-pyridinone derivatives as HIV-1 specific reverse transcriptase inhibitors. 1. Phthalimidoalkyl and -alkylamino analogues.Journal of medicinal chemistry, , Oct-16, Volume: 35, Issue:21, 1992
2-Pyridinone derivatives: a new class of nonnucleoside, HIV-1-specific reverse transcriptase inhibitors.Journal of medicinal chemistry, , Volume: 34, Issue:9, 1991
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.The Journal of biological chemistry, , Mar-16, Volume: 282, Issue:11, 2007
Trifluoromethyl-containing 3-alkoxymethyl- and 3-aryloxymethyl-2-pyridinones are potent inhibitors of HIV-1 non-nucleoside reverse transcriptase.Bioorganic & medicinal chemistry letters, , Feb-12, Volume: 11, Issue:3, 2001
Novel 1,5-diphenylpyrazole nonnucleoside HIV-1 reverse transcriptase inhibitors with enhanced activity versus the delavirdine-resistant P236L mutant: lead identification and SAR of 3- and 4-substituted derivatives.Journal of medicinal chemistry, , Mar-09, Volume: 43, Issue:5, 2000
Synthesis and anti-HIV activities of urea-PETT analogs belonging to a new class of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.Bioorganic & medicinal chemistry letters, , Jun-16, Volume: 8, Issue:12, 1998
Pyrrolobenzothiazepinones and pyrrolobenzoxazepinones: novel and specific non-nucleoside HIV-1 reverse transcriptase inhibitors with antiviral activity.Journal of medicinal chemistry, , Jul-05, Volume: 39, Issue:14, 1996
Phenethylthiazolylthiourea (PETT) compounds as a new class of HIV-1 reverse transcriptase inhibitors. 2. Synthesis and further structure-activity relationship studies of PETT analogs.Journal of medicinal chemistry, , Oct-11, Volume: 39, Issue:21, 1996
Targeting delavirdine/atevirdine resistant HIV-1: identification of (alkylamino)piperidine-containing bis(heteroaryl)piperazines as broad spectrum HIV-1 reverse transcriptase inhibitors.Journal of medicinal chemistry, , Sep-13, Volume: 39, Issue:19, 1996
Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors. 1. Synthesis and basic structure-activity relationship studies of PETT analogs.Journal of medicinal chemistry, , Dec-08, Volume: 38, Issue:25, 1995
Synthesis of a series of 4-(arylethynyl)-6-chloro-4-cyclopropyl-3,4-dihydroquinazolin-2(1H)-ones as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.Journal of medicinal chemistry, , Jul-22, Volume: 37, Issue:15, 1994
Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-carbonyl]-4-[3- [(1-methylethyl)amino]-pyridinyl]piJournal of medicinal chemistry, , May-14, Volume: 36, Issue:10, 1993
Selective non-nucleoside HIV-1 reverse transcriptase inhibitors. New 2,3-dihydrothiazolo[2,3-a]isoindol-5(9bH)-ones and related compounds with anti-HIV-1 activity.Journal of medicinal chemistry, , Aug-20, Volume: 36, Issue:17, 1993
Synthesis and evaluation of 2-pyridinone derivatives as specific HIV-1 reverse transcriptase inhibitors. 3. Pyridyl and phenyl analogs of 3-aminopyridin-2(1H)-one.Journal of medicinal chemistry, , Jan-22, Volume: 36, Issue:2, 1993
Synthesis and evaluation of 2-pyridinone derivatives as HIV-1-specific reverse transcriptase inhibitors. 4. 3-[2-(Benzoxazol-2-yl)ethyl]-5-ethyl-6-methylpyridin-2(1H)-one and analogues.Journal of medicinal chemistry, , Apr-16, Volume: 36, Issue:8, 1993
Synthesis and anti-HIV-1 activity of a series of imidazo[1,5-b]pyridazines.Journal of medicinal chemistry, , Nov-26, Volume: 36, Issue:24, 1993
Synthesis and evaluation of 2-pyridinone derivatives as HIV-1-specific reverse transcriptase inhibitors. 2. Analogues of 3-aminopyridin-2(1H)-one.Journal of medicinal chemistry, , Oct-16, Volume: 35, Issue:21, 1992
2-Pyridinone derivatives: a new class of nonnucleoside, HIV-1-specific reverse transcriptase inhibitors.Journal of medicinal chemistry, , Volume: 34, Issue:9, 1991
Crystal structure of tert-butyldimethylsilyl-spiroaminooxathioledioxide-thymine (TSAO-T) in complex with HIV-1 reverse transcriptase (RT) redefines the elastic limits of the non-nucleoside inhibitor-binding pocket.Journal of medicinal chemistry, , Apr-28, Volume: 54, Issue:8, 2011
Structure-activity relationships of [2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]- 3'-spiro-5' '-(4' '-amino-1' ',2' '-oxathiole-2' ',2' '-dioxide)thymine derivatives as inhibitors of HIV-1 reverse transcriptase dimerization.Journal of medicinal chemistry, , Aug-10, Volume: 49, Issue:16, 2006
Crystal structure of tert-butyldimethylsilyl-spiroaminooxathioledioxide-thymine (TSAO-T) in complex with HIV-1 reverse transcriptase (RT) redefines the elastic limits of the non-nucleoside inhibitor-binding pocket.Journal of medicinal chemistry, , Apr-28, Volume: 54, Issue:8, 2011
Structure-activity relationships of [2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]- 3'-spiro-5' '-(4' '-amino-1' ',2' '-oxathiole-2' ',2' '-dioxide)thymine derivatives as inhibitors of HIV-1 reverse transcriptase dimerization.Journal of medicinal chemistry, , Aug-10, Volume: 49, Issue:16, 2006
Hybrids of [TSAO-T]-[foscarnet]: The first conjugate of foscarnet with a non-nucleoside reverse transcriptase inhibitor through a labile covalent ester bond.Journal of medicinal chemistry, , Jun-17, Volume: 47, Issue:13, 2004
Synthesis of 3' '-substituted TSAO derivatives with anti-HIV-1 and anti-HIV-2 activity through an efficient palladium-catalyzed cross-coupling approach.Journal of medicinal chemistry, , Aug-29, Volume: 45, Issue:18, 2002
Design, synthesis, and biological evaluation of 1-[(2-benzyloxyl/alkoxyl)methyl]-5-halo-6-aryluracils as potent HIV-1 non-nucleoside reverse transcriptase inhibitors with an improved drug resistance profile.Journal of medicinal chemistry, , Mar-08, Volume: 55, Issue:5, 2012
Synthesis and biological evaluation of novel C5 halogen-functionalized S-DABO as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.Bioorganic & medicinal chemistry, , May-01, Volume: 18, Issue:9, 2010
Computer-aided design, synthesis, and anti-HIV-1 activity in vitro of 2-alkylamino-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as novel potent non-nucleoside reverse transcriptase inhibitors, also active against the Y181C variaJournal of medicinal chemistry, , Feb-12, Volume: 47, Issue:4, 2004
Prediction of activity for nonnucleoside inhibitors with HIV-1 reverse transcriptase based on Monte Carlo simulations.Journal of medicinal chemistry, , Jul-04, Volume: 45, Issue:14, 2002
Structure-based design, synthesis, and biological evaluation of conformationally restricted novel 2-alkylthio-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.Journal of medicinal chemistry, , Aug-02, Volume: 44, Issue:16, 2001
