Netropsin is a naturally occurring oligopeptide antibiotic that binds to DNA. Its synthesis involves a multi-step process using amino acid building blocks. Netropsin exhibits a strong affinity for AT-rich regions in DNA, specifically the minor groove, and this binding disrupts DNA replication and transcription. Its antitumor activity and potential as a research tool for studying DNA structure and function have made it an important subject of scientific investigation. The ability of netropsin to bind specifically to DNA has led to its use as a probe for investigating DNA structure and dynamics. Furthermore, netropsin has been modified and studied to improve its therapeutic potential and explore its use as a molecular tool for regulating gene expression.'
Netropsin: A basic polypeptide isolated from Streptomyces netropsis. It is cytotoxic and its strong, specific binding to A-T areas of DNA is useful to genetics research. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 4461 |
| CHEMBL ID | 307767 |
| SCHEMBL ID | 197747 |
| SCHEMBL ID | 24312520 |
| MeSH ID | M0014675 |
| Synonym |
|---|
| 64b3o0rd7n , |
| unii-64b3o0rd7n |
| 4-22-00-06712 (beilstein handbook reference) |
| bdbm50055660 |
| 4-(2-guanidino-acetylamino)-1-methyl-1h-pyrrole-2-carboxylic acid [5-(2-carbamimidoyl-ethylcarbamoyl)-1-methyl-2,3-dihydro-1h-pyrrol-3-yl]-amide |
| 2n-(3-amino-3-iminopropyl)-4-[4-amino(imino)methylaminomethylcarboxamido-1-methyl-1h-2-pyrrolylcarboxamido]-1-methyl-1h-2-pyrrolecarboxamide |
| 1-amino-3-(4-(4-(2-(amino(iminio)methylamino)acetamido)-1-methyl-1h-pyrrole-2-carboxamido)-1-methyl-1h-pyrrole-2-carboxamido)propan-1-iminium |
| 2n-(3-amino-3-iminopropyl)-4-[4-amino(imino)methylaminomethylcarboxamido-1-methyl-1h-2-pyrrolylcarboxamido]-1-methyl-1h-2-pyrrolecarboxamide(netropsin) |
| NCI60_002614 |
| antibiotic t-1384 |
| ch-777-a |
| nsc 3067 |
| k-117 |
| f 6 |
| antibiotic 1142 |
| 2814-a |
| t-1384 |
| t 1384 |
| brn 0376913 |
| n,4'-bi(pyrrole-2-carboxamide), n'-(2-carbamoylethyl)-4-((2-guanidinoacetimidoyl)amino)-1,1'-dimethyl- |
| 4-(2-carbamimidamidoacetamido)-n-{5-[(2-carbamimidoylethyl)carbamoyl]-1-methyl-1h-pyrrol-3-yl}-1-methyl-1h-pyrrole-2-carboxamide |
| bdbm17 |
| sinanomycin |
| 1438-30-8 |
| netropsin |
| congocidin |
| HSCI1_000283 |
| CHEMBL307767 , |
| n-[5-[(3-amino-3-iminopropyl)carbamoyl]-1-methylpyrrol-3-yl]-4-[[2-(diaminomethylideneamino)acetyl]amino]-1-methylpyrrole-2-carboxamide |
| netropsin dihydrochloride |
| 4-((((aminoiminomethyl)amino)acetyl)amino)-n-(5-(((3-amino-3-iminopropyl)amino)carbonyl)-1-methyl-1h-pyrrol-3-yl)-1-methyl-1h-pyrrole-2-carboxamide |
| netropsin [mi] |
| n'-(2-amidinoethyl)-4-(2-guanidinoacetamido)-1,1'-dimethyl-n,4'-bi(pyrrole-2-carboxamide) |
| IDBIFFKSXLYUOT-UHFFFAOYSA-N |
| SCHEMBL197747 |
| J-007877 |
| n-(5-{[(3z)-3-amino-3-iminopropyl]carbamoyl}-1-methyl-1h-pyrrol-3-yl)-4-[(n-carbamimidoylglycyl)amino]-1-methyl-1h-pyrrole-2-carboxamide |
| DTXSID00879834 |
| Q3874969 |
| n-(3-amino-3-iminopropyl)-4-(4-(2-guanidinoacetamido)-1-methyl-1h-pyrrole-2-carboxamido)-1-methyl-1h-pyrrole-2-carboxamide |
| antibiotic t 1384 |
| antibiotic t1384 |
| SCHEMBL24312520 |
| AKOS040744856 |
Netropsin is a dication that specifically binds primarily by hydrogen bonding in the minor groove at sites that have four or more contiguous A.T base pairs. It is a model for the study of drug-DNA interactions.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Netropsin is a dication that specifically binds primarily by hydrogen bonding in the minor groove at sites that have four or more contiguous A.T base pairs." | ( Effect of netropsin on one-electron oxidation of duplex DNA. Roberts, LW; Schuster, GB, ) | 1.26 |
| "Netropsin is a well-characterized DNA minor groove binding compound that serves as a model for the study of drug-DNA interactions. " | ( A host-guest approach for determining drug-DNA interactions: an example using netropsin. Georgiadis, MM; Goodwin, KD; Long, EC, 2005) | 2 |
Netropsin has been found to be in a fast chemical exchange with all three kinds of quadruplexes. Dist-A interacts tightly with Q1 and, at a less extent, with Q2. The molecule has an intrinsic twist that favors insertion into the minor groove of B-DNA.
