bevirimat: an HIV inhibitor; disrupts late step in processing HIV Major Core Protein p24, preventing the capsid precursor p25 from being converted to mature capsid p24 [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
bevirimat : A pentacyclic triterpenoid obtained by the formal condensation of 2,2-dimethylsuccinic acid with the 3-hydroxy group of betulinic acid. It is isolated from the Chinese herb Syzygium claviflorum. The first in the class of HIV-1 maturation inhibitors to be studied in humans, bevirimat was identified as a potent HIV drug candidate and several clinical trials were conducted, but development into a new drug was plagued by numerous resistance-related problems. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]
| ID Source | ID |
|---|---|
| PubMed CID | 457928 |
| CHEMBL ID | 404519 |
| CHEBI ID | 65484 |
| SCHEMBL ID | 2612026 |
| MeSH ID | M0458059 |
| Synonym |
|---|
| 3-o-(3'',3''-dimethylsuccinyl)-betulinic acid |
| 3-o-(3'',3''-dimethylsuccinyl)betulinic acid |
| bdbm50050955 |
| 3-o-(3'',3''-dimethyl-succinyl)-betulinic acid |
| 2,2-dimethyl-succinic acid 4-((1r,3as,5ar,5br,7ar,9s,11ar,11br,13ar,13br)-3a-carboxy-1-isopropenyl-5a,5b,8,8,11a-pentamethyl-icosahydro-cyclopenta[a]chrysen-9-yl) ester |
| dbs, pa-457 |
| mpc-4326 |
| pa-457 |
| (1r,3as,5ar,5br,7ar,9s,11ar,11br,13ar,13br)-9-(4-hydroxy-3,3-dimethyl-4-oxo-butanoyl)oxy-1-isopropenyl-5a,5b,8,8,11a-pentamethyl-1,2,3,4,5,6,7,7a,9,10,11,11b,12,13,13a,13b-hexadecahydrocyclopenta[a]chrysene-3a-carboxylic acid |
| BVM , |
| 3-o-(3',3'-dimethylsuccinyl)-betulinic acid |
| bevirimat |
| 2,2-dimethyl-succinic acid, 4-((1r,3as,5ar,5br,7ar,9s,11ar,11br,13ar,13br)-3a-carboxy-1-isopropenyl-5a,5b,8,8,11a-pentamethyl-eicosahydro-cyclopenta[a]chrysen-9-yl) ester |
| yk-fh312 |
| DSB , |
| CHEMBL404519 , |
| chebi:65484 , |
| pa-103001 |
| yk fh312 |
| s125dw66n8 , |
| o-(3,3-dimethylsuccinyl)betulinic acid |
| pa 457 |
| bevirimat [inn] |
| unii-s125dw66n8 |
| 174022-42-5 |
| lup-20(29)-en-28-oic acid, 3-(3-carboxy-3-methyl-1-oxobutoxy)-, (3beta)- |
| 3-o-(3',3'-dimethylsuccinyl)betulinic acid |
| bevirimatum |
| 3-o-(3',3'-dimethylsuccinyl) betulinic acid |
| (3beta)-3-[(3-carboxy-3-methylbutanoyl)oxy]lup-20(29)-en-28-oic acid |
| S9010 |
| bevirimat [mi] |
| DB06581 |
| HY-N0842 |
| SCHEMBL2612026 |
| AC-34026 |
| DTXSID20169749 |
| AKOS030526656 |
| mfcd00954243 |
| bevirimat, >=98% (hplc) |
| bevirimat(pa-457) |
| (1r,3as,5ar,5br,7ar,9s,11ar,11br,13br)-9-(3-carboxy-3-methylbutanoyloxy)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1h-cyclopenta[a]chrysene-3a-carboxylic acid |
| (1r,3as,5ar,5br,7ar,9s,11ar,11br,13ar,13br)-9-((3-carboxy-3-methylbutanoyl)oxy)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-3ah-cyclopenta[a]chrysene-3a-carboxylic acid |
| EX-A2381 |
| bevirimat; pa-457; mpc-4326 |
| YJEJKUQEXFSVCJ-WRFMNRASSA-N |
| 3beta-(3-carboxy-3-methylbutanoyloxy)lup-20(29)-en-28-oic acid |
| Q851897 |
| ZB1856 |
| bevirimat-dimeglumine |
| CCG-270147 |
| MS-30468 |
| NCGC00390568-02 |
| ZGA02242 |
| 2I4 , |
| 3alpha-[(3-carboxy-3-methylbutanoyl)oxy]-8alpha,9beta,10alpha,13alpha,17alpha,19beta-lup-20(29)-en-28-oic acid |