Estimation of binding affinities for HEPT and nevirapine analogues with HIV-1 reverse transcriptase via Monte Carlo simulations.Journal of medicinal chemistry, , Jan-18, Volume: 44, Issue:2, 2001
Antiviral drug design: computational analyses of the effects of the L100I mutation for HIV-RT on the binding of NNRTIs.Bioorganic & medicinal chemistry letters, , Nov-05, Volume: 11, Issue:21, 2001
N-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea and N'-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-chloropyridyl)]-thiourea as potent inhibitors of multidrug-resistant human immunodeficiency virus-1.Bioorganic & medicinal chemistry letters, , Sep-20, Volume: 9, Issue:18, 1999
N'-[2-(2-thiophene)ethyl]-N'-[2-(5-bromopyridyl)] thiourea as a potent inhibitor of NNI-resistant and multidrug-resistant human immunodeficiency virus-1.Bioorganic & medicinal chemistry letters, , Dec-20, Volume: 9, Issue:24, 1999
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Rational design of N-[2-(2,5-dimethoxyphenylethyl)]-N'-[2-(5-bromopyridyl)]-thiourea (HI-236) as a potent non-nucleoside inhibitor of drug-resistant human immunodeficiency virus.Bioorganic & medicinal chemistry letters, , Jun-07, Volume: 9, Issue:11, 1999
A 3D QSAR study of a series of HEPT analogues: the influence of conformational mobility on HIV-1 reverse transcriptase inhibition.Journal of medicinal chemistry, , Dec-19, Volume: 40, Issue:26, 1997
Complexes of HIV-1 reverse transcriptase with inhibitors of the HEPT series reveal conformational changes relevant to the design of potent non-nucleoside inhibitors.Journal of medicinal chemistry, , Apr-12, Volume: 39, Issue:8, 1996
Synopsis of some recent tactical application of bioisosteres in drug design.Journal of medicinal chemistry, , Apr-28, Volume: 54, Issue:8, 2011
Anti-human immunodeficiency virus activity, cross-resistance, cytotoxicity, and intracellular pharmacology of the 3'-azido-2',3'-dideoxypurine nucleosides.Antimicrobial agents and chemotherapy, , Volume: 53, Issue:9, 2009
Mechanisms by which the G333D mutation in human immunodeficiency virus type 1 Reverse transcriptase facilitates dual resistance to zidovudine and lamivudine.Antimicrobial agents and chemotherapy, , Volume: 52, Issue:1, 2008
Synthesis, anti-HIV activity, and resistance profile of thymidine phosphonomethoxy nucleosides and their bis-isopropyloxymethylcarbonyl (bisPOC) prodrugs.Bioorganic & medicinal chemistry, , Aug-15, Volume: 15, Issue:16, 2007
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Effects of the translocation status of human immunodeficiency virus type 1 reverse transcriptase on the efficiency of excision of tenofovir.Antimicrobial agents and chemotherapy, , Volume: 51, Issue:8, 2007
Synthesis of 2',3'-dideoxynucleoside 5'-alpha-P-borano-beta,gamma-(difluoromethylene)triphosphates and their inhibition of HIV-1 reverse transcriptase.Journal of medicinal chemistry, , Apr-07, Volume: 48, Issue:7, 2005
Inhibition of human immunodeficiency virus reverse transcriptase by synadenol triphosphate and its E-isomer.Journal of medicinal chemistry, , Oct-23, Volume: 46, Issue:22, 2003
Bifunctional inhibition of human immunodeficiency virus type 1 reverse transcriptase: mechanism and proof-of-concept as a novel therapeutic design strategy.Journal of medicinal chemistry, , May-23, Volume: 56, Issue:10, 2013
Impact of novel human immunodeficiency virus type 1 reverse transcriptase mutations P119S and T165A on 4'-ethynylthymidine analog resistance profile.Antimicrobial agents and chemotherapy, , Volume: 53, Issue:11, 2009
Anti-human immunodeficiency virus activity, cross-resistance, cytotoxicity, and intracellular pharmacology of the 3'-azido-2',3'-dideoxypurine nucleosides.Antimicrobial agents and chemotherapy, , Volume: 53, Issue:9, 2009
Mechanism of inhibition of human immunodeficiency virus type 1 reverse transcriptase by a stavudine analogue, 4'-ethynyl stavudine triphosphate.Antimicrobial agents and chemotherapy, , Volume: 52, Issue:6, 2008
Selective inhibition of porcine endogenous retrovirus replication in human cells by acyclic nucleoside phosphonates.Antimicrobial agents and chemotherapy, , Volume: 51, Issue:7, 2007
Synthesis, anti-HIV activity, and resistance profile of thymidine phosphonomethoxy nucleosides and their bis-isopropyloxymethylcarbonyl (bisPOC) prodrugs.Bioorganic & medicinal chemistry, , Aug-15, Volume: 15, Issue:16, 2007
Synthesis of 2',3'-dideoxynucleoside 5'-alpha-P-borano-beta,gamma-(difluoromethylene)triphosphates and their inhibition of HIV-1 reverse transcriptase.Journal of medicinal chemistry, , Apr-07, Volume: 48, Issue:7, 2005
Design, synthesis and antiviral activity of novel 4,5-disubstituted 7-(beta-D-ribofuranosyl)pyrrolo[2,3-d][1,2,3]triazines and the novel 3-amino-5-methyl-1-(beta-D-ribofuranosyl)- and 3-amino-5-methyl-1-(2-deoxy-beta-D-ribofuranosyl)-1,5-dihydro-1,4,5,6,7Journal of medicinal chemistry, , Jun-02, Volume: 48, Issue:11, 2005
6-N-Acyltriciribine analogues: structure-activity relationship between acyl carbon chain length and activity against HIV-1.Journal of medicinal chemistry, , Jun-15, Volume: 43, Issue:12, 2000
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Discovery and Structure-Based Optimization of 2-Ureidothiophene-3-carboxylic Acids as Dual Bacterial RNA Polymerase and Viral Reverse Transcriptase Inhibitors.Journal of medicinal chemistry, , Aug-11, Volume: 59, Issue:15, 2016
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Anti-human immunodeficiency virus activity, cross-resistance, cytotoxicity, and intracellular pharmacology of the 3'-azido-2',3'-dideoxypurine nucleosides.Antimicrobial agents and chemotherapy, , Volume: 53, Issue:9, 2009
Mechanisms by which the G333D mutation in human immunodeficiency virus type 1 Reverse transcriptase facilitates dual resistance to zidovudine and lamivudine.Antimicrobial agents and chemotherapy, , Volume: 52, Issue:1, 2008
Effects of the translocation status of human immunodeficiency virus type 1 reverse transcriptase on the efficiency of excision of tenofovir.Antimicrobial agents and chemotherapy, , Volume: 51, Issue:8, 2007
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.The Journal of biological chemistry, , Mar-16, Volume: 282, Issue:11, 2007
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.Antimicrobial agents and chemotherapy, , Volume: 51, Issue:6, 2007
Selective inhibition of porcine endogenous retrovirus replication in human cells by acyclic nucleoside phosphonates.Antimicrobial agents and chemotherapy, , Volume: 51, Issue:7, 2007
4'C-ethynyl-thymidine acts as a chain terminator during DNA-synthesis catalyzed by HIV-1 reverse transcriptase.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 15, Issue:4, 2005