| Excerpt | Reference | Relevance |
|---|---|---|
| "The netropsin molecule has an intrinsic twist that favors insertion into the minor groove of B-DNA, and it is given a small additional twist upon binding." | ( The molecular origin of DNA-drug specificity in netropsin and distamycin. Dickerson, RE; Goodsell, D; Kopka, ML; Pjura, P; Yoon, C, 1985) | 1.01 |
| "Netropsin, for example, has two DNA binding enthalpies in isothermal titration calorimetry (ITC) experiments that indicate the compound simultaneously forms two thermodynamically different complexes at a single AATT site." | ( Complexity in the binding of minor groove agents: netropsin has two thermodynamically different DNA binding modes at a single site. Le, V; Lewis, EA; Machha, V; Munde, M; Rettig, M; Wang, S; Wilson, WD, 2011) | 1.34 |
| "Netropsin has been found to be in a fast chemical exchange with all three kinds of quadruplexes, whereas Dist-A interacts tightly with Q1 and, at a less extent, with Q2." | ( Interaction of distamycin A and netropsin with quadruplex and duplex structures: a comparative 1H-NMR study. Esposito, V; Galeone, A; Mayol, L; Randazzo, A; Varra, M, 2002) | 1.32 |
| "Netropsin-diazene has fulfilled all of the design criteria, binding to the DNA duplex studied in the minor groove of the central AAAA tract in a 1:1 mode, preventing diyl dimerization and other side reactions from occurring." | ( The binding modes of a rationally designed photoactivated DNA nuclease determined by NMR. Bregant, TM; Fagan, PA; Little, RD; Spielmann, HP; Wemmer, DE, 1995) | 1.01 |
| "The netropsin molecule has an intrinsic twist that favors insertion into the minor groove of B-DNA, and it is given a small additional twist upon binding." | ( The molecular origin of DNA-drug specificity in netropsin and distamycin. Dickerson, RE; Goodsell, D; Kopka, ML; Pjura, P; Yoon, C, 1985) | 1.01 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " Distamycin A readily inhibited nucleic acid and protein synthesis and was more toxic to the ring stage than to the trophozoite stage in various parasite strains, irrespective of their susceptibility to chloroquine." | ( Selective toxicity to malaria parasites by non-intercalating DNA-binding ligands. Ginsburg, H; Krugliak, M; Nissani, E; Williamson, DH, 1993) | 0.29 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Plasminogen | Homo sapiens (human) | IC50 (µMol) | 35.0000 | 0.0250 | 3.6280 | 10.0000 | AID1802946 |
| Urokinase-type plasminogen activator | Homo sapiens (human) | IC50 (µMol) | 35.0000 | 0.0370 | 3.3859 | 10.0000 | AID1802946 |
| Trypsin-1 | Homo sapiens (human) | IC50 (µMol) | 35.0000 | 0.0035 | 1.5321 | 10.0000 | AID1802946 |
| DNA topoisomerase 1 | Homo sapiens (human) | IC50 (µMol) | 62.0000 | 0.0210 | 1.8626 | 10.0000 | AID211100 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1802684 | DNA-Dependent ATPase Assay from Article 10.1186/1471-2091-15-9: \\Plasmodium falciparum UvrD activities are downregulated by DNA-interacting compounds and its dsRNA inhibits malaria parasite growth.\\ | 2014 | BMC biochemistry, Apr-03, Volume: 15 | Plasmodium falciparum UvrD activities are downregulated by DNA-interacting compounds and its dsRNA inhibits malaria parasite growth. |
| AID1802685 | DNA Helicase Assay from Article 10.1186/1471-2091-15-9: \\Plasmodium falciparum UvrD activities are downregulated by DNA-interacting compounds and its dsRNA inhibits malaria parasite growth.\\ | 2014 | BMC biochemistry, Apr-03, Volume: 15 | Plasmodium falciparum UvrD activities are downregulated by DNA-interacting compounds and its dsRNA inhibits malaria parasite growth. |
| AID1802946 | Antiamidolytic Assay from Article 10.3109/14756360903389872: \\Carbocyclic potential DNA minor groove binders and their biological evaluation.\\ | 2010 | Journal of enzyme inhibition and medicinal chemistry, Oct, Volume: 25, Issue:5 | Carbocyclic potential DNA minor groove binders and their biological evaluation. |
| AID54423 | Denaturation temperature change on binding to AT to poly (dA)-poly(dT) | 1992 | Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3 | Structure and DNA binding activity of analogues of 1,5-bis(4-amidinophenoxy)pentane (pentamidine) |
| AID485536 | Inhibition of topoisomerase 1-mediated relaxation of supercoiled pBR322 DNA at 20 uM after 20 mins using ethidium bromide staining by electrophoresis relative to control | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11 | Design, synthesis and biological evaluation of a novel series of anthrapyrazoles linked with netropsin-like oligopyrrole carboxamides as anticancer agents. |
| AID691547 | Growth inhibition of human K562 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID38325 | Dose required to inhibit Human B-Lymphoblast (Raji) cell proliferation by 50% | 1989 | Journal of medicinal chemistry, May, Volume: 32, Issue:5 | Synthesis, DNA binding, and biological evaluation of synthetic precursors and novel analogues of netropsin. |