Bevirimat is a novel HIV-1 maturation inhibitor with a mechanism of action that is distinct from other antiretroviral agents. It is a first in class, orally active, potent and selective inhibitor of HIV- 1.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Bevirimat (1, BVM) is an anti-HIV agent that blocks HIV-1 replication by interfering with HIV-1 Gag-SP1 processing at a late stage of viral maturation. " | ( New betulinic acid derivatives for bevirimat-resistant human immunodeficiency virus type-1. Chen, CH; Dang, Z; Ho, P; Huang, L; Lee, KH; Qian, K; Zhu, L, 2013) | 2.11 |
| "Bevirimat is a novel HIV-1 maturation inhibitor with a mechanism of action that is distinct from other antiretroviral agents." | ( Bevirimat: a novel maturation inhibitor for the treatment of HIV-1 infection. Allaway, GP; Martin, DE; Salzwedel, K, 2008) | 2.51 |
| "Bevirimat is a first in class, orally active, potent and selective inhibitor of HIV-1. " | ( An oral human drug absorption study to assess the impact of site of delivery on the bioavailability of bevirimat. Connor, A; Doto, J; Ellis, C; Evans, P; Martin, DE, 2009) | 2.01 |
Bevirimat has a novel mechanism of action, specifically inhibiting cleavage of spacer peptide 1 (SP1) from the C-terminus of capsid. peak plasma concentrations attained approximately 1-3 h after dosing.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Bevirimat has a novel mechanism of action, specifically inhibiting cleavage of spacer peptide 1 (SP1) from the C-terminus of capsid which results in defective core condensation." | ( Potent activity of the HIV-1 maturation inhibitor bevirimat in SCID-hu Thy/Liv mice. Allaway, GP; Bare, JC; Joshi, P; Martin, DE; Sloan, B; Smith, PC; Stoddart, CA; Wild, CT, 2007) | 1.31 |
| "Bevirimat has demonstrated a consistent pharmacokinetic profile in healthy volunteers and HIV-infected patients, with peak plasma concentrations attained approximately 1-3 h after dosing." | ( Bevirimat: a novel maturation inhibitor for the treatment of HIV-1 infection. Allaway, GP; Martin, DE; Salzwedel, K, 2008) | 2.51 |
| "Bevirimat has a novel mechanism of action, specifically inhibiting cleavage of spacer peptide 1 (SP1) from the C-terminus of capsid which results in defective core condensation." | ( Potent activity of the HIV-1 maturation inhibitor bevirimat in SCID-hu Thy/Liv mice. Allaway, GP; Bare, JC; Joshi, P; Martin, DE; Sloan, B; Smith, PC; Stoddart, CA; Wild, CT, 2007) | 1.31 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " Single oral doses of BVM were well tolerated: there were no dose-limiting toxicities, and no serious adverse events were reported." | ( Safety and pharmacokinetics of Bevirimat (PA-457), a novel inhibitor of human immunodeficiency virus maturation, in healthy volunteers. Ballow, C; Blum, R; Burgess, GL; Doto, J; Galbraith, H; Martin, DE; Smith, PC; Wilton, J, 2007) | 0.63 |
| " There was no increase in adverse events observed for bevirimat compared with placebo, and no serious adverse events occurred." | ( Multiple-dose pharmacokinetics and safety of bevirimat, a novel inhibitor of HIV maturation, in healthy volunteers. Ballow, C; Blum, R; Doto, J; Galbraith, H; Martin, DE, 2007) | 0.85 |
The mean terminal elimination half-life of bevirimat ranged from 56.5 days to 21 days after dosing started. Plasma be virimat levels were measured from blood samples collected pre-dose on days 1-10 and then at approximately 48-hour intervals until 21 days later.