Synthesis of 2',3'-dideoxynucleoside 5'-alpha-P-borano-beta,gamma-(difluoromethylene)triphosphates and their inhibition of HIV-1 reverse transcriptase.Journal of medicinal chemistry, , Apr-07, Volume: 48, Issue:7, 2005
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A 3D QSAR study of a series of HEPT analogues: the influence of conformational mobility on HIV-1 reverse transcriptase inhibition.Journal of medicinal chemistry, , Dec-19, Volume: 40, Issue:26, 1997
The Journey of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) from Lab to Clinic.Journal of medicinal chemistry, , 05-23, Volume: 62, Issue:10, 2019
Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-carbonyl]-4-[3- [(1-methylethyl)amino]-pyridinyl]piJournal of medicinal chemistry, , May-14, Volume: 36, Issue:10, 1993
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The inophyllums, novel inhibitors of HIV-1 reverse transcriptase isolated from the Malaysian tree, Calophyllum inophyllum Linn.Journal of medicinal chemistry, , Dec-24, Volume: 36, Issue:26, 1993
Design, synthesis, and biological evaluation of novel double-winged galloyl derivatives as HIV-1 RNase H inhibitors.European journal of medicinal chemistry, , Oct-05, Volume: 240, 2022
Quinolinonyl Non-Diketo Acid Derivatives as Inhibitors of HIV-1 Ribonuclease H and Polymerase Functions of Reverse Transcriptase.Journal of medicinal chemistry, , 06-24, Volume: 64, Issue:12, 2021
Design, synthesis and biological evaluation of 3-hydroxyquinazoline-2,4(1H,3H)-diones as dual inhibitors of HIV-1 reverse transcriptase-associated RNase H and integrase.Bioorganic & medicinal chemistry, , 09-01, Volume: 27, Issue:17, 2019
5-Hydroxypyrido[2,3-b]pyrazin-6(5H)-one derivatives as novel dual inhibitors of HIV-1 reverse transcriptase-associated ribonuclease H and integrase.European journal of medicinal chemistry, , Jul-15, Volume: 155, 2018
Structure-guided approach identifies a novel class of HIV-1 ribonuclease H inhibitors: binding mode insights through magnesium complexation and site-directed mutagenesis studies.MedChemComm, , Mar-01, Volume: 9, Issue:3, 2018
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A score years' update in the synthesis and biological evaluation of medicinally important 2-pyridones.European journal of medicinal chemistry, , Mar-15, Volume: 232, 2022
Principal components describing biological activities and molecular diversity of heterocyclic aromatic ring fragments.Journal of medicinal chemistry, , Sep-27, Volume: 39, Issue:20, 1996
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Prediction of activity for nonnucleoside inhibitors with HIV-1 reverse transcriptase based on Monte Carlo simulations.Journal of medicinal chemistry, , Jul-04, Volume: 45, Issue:14, 2002
Synthesis and evaluation of quinoxalinones as HIV-1 reverse transcriptase inhibitors.Bioorganic & medicinal chemistry letters, , Aug-07, Volume: 10, Issue:15, 2000
Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK.Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
Structure-Based Discovery of Novel NHJournal of medicinal chemistry, , 06-23, Volume: 65, Issue:12, 2022
[no title available]Bioorganic & medicinal chemistry, , 01-01, Volume: 53, 2022
Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.Journal of medicinal chemistry, , 07-22, Volume: 64, Issue:14, 2021
Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies.Journal of medicinal chemistry, , 09-23, Volume: 64, Issue:18, 2021
2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 NNRTIs: Rational Design, Synthesis, Activity Evaluation, and Crystallographic Studies.Journal of medicinal chemistry, , 04-08, Volume: 64, Issue:7, 2021
Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs.Bioorganic & medicinal chemistry, , 06-15, Volume: 40, 2021
[no title available]Journal of medicinal chemistry, , 09-23, Volume: 64, Issue:18, 2021
Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.Bioorganic & medicinal chemistry, , 07-15, Volume: 42, 2021
Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.European journal of medicinal chemistry, , Feb-05, Volume: 211, 2021
Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high FspEuropean journal of medicinal chemistry, , Mar-05, Volume: 213, 2021
Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from Journal of medicinal chemistry, , 04-22, Volume: 64, Issue:8, 2021
Fragment hopping-based discovery of novel sulfinylacetamide-diarylpyrimidines (DAPYs) as HIV-1 nonnucleoside reverse transcriptase inhibitors.European journal of medicinal chemistry, , Jan-01, Volume: 185, 2020
New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.European journal of medicinal chemistry, , Dec-15, Volume: 208, 2020
[no title available]Journal of medicinal chemistry, , 05-14, Volume: 63, Issue:9, 2020
Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles.Journal of medicinal chemistry, , 12-26, Volume: 62, Issue:24, 2019
Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.Journal of medicinal chemistry, , 01-24, Volume: 62, Issue:2, 2019
Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.Journal of medicinal chemistry, , 02-14, Volume: 62, Issue:3, 2019
Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors.European journal of medicinal chemistry, , Nov-15, Volume: 182, 2019
[no title available]Journal of medicinal chemistry, , 02-28, Volume: 62, Issue:4, 2019
Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.European journal of medicinal chemistry, , May-10, Volume: 151, 2018
Design and synthesis of a novel series of non-nucleoside HIV-1 inhibitors bearing pyrimidine and N-substituted aromatic piperazine.Bioorganic & medicinal chemistry letters, , 12-01, Volume: 28, Issue:22, 2018
The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery.ACS medicinal chemistry letters, , Apr-12, Volume: 9, Issue:4, 2018
Discovery of Novel Diarylpyrimidine Derivatives as Potent HIV-1 NNRTIs Targeting the "NNRTI Adjacent" Binding Site.ACS medicinal chemistry letters, , Apr-12, Volume: 9, Issue:4, 2018
Advances in diarylpyrimidines and related analogues as HIV-1 nonnucleoside reverse transcriptase inhibitors.European journal of medicinal chemistry, , Oct-05, Volume: 158, 2018
Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR.Bioorganic & medicinal chemistry, , 04-15, Volume: 25, Issue:8, 2017
Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives as potent HIV-1 NNRTIs.European journal of medicinal chemistry, , Nov-10, Volume: 140, 2017
Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.Journal of medicinal chemistry, , 05-25, Volume: 60, Issue:10, 2017