| AID691591 | Growth inhibition of human PC3 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID691585 | Growth inhibition of human ACHN cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID95872 | Inhibitory concentration that reduced the viability of KB cell population by 50%. | 1997 | Journal of medicinal chemistry, Jan-17, Volume: 40, Issue:2 | Camptothecin and minor-groove binder hybrid molecules: synthesis, inhibition of topoisomerase I, and anticancer cytotoxicity in vitro. |
| AID425485 | Displacement of ethidium bromide from DNA ATAT region by CIS-FID analysis | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14 | CSI-FID: high throughput label-free detection of DNA binding molecules. |
| AID161449 | Minimum cytotoxic concentration required to cause a microscopically detectable alteration of normal cell morphology and show antiviral activity in primary rabbit kidney (PRK) cells | 1989 | Journal of medicinal chemistry, May, Volume: 32, Issue:5 | Synthesis, DNA binding, and biological evaluation of synthetic precursors and novel analogues of netropsin. |
| AID225773 | Association constant against polynucleotide poly (dG-dC) | 1989 | Journal of medicinal chemistry, May, Volume: 32, Issue:5 | Synthesis, DNA binding, and biological evaluation of synthetic precursors and novel analogues of netropsin. |
| AID54424 | Denaturation temperature change on binding on GC to poly(dGC)-poly(dGC) | 1992 | Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3 | Structure and DNA binding activity of analogues of 1,5-bis(4-amidinophenoxy)pentane (pentamidine) |
| AID425456 | Binding affinity to DNA minor groove region CGCAAATTTGCG assessed as melting temperature at 6 uM by thermal denaturation study | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14 | Synthesis and evaluation of a netropsin-proximicin-hybrid library for DNA binding and cytotoxicity. |
| AID691575 | Growth inhibition of human SK-MEL-5 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID649516 | Antimicrobial activity against Staphylococcus aureus SA 1199B over-expressing NorA MDR efflux pump after 24 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6 | Efficient synthesis and biological evaluation of proximicins A, B and C. |
| AID691556 | Growth inhibition of human NCI-322M cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID425475 | Displacement of ethidium bromide from minor groove region of DNA at 3 uM by CIS-FID analysis | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14 | CSI-FID: high throughput label-free detection of DNA binding molecules. |
| AID691580 | Growth inhibition of human OVCAR4 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID142334 | Dose required to inhibit Murine leukemia (L1210) cell proliferation by 50% | 1989 | Journal of medicinal chemistry, May, Volume: 32, Issue:5 | Synthesis, DNA binding, and biological evaluation of synthetic precursors and novel analogues of netropsin. |
| AID395133 | Binding affinity to poly(dA).poly(dT) duplex DNA assessed as ratio of KA to KB by ESI-MS analysis | 2008 | European journal of medicinal chemistry, Nov, Volume: 43, Issue:11 | Ligand binding to nucleic acids and proteins: Does selectivity increase with strength? |
| AID649519 | Antimicrobial activity against Escherichia coli NCTC 10418 after 24 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6 | Efficient synthesis and biological evaluation of proximicins A, B and C. |
| AID1196717 | Inhibition of Staphylococcus aureus UPPS using FPP/IPP as substrate by spectrophotometry | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3 | Antibacterial drug leads: DNA and enzyme multitargeting. |
| AID425480 | Displacement of ethidium bromide from DNA AAAA region by CIS-FID analysis | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14 | CSI-FID: high throughput label-free detection of DNA binding molecules. |
| AID691558 | Growth inhibition of human HCC2998 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID691588 | Growth inhibition of human SN12C cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID54426 | Denaturation temperature change on binding to calf thymus DNA | 1992 | Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3 | Structure and DNA binding activity of analogues of 1,5-bis(4-amidinophenoxy)pentane (pentamidine) |
| AID465964 | Binding affinity to poly dA/dT DNA assessed as change in melting temperature by thermal denaturation assay | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5 | Semi-automated high-throughput fluorescent intercalator displacement-based discovery of cytotoxic DNA binding agents from a large compound library. |
| AID425459 | Binding affinity to DNA minor groove region CATGGCCATG assessed as change in melting temperature at 6 uM by thermal denaturation study | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14 | Synthesis and evaluation of a netropsin-proximicin-hybrid library for DNA binding and cytotoxicity. |
| AID691555 | Growth inhibition of human NCI-H23 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID691564 | Growth inhibition of human SF295 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID691552 | Growth inhibition of human HOP62 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID469768 | Binding affinity to Poly(dA.dT)2 DNA in phosphate buffer assessed as change in melting temperature | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22 | Asymmetrical diaromatic guanidinium/2-aminoimidazolinium derivatives: synthesis and DNA affinity. |
| AID691546 | Growth inhibition of human HL60 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID691562 | Growth inhibition of human SW620 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID691557 | Growth inhibition of human NCI-H522 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID691548 | Growth inhibition of human RPMI8226 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID1196720 | Binding affinity to DNA dodecamer complex (CGCGAATTCGCG)2 (unknown origin) assessed as change in melting temperature by differential scanning calorimetry | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3 | Antibacterial drug leads: DNA and enzyme multitargeting. |
| AID691545 | Growth inhibition of human CCRF-CEM cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID485537 | Binding affinity to calf thymus DNA assessed as increase in melting temperature at 1 uM by spectrophotometer analysis | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11 | Design, synthesis and biological evaluation of a novel series of anthrapyrazoles linked with netropsin-like oligopyrrole carboxamides as anticancer agents. |
| AID691579 | Growth inhibition of human OVCAR3 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID649517 | Antimicrobial activity against epidemic methicillin-resistant Staphylococcus aureus 15 after 24 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6 | Efficient synthesis and biological evaluation of proximicins A, B and C. |
| AID485542 | Resistant factor, ratio of IC50 human K/VP.5 cells to IC50 for human K562 cells | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11 | Design, synthesis and biological evaluation of a novel series of anthrapyrazoles linked with netropsin-like oligopyrrole carboxamides as anticancer agents. |
| AID691668 | Growth inhibition of human HCT116 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID485541 | Cytotoxicity against human K/VP.5 cells after 72 hrs by MTS assay | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11 | Design, synthesis and biological evaluation of a novel series of anthrapyrazoles linked with netropsin-like oligopyrrole carboxamides as anticancer agents. |
| AID691595 | Growth inhibition of human BT549 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID691571 | Growth inhibition of human M14 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID425487 | Displacement of ethidium bromide from DNA TTAA region by CIS-FID analysis | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14 | CSI-FID: high throughput label-free detection of DNA binding molecules. |
| AID691577 | Growth inhibition of human UACC62 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID485543 | Cytotoxicity against hamster DC-3F cells | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11 | Design, synthesis and biological evaluation of a novel series of anthrapyrazoles linked with netropsin-like oligopyrrole carboxamides as anticancer agents. |
| AID218401 | Minimum inhibitory concentration required to reduce Coxsackie virus B4 induced cytopathogenicity by 50% in african green monkey (VeroB) cells | 1989 | Journal of medicinal chemistry, May, Volume: 32, Issue:5 | Synthesis, DNA binding, and biological evaluation of synthetic precursors and novel analogues of netropsin. |
| AID1196716 | Inhibition of Escherichia coli UPPS using FPP/IPP as substrate by spectrophotometry | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3 | Antibacterial drug leads: DNA and enzyme multitargeting. |
| AID425483 | Displacement of ethidium bromide from DNA ATTA region by CIS-FID analysis | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14 | CSI-FID: high throughput label-free detection of DNA binding molecules. |
| AID425476 | Displacement of ethidium bromide from DNA TAGAATA region at 3 uM by CIS-FID analysis | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14 | CSI-FID: high throughput label-free detection of DNA binding molecules. |
| AID691570 | Growth inhibition of human MALME-3M cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID210142 | Dose required to inhibit Human T-Lymphoblast (Molt/4F) cell proliferation by 50% | 1989 | Journal of medicinal chemistry, May, Volume: 32, Issue:5 | Synthesis, DNA binding, and biological evaluation of synthetic precursors and novel analogues of netropsin. |
| AID691593 | Growth inhibition of human MDA-MB-231 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID54252 | Relative binding constant to calf thymus DNA | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | Novel linked antiviral and antitumor agents related to netropsin and distamycin: synthesis and biological evaluation. |
| AID54425 | DNA binding property estimated by measuring denaturation temperature on GC to poly (dGC)-poly(dGC), normalized to ethidium bromide | 1992 | Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3 | Structure and DNA binding activity of analogues of 1,5-bis(4-amidinophenoxy)pentane (pentamidine) |