Discovery of Thiophene[3,2-ACS medicinal chemistry letters, , Nov-09, Volume: 8, Issue:11, 2017
Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.Journal of medicinal chemistry, , 08-10, Volume: 60, Issue:15, 2017
Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach.Bioorganic & medicinal chemistry, , 09-15, Volume: 24, Issue:18, 2016
Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket.European journal of medicinal chemistry, , Jun-10, Volume: 115, 2016
Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.Journal of medicinal chemistry, , 09-08, Volume: 59, Issue:17, 2016
Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket.European journal of medicinal chemistry, , Feb-15, Volume: 109, 2016
Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket.European journal of medicinal chemistry, , Oct-04, Volume: 121, 2016
Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy.Bioorganic & medicinal chemistry, , 07-01, Volume: 24, Issue:13, 2016
1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus.Bioorganic & medicinal chemistry, , 06-01, Volume: 24, Issue:11, 2016
Novel (2,6-difluorophenyl)(2-(phenylamino)pyrimidin-4-yl)methanones with restricted conformation as potent non-nucleoside reverse transcriptase inhibitors against HIV-1.European journal of medicinal chemistry, , Oct-21, Volume: 122, 2016
Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 4: design, synthesis and biological evaluation of novel imidazo[1,2-a]pyrazines.European journal of medicinal chemistry, , Mar-26, Volume: 93, 2015
Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches.European journal of medicinal chemistry, , Mar-06, Volume: 92, 2015
Anti-HIV diarylpyrimidine-quinolone hybrids and their mode of action.Bioorganic & medicinal chemistry, , Jul-01, Volume: 23, Issue:13, 2015
A novel family of diarylpyrimidines (DAPYs) featuring a diatomic linker: Design, synthesis and anti-HIV activities.Bioorganic & medicinal chemistry, , Oct-15, Volume: 23, Issue:20, 2015
Fused heterocyclic compounds bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 1: design, synthesis and biological evaluation of novel 5,7-disubstituted pyrazolo[1,5-a]pyrimidine derivatives.Bioorganic & medicinal chemistry, , Apr-01, Volume: 22, Issue:7, 2014
Discovery of nitropyridine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors via a structure-based core refining approach.European journal of medicinal chemistry, , Apr-09, Volume: 76, 2014
Discovery of 2-pyridone derivatives as potent HIV-1 NNRTIs using molecular hybridization based on crystallographic overlays.Bioorganic & medicinal chemistry, , Mar-15, Volume: 22, Issue:6, 2014
Design, synthesis and preliminary SAR studies of novel N-arylmethyl substituted piperidine-linked aniline derivatives as potent HIV-1 NNRTIs.Bioorganic & medicinal chemistry, , Jan-01, Volume: 22, Issue:1, 2014
Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.Journal of medicinal chemistry, , Dec-11, Volume: 57, Issue:23, 2014
Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors.Bioorganic & medicinal chemistry, , Apr-15, Volume: 22, Issue:8, 2014
New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.European journal of medicinal chemistry, , Jun-10, Volume: 80, 2014
Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors.European journal of medicinal chemistry, , Volume: 65, 2013
Towards new C6-rigid S-DABO HIV-1 reverse transcriptase inhibitors: synthesis, biological investigation and molecular modeling studies.Bioorganic & medicinal chemistry, , Nov-01, Volume: 21, Issue:21, 2013
Synthesis and biological evaluation of pyridazine derivatives as novel HIV-1 NNRTIs.Bioorganic & medicinal chemistry, , Apr-01, Volume: 21, Issue:7, 2013
Chiral resolution, absolute configuration assignment and biological activity of racemic diarylpyrimidine CH(OH)-DAPY as potent nonnucleoside HIV-1 reverse transcriptase inhibitors.European journal of medicinal chemistry, , Volume: 53, 2012
New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors.Journal of medicinal chemistry, , Jul-26, Volume: 55, Issue:14, 2012
Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors.European journal of medicinal chemistry, , Volume: 51, 2012
Exploration of piperidine-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Phenyl derivatives with broad potency against resistant mutant viruses.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 20, Issue:20, 2010
The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity.Antimicrobial agents and chemotherapy, , Volume: 54, Issue:6, 2010
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.Antimicrobial agents and chemotherapy, , Volume: 53, Issue:6, 2009
Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.Antimicrobial agents and chemotherapy, , Volume: 53, Issue:11, 2009
Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.Journal of medicinal chemistry, , 01-24, Volume: 62, Issue:2, 2019
Advances in diarylpyrimidines and related analogues as HIV-1 nonnucleoside reverse transcriptase inhibitors.European journal of medicinal chemistry, , Oct-05, Volume: 158, 2018
2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.Journal of medicinal chemistry, , Apr-12, Volume: 55, Issue:7, 2012
Novel diarylpyridinones, diarylpyridazinones and diarylphthalazinones as potential HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs).Bioorganic & medicinal chemistry, , Oct-15, Volume: 19, Issue:20, 2011
Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.Journal of medicinal chemistry, , Apr-28, Volume: 54, Issue:8, 2011
The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity.Antimicrobial agents and chemotherapy, , Volume: 54, Issue:6, 2010
Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.Antimicrobial agents and chemotherapy, , Volume: 53, Issue:11, 2009
Inhibition of tubulin polymerization by select alkenyldiarylmethanes.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 18, Issue:2, 2008
Synthesis and biological evaluation of alkenyldiarylmethane HIV-1 non-nucleoside reverse transcriptase inhibitors that possess increased hydrolytic stability.Journal of medicinal chemistry, , Oct-04, Volume: 50, Issue:20, 2007
The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors.Journal of medicinal chemistry, , Nov-22, Volume: 44, Issue:24, 2001
Novel modifications in the alkenyldiarylmethane (ADAM) series of non-nucleoside reverse transcriptase inhibitors.Journal of medicinal chemistry, , Nov-18, Volume: 42, Issue:23, 1999
New alkenyldiarylmethanes with enhanced potencies as anti-HIV agents which act as non-nucleoside reverse transcriptase inhibitors.Journal of medicinal chemistry, , Jun-04, Volume: 41, Issue:12, 1998
Synthesis of a non-nucleoside reverse transcriptase inhibitor in the alkenyldiarylmethane (ADAM) series with optimized potency and therapeutic index.Bioorganic & medicinal chemistry letters, , Jan-20, Volume: 8, Issue:2, 1998
Design, synthesis, and anti-HIV activity of 4'-modified carbocyclic nucleoside phosphonate reverse transcriptase inhibitors.Bioorganic & medicinal chemistry, , Feb-15, Volume: 17, Issue:4, 2009
The role of 2',3'-unsaturation on the antiviral activity of anti-HIV nucleosides against 3TC-resistant mutant (M184V).Bioorganic & medicinal chemistry letters, , Jun-16, Volume: 13, Issue:12, 2003
Anti-HIV activity of aromatic and heterocyclic thiazolyl thiourea compounds.Bioorganic & medicinal chemistry letters, , Feb-26, Volume: 11, Issue:4, 2001
Novel 2,2-dioxide-4,4-disubstituted-1,3-H-2,1,3-benzothiadiazines as non-nucleoside reverse transcriptase inhibitors.Bioorganic & medicinal chemistry letters, , Jan-17, Volume: 10, Issue:2, 2000
Novel 1,5-diphenylpyrazole nonnucleoside HIV-1 reverse transcriptase inhibitors with enhanced activity versus the delavirdine-resistant P236L mutant: lead identification and SAR of 3- and 4-substituted derivatives.Journal of medicinal chemistry, , Mar-09, Volume: 43, Issue:5, 2000
Targeting delavirdine/atevirdine resistant HIV-1: identification of (alkylamino)piperidine-containing bis(heteroaryl)piperazines as broad spectrum HIV-1 reverse transcriptase inhibitors.Journal of medicinal chemistry, , Sep-13, Volume: 39, Issue:19, 1996
Novel pyridinone derivatives as non-nucleoside reverse transcriptase inhibitors (NNRTIs) with high potency against NNRTI-resistant HIV-1 strains.Journal of medicinal chemistry, , May-09, Volume: 56, Issue:9, 2013
Design, synthesis, and biological evaluation of 1-[(2-benzyloxyl/alkoxyl)methyl]-5-halo-6-aryluracils as potent HIV-1 non-nucleoside reverse transcriptase inhibitors with an improved drug resistance profile.Journal of medicinal chemistry, , Mar-08, Volume: 55, Issue:5, 2012
N-3 Hydroxylation of Pyrimidine-2,4-diones Yields Dual Inhibitors of HIV Reverse Transcriptase and Integrase.ACS medicinal chemistry letters, , Volume: 2, Issue:1, 2011
Rationally designed dual inhibitors of HIV reverse transcriptase and integrase.Journal of medicinal chemistry, , Jul-26, Volume: 50, Issue:15, 2007
Complexes of HIV-1 reverse transcriptase with inhibitors of the HEPT series reveal conformational changes relevant to the design of potent non-nucleoside inhibitors.Journal of medicinal chemistry, , Apr-12, Volume: 39, Issue:8, 1996
Synthesis, antiviral activity, cytotoxicity and cellular pharmacology of l-3'-azido-2',3'-dideoxypurine nucleosides.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
Newly synthesized L-enantiomers of 3'-fluoro-modified beta-2'-deoxyribonucleoside 5'-triphosphates inhibit hepatitis B DNA polymerases but not the five cellular DNA polymerases alpha, beta, gamma, delta, and epsilon nor HIV-1 reverse transcriptase.Journal of medicinal chemistry, , Jun-04, Volume: 41, Issue:12, 1998
Prediction of activity for nonnucleoside inhibitors with HIV-1 reverse transcriptase based on Monte Carlo simulations.Journal of medicinal chemistry, , Jul-04, Volume: 45, Issue:14, 2002
Estimation of binding affinities for HEPT and nevirapine analogues with HIV-1 reverse transcriptase via Monte Carlo simulations.Journal of medicinal chemistry, , Jan-18, Volume: 44, Issue:2, 2001
Novel non-nucleoside inhibitors of human immunodeficiency virus type 1 reverse transcriptase. 5. 4-Substituted and 2,4-disubstituted analogs of nevirapine.Journal of medicinal chemistry, , Nov-24, Volume: 38, Issue:24, 1995
Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 1. Tricyclic pyridobenzo- and dipyridodiazepinones.Journal of medicinal chemistry, , Volume: 34, Issue:7, 1991
Synthesis and Antiviral Evaluation of Carbocyclic Nucleoside Analogs of Nucleoside Reverse Transcriptase Translocation Inhibitor MK-8591 (4'-Ethynyl-2-fluoro-2'-deoxyadenosine).Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
Synthesis, antiviral activity, cytotoxicity and cellular pharmacology of l-3'-azido-2',3'-dideoxypurine nucleosides.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
Anti-human immunodeficiency virus activity, cross-resistance, cytotoxicity, and intracellular pharmacology of the 3'-azido-2',3'-dideoxypurine nucleosides.Antimicrobial agents and chemotherapy, , Volume: 53, Issue:9, 2009
Mechanisms by which the G333D mutation in human immunodeficiency virus type 1 Reverse transcriptase facilitates dual resistance to zidovudine and lamivudine.Antimicrobial agents and chemotherapy, , Volume: 52, Issue:1, 2008
Synthesis and evaluation of 2'-substituted cyclobutyl nucleosides and nucleotides as potential anti-HIV agents.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 17, Issue:12, 2007
Synthesis of 2',3'-dideoxynucleoside 5'-alpha-P-borano-beta,gamma-(difluoromethylene)triphosphates and their inhibition of HIV-1 reverse transcriptase.Journal of medicinal chemistry, , Apr-07, Volume: 48, Issue:7, 2005
Effects of fluorine substitution of cytosine analogues on the binding affinity to HIV-1 reverse transcriptase.Bioorganic & medicinal chemistry letters, , Jan-19, Volume: 14, Issue:2, 2004
Novel indole-3-sulfonamides as potent HIV non-nucleoside reverse transcriptase inhibitors (NNRTIs).Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 18, Issue:2, 2008
Novel indolyl aryl sulfones active against HIV-1 carrying NNRTI resistance mutations: synthesis and SAR studies.Journal of medicinal chemistry, , Jun-05, Volume: 46, Issue:12, 2003
Design, synthesis, and anti-HIV activity of 4'-modified carbocyclic nucleoside phosphonate reverse transcriptase inhibitors.Bioorganic & medicinal chemistry, , Feb-15, Volume: 17, Issue:4, 2009
Synthesis and anti-HIV activity of GS-9148 (2'-Fd4AP), a novel nucleoside phosphonate HIV reverse transcriptase inhibitor.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 18, Issue:3, 2008
Effects of the translocation status of human immunodeficiency virus type 1 reverse transcriptase on the efficiency of excision of tenofovir.Antimicrobial agents and chemotherapy, , Volume: 51, Issue:8, 2007
Synthesis, anti-HIV activity, and resistance profile of thymidine phosphonomethoxy nucleosides and their bis-isopropyloxymethylcarbonyl (bisPOC) prodrugs.Bioorganic & medicinal chemistry, , Aug-15, Volume: 15, Issue:16, 2007
Efavirenz a nonnucleoside reverse transcriptase inhibitor of first-generation: Approaches based on its medicinal chemistry.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Trifluoromethyl-containing 3-alkoxymethyl- and 3-aryloxymethyl-2-pyridinones are potent inhibitors of HIV-1 non-nucleoside reverse transcriptase.Bioorganic & medicinal chemistry letters, , Feb-12, Volume: 11, Issue:3, 2001