| AID691565 | Growth inhibition of human SF539 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID691589 | Growth inhibition of human TK10 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID1445928 | Stabilization of FAM/TAMRA-labeled AT-rich DNA duplex (unknown origin) assessed as change in melting temperature at 5 uM by FRET-based assay | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | Triaryl Benzimidazoles as a New Class of Antibacterial Agents against Resistant Pathogenic Microorganisms. |
| AID200294 | Inhibitory concentration that reduced the viability of SKVLB cell population by 50%. | 1997 | Journal of medicinal chemistry, Jan-17, Volume: 40, Issue:2 | Camptothecin and minor-groove binder hybrid molecules: synthesis, inhibition of topoisomerase I, and anticancer cytotoxicity in vitro. |
| AID54427 | DNA binding activity as denaturation temperatures on AT to poly (dA)-poly(dT) normalized to ethidium bromide | 1992 | Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3 | Structure and DNA binding activity of analogues of 1,5-bis(4-amidinophenoxy)pentane (pentamidine) |
| AID691583 | Growth inhibition of human NCI-ADR-RES cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID218402 | Minimum inhibitory concentration required to reduce Sindbis virus induced cytopathogenicity by 50% in african green monkey (VeroB) cells | 1989 | Journal of medicinal chemistry, May, Volume: 32, Issue:5 | Synthesis, DNA binding, and biological evaluation of synthetic precursors and novel analogues of netropsin. |
| AID54984 | Thermal denaturation in sonicated calf thymus DNA (CT DNA) | 1993 | Journal of medicinal chemistry, Jun-11, Volume: 36, Issue:12 | Structure, DNA minor groove binding, and base pair specificity of alkyl- and aryl-linked bis(amidinobenzimidazoles) and bis(amidinoindoles). |
| AID218406 | Minimum inhibitory concentration required to reduce semliki forest virus induced cytopathogenicity by 50% in african green monkey (VeroB) cells | 1989 | Journal of medicinal chemistry, May, Volume: 32, Issue:5 | Synthesis, DNA binding, and biological evaluation of synthetic precursors and novel analogues of netropsin. |
| AID691576 | Growth inhibition of human UACC257 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID478754 | Binding affinity to d(CGCGAATTCGCG)2 dodecamer assessed as change in melting temperature | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5 | Theoretical models of pentamidine analogs activity based on their DNA minor groove complexes. |
| AID1698748 | Binding affinity to calf thymus DNA assessed as change in melting temperature at DNA to ligand ratio at 40:1 by spectrophotometric method | 2020 | Journal of natural products, 10-23, Volume: 83, Issue:10 | Synthesis and Stereochemical Assignment of Conioidine A: DNA- and HSA-Binding Studies of the Four Diastereomers. |
| AID691592 | Growth inhibition of human MCF7 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID691578 | Growth inhibition of human IGROV1 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID691553 | Growth inhibition of human HOP92 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID465963 | Binding affinity to calf thymus DNA assessed as decrease in ethidium bromide fluorescence at 10 uM by HT-FID assay | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5 | Semi-automated high-throughput fluorescent intercalator displacement-based discovery of cytotoxic DNA binding agents from a large compound library. |
| AID48651 | Dose required to inhibit Murine mammary carcinoma (FM3A) cell proliferation by 50% | 1989 | Journal of medicinal chemistry, May, Volume: 32, Issue:5 | Synthesis, DNA binding, and biological evaluation of synthetic precursors and novel analogues of netropsin. |
| AID691596 | Growth inhibition of human T47D cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID425478 | Displacement of ethidium bromide from DNA TATTAGA region at 3 uM by CIS-FID analysis | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14 | CSI-FID: high throughput label-free detection of DNA binding molecules. |
| AID165910 | Inhibitory effect on the proliferation of human B lymphoblast (Raji ) cells | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | Novel linked antiviral and antitumor agents related to netropsin and distamycin: synthesis and biological evaluation. |
| AID691574 | Growth inhibition of human SK-MEL-28 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID425477 | Displacement of ethidium bromide from DNA TGAATAA region at 3 uM by CIS-FID analysis | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14 | CSI-FID: high throughput label-free detection of DNA binding molecules. |
| AID87161 | Minimum inhibitory concentration required to reduce Coxsackie virus B4 induced cytopathogenicity by 50% in HeLa cells | 1989 | Journal of medicinal chemistry, May, Volume: 32, Issue:5 | Synthesis, DNA binding, and biological evaluation of synthetic precursors and novel analogues of netropsin. |