4,1-Benzoxazepinone analogues of efavirenz (Sustiva) as HIV-1 reverse transcriptase inhibitors.Bioorganic & medicinal chemistry letters, , Jun-04, Volume: 11, Issue:11, 2001
3,3a-Dihydropyrano[4,3,2-de]quinazolin-2(1H)-ones are potent non-nucleoside reverse transcriptase inhibitors.Bioorganic & medicinal chemistry letters, , Jan-22, Volume: 11, Issue:2, 2001
Novel 2,2-dioxide-4,4-disubstituted-1,3-H-2,1,3-benzothiadiazines as non-nucleoside reverse transcriptase inhibitors.Bioorganic & medicinal chemistry letters, , Jan-17, Volume: 10, Issue:2, 2000
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.Journal of medicinal chemistry, , May-18, Volume: 43, Issue:10, 2000
Combining docking, molecular dynamics and the linear interaction energy method to predict binding modes and affinities for non-nucleoside inhibitors to HIV-1 reverse transcriptase.Journal of medicinal chemistry, , May-08, Volume: 51, Issue:9, 2008
Synthesis and antiviral activity of 4-benzyl pyridinone derivatives as potent and selective non-nucleoside human immunodeficiency virus type 1 reverse transcriptase inhibitors.Journal of medicinal chemistry, , Oct-19, Volume: 43, Issue:21, 2000
Synthesis, structure-activity relationships, and docking studies of N-phenylarylformamide derivatives (PAFAs) as non-nucleoside HIV reverse transcriptase inhibitors.European journal of medicinal chemistry, , Volume: 58, 2012
3D-QSAR models on clinically relevant K103N mutant HIV-1 reverse transcriptase obtained from two strategic considerations.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 18, Issue:3, 2008
The design and synthesis of diaryl ether second generation HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) with enhanced potency versus key clinical mutations.Bioorganic & medicinal chemistry letters, , May-01, Volume: 18, Issue:9, 2008
Design, synthesis, biochemical, and antiviral evaluations of C6 benzyl and C6 biarylmethyl substituted 2-hydroxylisoquinoline-1,3-diones: dual inhibition against HIV reverse transcriptase-associated RNase H and polymerase with antiviral activities.Journal of medicinal chemistry, , Jan-22, Volume: 58, Issue:2, 2015
Pyridopyrimidinone inhibitors of HIV-1 RNase H.European journal of medicinal chemistry, , Aug-18, Volume: 83, 2014
Potent and selective HIV-1 ribonuclease H inhibitors based on a 1-hydroxy-1,8-naphthyridin-2(1H)-one scaffold.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 20, Issue:22, 2010
Design, synthesis, and biological evaluation of a series of 2-hydroxyisoquinoline-1,3(2H,4H)-diones as dual inhibitors of human immunodeficiency virus type 1 integrase and the reverse transcriptase RNase H domain.Journal of medicinal chemistry, , Dec-25, Volume: 51, Issue:24, 2008
Molecular modeling calculations of HIV-1 reverse transcriptase nonnucleoside inhibitors: correlation of binding energy with biological activity for novel 2-aryl-substituted benzimidazole analogues.Journal of medicinal chemistry, , May-08, Volume: 46, Issue:10, 2003
Prediction of activity for nonnucleoside inhibitors with HIV-1 reverse transcriptase based on Monte Carlo simulations.Journal of medicinal chemistry, , Jul-04, Volume: 45, Issue:14, 2002
Prediction of the binding free energies of new TIBO-like HIV-1 reverse transcriptase inhibitors using a combination of PROFEC, PB/SA, CMC/MD, and free energy calculations.Journal of medicinal chemistry, , Mar-11, Volume: 42, Issue:5, 1999
Prediction of binding affinities for TIBO inhibitors of HIV-1 reverse transcriptase using Monte Carlo simulations in a linear response method.Journal of medicinal chemistry, , Dec-17, Volume: 41, Issue:26, 1998
Comparative molecular moment analysis (CoMMA): 3D-QSAR without molecular superposition.Journal of medicinal chemistry, , May-24, Volume: 39, Issue:11, 1996
Non-nucleoside inhibitors of HIV-1 reverse transcriptase: molecular modeling and X-ray structure investigations.Journal of medicinal chemistry, , Mar-19, Volume: 36, Issue:6, 1993
Selective non-nucleoside HIV-1 reverse transcriptase inhibitors. New 2,3-dihydrothiazolo[2,3-a]isoindol-5(9bH)-ones and related compounds with anti-HIV-1 activity.Journal of medicinal chemistry, , Aug-20, Volume: 36, Issue:17, 1993
Synthesis and evaluation of 2-pyridinone derivatives as specific HIV-1 reverse transcriptase inhibitors. 3. Pyridyl and phenyl analogs of 3-aminopyridin-2(1H)-one.Journal of medicinal chemistry, , Jan-22, Volume: 36, Issue:2, 1993
Molecular modeling calculations of HIV-1 reverse transcriptase nonnucleoside inhibitors: correlation of binding energy with biological activity for novel 2-aryl-substituted benzimidazole analogues.Journal of medicinal chemistry, , May-08, Volume: 46, Issue:10, 2003
Prediction of activity for nonnucleoside inhibitors with HIV-1 reverse transcriptase based on Monte Carlo simulations.Journal of medicinal chemistry, , Jul-04, Volume: 45, Issue:14, 2002
Antiviral drug design: computational analyses of the effects of the L100I mutation for HIV-RT on the binding of NNRTIs.Bioorganic & medicinal chemistry letters, , Nov-05, Volume: 11, Issue:21, 2001
Prediction of the binding free energies of new TIBO-like HIV-1 reverse transcriptase inhibitors using a combination of PROFEC, PB/SA, CMC/MD, and free energy calculations.Journal of medicinal chemistry, , Mar-11, Volume: 42, Issue:5, 1999
Prediction of binding affinities for TIBO inhibitors of HIV-1 reverse transcriptase using Monte Carlo simulations in a linear response method.Journal of medicinal chemistry, , Dec-17, Volume: 41, Issue:26, 1998
Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors. 1. Synthesis and basic structure-activity relationship studies of PETT analogs.Journal of medicinal chemistry, , Dec-08, Volume: 38, Issue:25, 1995
The inophyllums, novel inhibitors of HIV-1 reverse transcriptase isolated from the Malaysian tree, Calophyllum inophyllum Linn.Journal of medicinal chemistry, , Dec-24, Volume: 36, Issue:26, 1993
Molecular modeling calculations of HIV-1 reverse transcriptase nonnucleoside inhibitors: correlation of binding energy with biological activity for novel 2-aryl-substituted benzimidazole analogues.Journal of medicinal chemistry, , May-08, Volume: 46, Issue:10, 2003
Prediction of activity for nonnucleoside inhibitors with HIV-1 reverse transcriptase based on Monte Carlo simulations.Journal of medicinal chemistry, , Jul-04, Volume: 45, Issue:14, 2002
Prediction of the binding free energies of new TIBO-like HIV-1 reverse transcriptase inhibitors using a combination of PROFEC, PB/SA, CMC/MD, and free energy calculations.Journal of medicinal chemistry, , Mar-11, Volume: 42, Issue:5, 1999
Prediction of binding affinities for TIBO inhibitors of HIV-1 reverse transcriptase using Monte Carlo simulations in a linear response method.Journal of medicinal chemistry, , Dec-17, Volume: 41, Issue:26, 1998
Comparative molecular moment analysis (CoMMA): 3D-QSAR without molecular superposition.Journal of medicinal chemistry, , May-24, Volume: 39, Issue:11, 1996
[d4U]-spacer-[HI-236] double-drug inhibitors of HIV-1 reverse-transcriptase.Bioorganic & medicinal chemistry, , Jul-01, Volume: 18, Issue:13, 2010
C-2-aryl O-substituted HI-236 derivatives as non-nucleoside HIV-1 reverse-transcriptase inhibitors.Bioorganic & medicinal chemistry, , Dec-15, Volume: 16, Issue:24, 2008
Antioxidant function of phenethyl-5-bromo-pyridyl thiourea compounds with potent anti-HIV activity.Bioorganic & medicinal chemistry letters, , Jan-03, Volume: 10, Issue:1, 2000
Rational design of N-[2-(2,5-dimethoxyphenylethyl)]-N'-[2-(5-bromopyridyl)]-thiourea (HI-236) as a potent non-nucleoside inhibitor of drug-resistant human immunodeficiency virus.Bioorganic & medicinal chemistry letters, , Jun-07, Volume: 9, Issue:11, 1999
Parallel one-pot synthesis and structure-activity relationship study of symmetric formimidoester disulfides as a novel class of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.Bioorganic & medicinal chemistry, , Jun-15, Volume: 16, Issue:12, 2008
Thiocarbamates as non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 2: Parallel synthesis, molecular modelling and structure-activity relationship studies on analogues of O-(2-phenylethyl)-N-phenylthiocarbamate.Bioorganic & medicinal chemistry, , Apr-01, Volume: 16, Issue:7, 2008
Design, synthesis, SAR, and molecular modeling studies of acylthiocarbamates: a novel series of potent non-nucleoside HIV-1 reverse transcriptase inhibitors structurally related to phenethylthiazolylthiourea derivatives.Journal of medicinal chemistry, , Feb-27, Volume: 46, Issue:5, 2003
Prediction of activity for nonnucleoside inhibitors with HIV-1 reverse transcriptase based on Monte Carlo simulations.Journal of medicinal chemistry, , Jul-04, Volume: 45, Issue:14, 2002
Stereochemistry of halopyridyl and thiazolyl thiourea compounds is a major determinant of their potency as nonnucleoside inhibitors of HIV-1 reverse transcriptase.Bioorganic & medicinal chemistry letters, , Sep-18, Volume: 10, Issue:18, 2000
N-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea and N'-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-chloropyridyl)]-thiourea as potent inhibitors of multidrug-resistant human immunodeficiency virus-1.Bioorganic & medicinal chemistry letters, , Sep-20, Volume: 9, Issue:18, 1999
N'-[2-(2-thiophene)ethyl]-N'-[2-(5-bromopyridyl)] thiourea as a potent inhibitor of NNI-resistant and multidrug-resistant human immunodeficiency virus-1.Bioorganic & medicinal chemistry letters, , Dec-20, Volume: 9, Issue:24, 1999
Rational design of N-[2-(2,5-dimethoxyphenylethyl)]-N'-[2-(5-bromopyridyl)]-thiourea (HI-236) as a potent non-nucleoside inhibitor of drug-resistant human immunodeficiency virus.Bioorganic & medicinal chemistry letters, , Jun-07, Volume: 9, Issue:11, 1999
Synthesis and anti-HIV activities of urea-PETT analogs belonging to a new class of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.Bioorganic & medicinal chemistry letters, , Jun-16, Volume: 8, Issue:12, 1998
Phenethylthiazolylthiourea (PETT) compounds as a new class of HIV-1 reverse transcriptase inhibitors. 2. Synthesis and further structure-activity relationship studies of PETT analogs.Journal of medicinal chemistry, , Oct-11, Volume: 39, Issue:21, 1996
Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors. 1. Synthesis and basic structure-activity relationship studies of PETT analogs.Journal of medicinal chemistry, , Dec-08, Volume: 38, Issue:25, 1995
Prediction of activity for nonnucleoside inhibitors with HIV-1 reverse transcriptase based on Monte Carlo simulations.Journal of medicinal chemistry, , Jul-04, Volume: 45, Issue:14, 2002
Antiviral drug design: computational analyses of the effects of the L100I mutation for HIV-RT on the binding of NNRTIs.Bioorganic & medicinal chemistry letters, , Nov-05, Volume: 11, Issue:21, 2001
Recent developments of 2-aminothiazoles in medicinal chemistry.European journal of medicinal chemistry, , Feb-15, Volume: 109, 2016
Prediction of activity for nonnucleoside inhibitors with HIV-1 reverse transcriptase based on Monte Carlo simulations.Journal of medicinal chemistry, , Jul-04, Volume: 45, Issue:14, 2002
Synthesis and anti-HIV activities of urea-PETT analogs belonging to a new class of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.Bioorganic & medicinal chemistry letters, , Jun-16, Volume: 8, Issue:12, 1998
Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors. 1. Synthesis and basic structure-activity relationship studies of PETT analogs.Journal of medicinal chemistry, , Dec-08, Volume: 38, Issue:25, 1995
N-Substituted Quinolinonyl Diketo Acid Derivatives as HIV Integrase Strand Transfer Inhibitors and Their Activity against RNase H Function of Reverse Transcriptase.Journal of medicinal chemistry, , Jun-11, Volume: 58, Issue:11, 2015
Basic quinolinonyl diketo acid derivatives as inhibitors of HIV integrase and their activity against RNase H function of reverse transcriptase.Journal of medicinal chemistry, , Apr-24, Volume: 57, Issue:8, 2014
Efavirenz a nonnucleoside reverse transcriptase inhibitor of first-generation: Approaches based on its medicinal chemistry.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Trifluoromethyl-containing 3-alkoxymethyl- and 3-aryloxymethyl-2-pyridinones are potent inhibitors of HIV-1 non-nucleoside reverse transcriptase.Bioorganic & medicinal chemistry letters, , Feb-12, Volume: 11, Issue:3, 2001
3,3a-Dihydropyrano[4,3,2-de]quinazolin-2(1H)-ones are potent non-nucleoside reverse transcriptase inhibitors.Bioorganic & medicinal chemistry letters, , Jan-22, Volume: 11, Issue:2, 2001
4,1-Benzoxazepinone analogues of efavirenz (Sustiva) as HIV-1 reverse transcriptase inhibitors.Bioorganic & medicinal chemistry letters, , Jun-04, Volume: 11, Issue:11, 2001
Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK.Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors.Journal of medicinal chemistry, , 03-10, Volume: 65, Issue:5, 2022
Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies.Journal of medicinal chemistry, , 09-23, Volume: 64, Issue:18, 2021
[no title available]Journal of medicinal chemistry, , 09-23, Volume: 64, Issue:18, 2021