| AID465967 | Cytotoxicity against human SF-767 cells assessed as viable cells after 72 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5 | Semi-automated high-throughput fluorescent intercalator displacement-based discovery of cytotoxic DNA binding agents from a large compound library. |
| AID1698747 | Displacement of EtBr from calf thymus DNA assessed per base pair incubated for 3 mins by fluorescence based assay | 2020 | Journal of natural products, 10-23, Volume: 83, Issue:10 | Synthesis and Stereochemical Assignment of Conioidine A: DNA- and HSA-Binding Studies of the Four Diastereomers. |
| AID156851 | Minimum inhibitory concentration required to reduce vesicular stomatitis virus induced cytopathogenicity by 50% in primary rabbit kidney cells (PRK) | 1989 | Journal of medicinal chemistry, May, Volume: 32, Issue:5 | Synthesis, DNA binding, and biological evaluation of synthetic precursors and novel analogues of netropsin. |
| AID425458 | Binding affinity to DNA minor groove region CATGGCCATG assessed as melting temperature at 6 uM by thermal denaturation study | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14 | Synthesis and evaluation of a netropsin-proximicin-hybrid library for DNA binding and cytotoxicity. |
| AID649514 | Antimicrobial activity against Staphylococcus aureus ATCC 29523 after 24 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6 | Efficient synthesis and biological evaluation of proximicins A, B and C. |
| AID425488 | Binding affinity to minor groove region of DNA | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14 | CSI-FID: high throughput label-free detection of DNA binding molecules. |
| AID425486 | Displacement of ethidium bromide from DNA TATA region by CIS-FID analysis | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14 | CSI-FID: high throughput label-free detection of DNA binding molecules. |
| AID691572 | Growth inhibition of human MDA-MB-435 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID87163 | Minimum inhibitory concentration required to reduce vesicular stomatitis virus induced cytopathogenicity by 50% in HeLa cells | 1989 | Journal of medicinal chemistry, May, Volume: 32, Issue:5 | Synthesis, DNA binding, and biological evaluation of synthetic precursors and novel analogues of netropsin. |
| AID55646 | The ionization constant (pKa) for the compound | 2000 | Journal of medicinal chemistry, Aug-24, Volume: 43, Issue:17 | DNA binding, solubility, and partitioning characteristics of extended lexitropsins. |
| AID691559 | Growth inhibition of human HCT15 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID691550 | Growth inhibition of human A549 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID1196718 | Antimicrobial activity against Escherichia coli K-12 after 3 hrs by broth microdilution method | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3 | Antibacterial drug leads: DNA and enzyme multitargeting. |
| AID233938 | Ratio between poly-dAdT and poly-dGdC binding | 1993 | Journal of medicinal chemistry, Jun-11, Volume: 36, Issue:12 | Structure, DNA minor groove binding, and base pair specificity of alkyl- and aryl-linked bis(amidinobenzimidazoles) and bis(amidinoindoles). |
| AID1445900 | Stabilization of FAM/TAMRA-labeled AT-rich DNA duplex (unknown origin) assessed as change in melting temperature at 1 uM by FRET-based assay | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | Triaryl Benzimidazoles as a New Class of Antibacterial Agents against Resistant Pathogenic Microorganisms. |
| AID649515 | Antimicrobial activity against epidemic methicillin-resistant Staphylococcus aureus 16 after 24 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6 | Efficient synthesis and biological evaluation of proximicins A, B and C. |
| AID87142 | Minimum cytotoxic concentration required to cause a microscopically detectable alteration of normal cell morphology and show antiviral activity in HeLa cells | 1989 | Journal of medicinal chemistry, May, Volume: 32, Issue:5 | Synthesis, DNA binding, and biological evaluation of synthetic precursors and novel analogues of netropsin. |
| AID31893 | Thermal denaturation in sonicated poly(dA)-poly(dT) homopolymer (AT) | 1993 | Journal of medicinal chemistry, Jun-11, Volume: 36, Issue:12 | Structure, DNA minor groove binding, and base pair specificity of alkyl- and aryl-linked bis(amidinobenzimidazoles) and bis(amidinoindoles). |
| AID425484 | Displacement of ethidium bromide from DNA AAAT region by CIS-FID analysis | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14 | CSI-FID: high throughput label-free detection of DNA binding molecules. |
| AID691549 | Growth inhibition of human SR cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID485540 | Cytotoxicity against human K562 cells after 72 hrs by MTS assay | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11 | Design, synthesis and biological evaluation of a novel series of anthrapyrazoles linked with netropsin-like oligopyrrole carboxamides as anticancer agents. |