Covalent Inhibition of Wild-Type HIV-1 Reverse Transcriptase Using a Fluorosulfate Warhead.ACS medicinal chemistry letters, , Feb-11, Volume: 12, Issue:2, 2021
[no title available]Journal of medicinal chemistry, , 05-14, Volume: 63, Issue:9, 2020
Molecular and cellular studies evaluating a potent 2-cyanoindolizine catechol diether NNRTI targeting wildtype and Y181C mutant HIV-1 reverse transcriptase.Bioorganic & medicinal chemistry letters, , 08-15, Volume: 29, Issue:16, 2019
[no title available]Journal of medicinal chemistry, , 02-28, Volume: 62, Issue:4, 2019
Biological evaluation of molecules of the azaBINOL class as antiviral agents: Inhibition of HIV-1 RNase H activity by 7-isopropoxy-8-(naphth-1-yl)quinoline.Bioorganic & medicinal chemistry, , 08-15, Volume: 27, Issue:16, 2019
Drug-like property-driven optimization of 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against rilpivirine-resistant mutant virus.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 27, Issue:12, 2017
Potent Inhibitors Active against HIV Reverse Transcriptase with K101P, a Mutation Conferring Rilpivirine Resistance.ACS medicinal chemistry letters, , Oct-08, Volume: 6, Issue:10, 2015
Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors.European journal of medicinal chemistry, , Volume: 65, 2013
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.Antimicrobial agents and chemotherapy, , Volume: 54, Issue:2, 2010
Chromenone derivatives as a versatile scaffold with dual mode of inhibition of HIV-1 reverse transcriptase-associated Ribonuclease H function and integrase activity.European journal of medicinal chemistry, , Nov-15, Volume: 182, 2019
(3Z)-3-(2-[4-(aryl)-1,3-thiazol-2-yl]hydrazin-1-ylidene)-2,3-dihydro-1H-indol-2-one derivatives as dual inhibitors of HIV-1 reverse transcriptase.European journal of medicinal chemistry, , Mar-26, Volume: 93, 2015
6-(1-Benzyl-1H-pyrrol-2-yl)-2,4-dioxo-5-hexenoic acids as dual inhibitors of recombinant HIV-1 integrase and ribonuclease H, synthesized by a parallel synthesis approach.Journal of medicinal chemistry, , Nov-14, Volume: 56, Issue:21, 2013
Development of a series of 3-hydroxyquinolin-2(1H)-ones as selective inhibitors of HIV-1 reverse transcriptase associated RNase H activity.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 22, Issue:12, 2012
Design, synthesis, and anti-HIV activity of 4'-modified carbocyclic nucleoside phosphonate reverse transcriptase inhibitors.Bioorganic & medicinal chemistry, , Feb-15, Volume: 17, Issue:4, 2009
Synthesis and anti-HIV activity of GS-9148 (2'-Fd4AP), a novel nucleoside phosphonate HIV reverse transcriptase inhibitor.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 18, Issue:3, 2008
Discovery of Phenylaminopyridine Derivatives as Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors.ACS medicinal chemistry letters, , Aug-09, Volume: 3, Issue:8, 2012
Design and synthesis of pyridone inhibitors of non-nucleoside reverse transcriptase.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 21, Issue:24, 2011
Design and synthesis of conformationally constrained inhibitors of non-nucleoside reverse transcriptase.Journal of medicinal chemistry, , Nov-24, Volume: 54, Issue:22, 2011
Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.Journal of medicinal chemistry, , Nov-26, Volume: 52, Issue:22, 2009
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.Antimicrobial agents and chemotherapy, , Volume: 53, Issue:6, 2009
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.Journal of medicinal chemistry, , Oct-23, Volume: 51, Issue:20, 2008
Pharmacophore-based design of novel 3-hydroxypyrimidine-2,4-dione subtypes as inhibitors of HIV reverse transcriptase-associated RNase H: Tolerance of a nonflexible linker.European journal of medicinal chemistry, , Mar-15, Volume: 166, 2019
6-Arylthio-3-hydroxypyrimidine-2,4-diones potently inhibited HIV reverse transcriptase-associated RNase H with antiviral activity.European journal of medicinal chemistry, , Aug-05, Volume: 156, 2018
Design, synthesis and biological evaluations of N-Hydroxy thienopyrimidine-2,4-diones as inhibitors of HIV reverse transcriptase-associated RNase H.European journal of medicinal chemistry, , Dec-01, Volume: 141, 2017
3-Hydroxypyrimidine-2,4-dione-5-N-benzylcarboxamides Potently Inhibit HIV-1 Integrase and RNase H.Journal of medicinal chemistry, , 07-14, Volume: 59, Issue:13, 2016
N-Substituted Quinolinonyl Diketo Acid Derivatives as HIV Integrase Strand Transfer Inhibitors and Their Activity against RNase H Function of Reverse Transcriptase.Journal of medicinal chemistry, , Jun-11, Volume: 58, Issue:11, 2015
Basic quinolinonyl diketo acid derivatives as inhibitors of HIV integrase and their activity against RNase H function of reverse transcriptase.Journal of medicinal chemistry, , Apr-24, Volume: 57, Issue:8, 2014
Pharmacophore-based design of novel 3-hydroxypyrimidine-2,4-dione subtypes as inhibitors of HIV reverse transcriptase-associated RNase H: Tolerance of a nonflexible linker.European journal of medicinal chemistry, , Mar-15, Volume: 166, 2019
6-Arylthio-3-hydroxypyrimidine-2,4-diones potently inhibited HIV reverse transcriptase-associated RNase H with antiviral activity.European journal of medicinal chemistry, , Aug-05, Volume: 156, 2018
3-Hydroxypyrimidine-2,4-dione-5-N-benzylcarboxamides Potently Inhibit HIV-1 Integrase and RNase H.Journal of medicinal chemistry, , 07-14, Volume: 59, Issue:13, 2016
[no title available]European journal of medicinal chemistry, , Oct-05, Volume: 240, 2022
Design, synthesis and biological evaluation of novel acetamide-substituted doravirine and its prodrugs as potent HIV-1 NNRTIs.Bioorganic & medicinal chemistry, , 02-01, Volume: 27, Issue:3, 2019
Synopsis of some recent tactical application of bioisosteres in drug design.Journal of medicinal chemistry, , Apr-28, Volume: 54, Issue:8, 2011
Synthesis, antiviral activity, cytotoxicity and cellular pharmacology of l-3'-azido-2',3'-dideoxypurine nucleosides.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
Anti-human immunodeficiency virus activity, cross-resistance, cytotoxicity, and intracellular pharmacology of the 3'-azido-2',3'-dideoxypurine nucleosides.Antimicrobial agents and chemotherapy, , Volume: 53, Issue:9, 2009
Anti-human immunodeficiency virus activity, cross-resistance, cytotoxicity, and intracellular pharmacology of the 3'-azido-2',3'-dideoxypurine nucleosides.Antimicrobial agents and chemotherapy, , Volume: 53, Issue:9, 2009
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.Antimicrobial agents and chemotherapy, , Volume: 51, Issue:6, 2007