| AID485539 | Inhibition of human recombinant topoisomerase 2 alpha assessed as stabilization of enzyme-PBR322 DNA complex at 100 uM relative to control | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11 | Design, synthesis and biological evaluation of a novel series of anthrapyrazoles linked with netropsin-like oligopyrrole carboxamides as anticancer agents. |
| AID87162 | Minimum inhibitory concentration required to reduce polio virus -1 induced cytopathogenicity by 50% in HeLa cells | 1989 | Journal of medicinal chemistry, May, Volume: 32, Issue:5 | Synthesis, DNA binding, and biological evaluation of synthetic precursors and novel analogues of netropsin. |
| AID72882 | Thermal denaturation in alternating poly(dG-dC)-poly(dG-dC) homopolymer (GC) | 1993 | Journal of medicinal chemistry, Jun-11, Volume: 36, Issue:12 | Structure, DNA minor groove binding, and base pair specificity of alkyl- and aryl-linked bis(amidinobenzimidazoles) and bis(amidinoindoles). |
| AID162422 | Association constant against the polynucleotide poly (dA-dT). | 1989 | Journal of medicinal chemistry, May, Volume: 32, Issue:5 | Synthesis, DNA binding, and biological evaluation of synthetic precursors and novel analogues of netropsin. |
| AID425481 | Displacement of ethidium bromide from DNA ATAA region by CIS-FID analysis | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14 | CSI-FID: high throughput label-free detection of DNA binding molecules. |
| AID691590 | Growth inhibition of human UO31 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID211100 | Inhibit supercoil relaxation property of topoisomerase I. | 1997 | Journal of medicinal chemistry, Jan-17, Volume: 40, Issue:2 | Camptothecin and minor-groove binder hybrid molecules: synthesis, inhibition of topoisomerase I, and anticancer cytotoxicity in vitro. |
| AID691582 | Growth inhibition of human OVCAR8 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID72032 | Inhibitory effect on the proliferation of murine mammary carcinoma (FM3A ) cells | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | Novel linked antiviral and antitumor agents related to netropsin and distamycin: synthesis and biological evaluation. |
| AID28674 | Distribution coefficient of the compound at pH 7.4 (logD) | 2000 | Journal of medicinal chemistry, Aug-24, Volume: 43, Issue:17 | DNA binding, solubility, and partitioning characteristics of extended lexitropsins. |
| AID691567 | Growth inhibition of human SNB75 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID162424 | Ratio of association constant of poly (dA-dT) and poly (dG-dC) | 1989 | Journal of medicinal chemistry, May, Volume: 32, Issue:5 | Synthesis, DNA binding, and biological evaluation of synthetic precursors and novel analogues of netropsin. |
| AID425479 | Displacement of ethidium bromide from DNA AATA region by CIS-FID analysis | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14 | CSI-FID: high throughput label-free detection of DNA binding molecules. |
| AID425457 | Binding affinity to DNA minor groove region CGCAAATTTGCG assessed as change in melting temperature at 6 uM by thermal denaturation study | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14 | Synthesis and evaluation of a netropsin-proximicin-hybrid library for DNA binding and cytotoxicity. |
| AID33367 | Minimum cytotoxic concentration required to cause a microscopically detectable alteration of normal cell morphology and show antiviral activity in african green monkey (Vero B) cells | 1989 | Journal of medicinal chemistry, May, Volume: 32, Issue:5 | Synthesis, DNA binding, and biological evaluation of synthetic precursors and novel analogues of netropsin. |
| AID691667 | Growth inhibition of human MOLT4 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID425482 | Displacement of ethidium bromide from DNA TAAA region by CIS-FID analysis | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14 | CSI-FID: high throughput label-free detection of DNA binding molecules. |
| AID691586 | Growth inhibition of human Caki1 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID23682 | Partition coefficient of the compound (logP) | 2000 | Journal of medicinal chemistry, Aug-24, Volume: 43, Issue:17 | DNA binding, solubility, and partitioning characteristics of extended lexitropsins. |
| AID218404 | Minimum inhibitory concentration required to reduce parainfluenza virus-3 induced cytopathogenicity by 50% in african green monkey (VeroB) cells | 1989 | Journal of medicinal chemistry, May, Volume: 32, Issue:5 | Synthesis, DNA binding, and biological evaluation of synthetic precursors and novel analogues of netropsin. |
| AID691587 | Growth inhibition of human RXF393 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID1196719 | Antimicrobial activity against Staphylococcus aureus Newman after 9 hrs by spectrophotometry | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3 | Antibacterial drug leads: DNA and enzyme multitargeting. |
| AID691566 | Growth inhibition of human SNB19 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID465965 | Binding affinity to G/C-rich DNA oligonucleotide assessed as change in melting temperature by thermal denaturation assay | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5 | Semi-automated high-throughput fluorescent intercalator displacement-based discovery of cytotoxic DNA binding agents from a large compound library. |
| AID691597 | Growth inhibition of human MDA-MB-468 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID691554 | Growth inhibition of human NCI-H226 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID84455 | Inhibitory concentration that reduced the viability of HT 29 cell population by 50%. | 1997 | Journal of medicinal chemistry, Jan-17, Volume: 40, Issue:2 | Camptothecin and minor-groove binder hybrid molecules: synthesis, inhibition of topoisomerase I, and anticancer cytotoxicity in vitro. |
| AID691568 | Growth inhibition of human U251 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID691561 | Growth inhibition of human KM12 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID485538 | Inhibition of human recombinant topoisomerase 2 alpha-mediated Crithidia fasciculate kDNA decatenation at 20 uM relative to control | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11 | Design, synthesis and biological evaluation of a novel series of anthrapyrazoles linked with netropsin-like oligopyrrole carboxamides as anticancer agents. |
| AID691584 | Growth inhibition of human SKOV3 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID691563 | Growth inhibition of human SF268 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID691581 | Growth inhibition of human OVCAR5 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID156849 | Minimum inhibitory concentration required to reduce vaccinia virus induced cytopathogenicity by 50% in primary rabbit kidney cells (PRK) | 1989 | Journal of medicinal chemistry, May, Volume: 32, Issue:5 | Synthesis, DNA binding, and biological evaluation of synthetic precursors and novel analogues of netropsin. |
| AID649518 | Antimicrobial activity against Enterococcus faecalis NCTC 12697 after 24 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6 | Efficient synthesis and biological evaluation of proximicins A, B and C. |
| AID156843 | Minimum inhibitory concentration required to reduce herpes simplex virus-1 (KOS)induced cytopathogenicity by 50% in primary rabbit kidney cells (PRK) | 1989 | Journal of medicinal chemistry, May, Volume: 32, Issue:5 | Synthesis, DNA binding, and biological evaluation of synthetic precursors and novel analogues of netropsin. |
| AID691569 | Growth inhibition of human LOXIMVI cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID691551 | Growth inhibition of human EKVX cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID98695 | Inhibitory effect on the proliferation of murine leukemia (L1210 ) cells | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | Novel linked antiviral and antitumor agents related to netropsin and distamycin: synthesis and biological evaluation. |
| AID465966 | Binding affinity to calf thymus DNA assessed as decrease in ethidium bromide fluorescence by FID assay | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5 | Semi-automated high-throughput fluorescent intercalator displacement-based discovery of cytotoxic DNA binding agents from a large compound library. |
| AID1698746 | Displacement of EtBr from calf thymus DNA incubated for 3 mins by fluorescence based assay | 2020 | Journal of natural products, 10-23, Volume: 83, Issue:10 | Synthesis and Stereochemical Assignment of Conioidine A: DNA- and HSA-Binding Studies of the Four Diastereomers. |
| AID691560 | Growth inhibition of human HT-29 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID218405 | Minimum inhibitory concentration required to reduce reovirus-1 induced cytopathogenicity by 50% in african green monkey (VeroB)cells | 1989 | Journal of medicinal chemistry, May, Volume: 32, Issue:5 | Synthesis, DNA binding, and biological evaluation of synthetic precursors and novel analogues of netropsin. |
| AID31892 | Thermal denaturation in alternating poly(dA-dT)poly(dA-dT) homopolymer (AT) | 1993 | Journal of medicinal chemistry, Jun-11, Volume: 36, Issue:12 | Structure, DNA minor groove binding, and base pair specificity of alkyl- and aryl-linked bis(amidinobenzimidazoles) and bis(amidinoindoles). |
| AID691573 | Growth inhibition of human SK-MEL-2 cells after 48 hrs by cell counting analysis | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs. |
| AID156845 | Minimum inhibitory concentration required to reduce herpes simplex virus-2 (G)induced cytopathogenicity by 50% in primary rabbit kidney cells (PRK) | 1989 | Journal of medicinal chemistry, May, Volume: 32, Issue:5 | Synthesis, DNA binding, and biological evaluation of synthetic precursors and novel analogues of netropsin. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 152 (28.04) | 18.7374 |
| 1990's | 178 (32.84) | 18.2507 |
| 2000's | 121 (22.32) | 29.6817 |
| 2010's | 80 (14.76) | 24.3611 |
| 2020's | 11 (2.03) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (29.48) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 31 (5.19%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 566 (94.81%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||