| Excerpt | Reference | Relevance |
|---|---|---|
| " Since these agents will be used in combination with other new and existing antiretrovirals, understanding the potential for drug interactions between these compounds is critical to their appropriate use." | ( Drug interactions with new and investigational antiretrovirals. Brown, KC; Kashuba, AD; Paul, S, 2009) | 0.35 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " BVM was well absorbed after oral administration, with peak plasma concentrations being achieved 1 to 3 h after dosing." | ( Safety and pharmacokinetics of Bevirimat (PA-457), a novel inhibitor of human immunodeficiency virus maturation, in healthy volunteers. Ballow, C; Blum, R; Burgess, GL; Doto, J; Galbraith, H; Martin, DE; Smith, PC; Wilton, J, 2007) | 0.63 |
| " Oral bioavailability for the 25 mg/kg dose of bevirimat was estimated at 22-24% by pharmacokinetic and mass-balance methods, with bioavailability decreasing disproportionately with increasing dose for the 600 mg/kg group." | ( The absorption, distribution, metabolism and elimination of bevirimat in rats. Bullock, P; Larsen, D; Martin, DE; Press, R; Wehrman, T, 2008) | 0.85 |
| " In earlier studies in HIV-1-infected patients, an immediate-release tablet formulation exhibited a relative bioavailability (F(rel)) of 50% or greater and a higher intersubject variability than an oral solution." | ( An oral human drug absorption study to assess the impact of site of delivery on the bioavailability of bevirimat. Connor, A; Doto, J; Ellis, C; Evans, P; Martin, DE, 2009) | 0.57 |
Bevirimat shows dose-proportional pharmacokinetics during repeated dosing for 10 days. Testing for dose-Proportionality showed that exposure to bevirim at was proportional to the dose.
| Role | Description |
|---|---|
| metabolite | Any intermediate or product resulting from metabolism. The term 'metabolite' subsumes the classes commonly known as primary and secondary metabolites. |
| HIV-1 maturation inhibitor | A compound that blocks the processing of the Gag precursor protein in HIV-1 by the viral protease enzyme, leading to the formation of noninfectious, immature virus particles that are incapable of infecting other cells. |
| [role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Class | Description |
|---|---|
| pentacyclic triterpenoid | |
| dicarboxylic acid monoester | A monoester of a dicarboxylic acid. |
| monocarboxylic acid | An oxoacid containing a single carboxy group. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Gag-Pol polyprotein | HIV-1 M:B_HXB2R | IC50 (µMol) | 0.5520 | 0.0006 | 0.9141 | 8.3200 | AID1391862 |
| Protease | Human immunodeficiency virus 1 | IC50 (µMol) | 171.0000 | 0.0001 | 0.2248 | 7.3200 | AID198242 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Gag-Pol polyprotein | HIV-1 M:B_HXB2R | EC50 (µMol) | 0.4369 | 0.0100 | 0.4369 | 1.1200 | AID1391859; AID1391860; AID1391868; AID1391874; AID1391875 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| viral life cycle | Gag-Pol polyprotein | HIV-1 M:B_HXB2R |
| establishment of integrated proviral latency | Gag-Pol polyprotein | HIV-1 M:B_HXB2R |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| peptidase activity | Gag-Pol polyprotein | HIV-1 M:B_HXB2R |
| integrase activity | Gag-Pol polyprotein | HIV-1 M:B_HXB2R |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1745854 | NCATS anti-infectives library activity on HEK293 viability as a counter-qHTS vs the C. elegans viability qHTS | 2023 | Disease models & mechanisms, 03-01, Volume: 16, Issue:3 | In vivo quantitative high-throughput screening for drug discovery and comparative toxicology. |
| AID1745855 | NCATS anti-infectives library activity on the primary C. elegans qHTS viability assay | 2023 | Disease models & mechanisms, 03-01, Volume: 16, Issue:3 | In vivo quantitative high-throughput screening for drug discovery and comparative toxicology. |
| AID621549 | Antiviral activity against HIV1 | 2011 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19 | New betulinic acid derivatives as potent proteasome inhibitors. |
| AID728083 | Inhibition of wild type Human immunodeficiency virus 1 NL4-3 envelope glycoprotein gp160-mediated cell-cell fusion between virus-infected monkey COS cells to human TZM-bl cells after 24 hrs by luciferase reporter gene assay | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5 | New betulinic acid derivatives for bevirimat-resistant human immunodeficiency virus type-1. |
| AID369584 | Cmax in healthy human plasma after 25 mg oral dose, normalised for 70 kg subject | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | Safety and pharmacokinetics of Bevirimat (PA-457), a novel inhibitor of human immunodeficiency virus maturation, in healthy volunteers. |
| AID1672254 | AUC in rat for 6 hrs | 2019 | ACS medicinal chemistry letters, Mar-14, Volume: 10, Issue:3 | Second Generation Inhibitors of HIV-1 Maturation. |
| AID1391861 | Ratio of EC50 for binding affinity to CA-SP1 P373S mutant in HIV-1 subtype B NL4-3 infected in human MT2 cells in presence of 15 mg/ml HSA to EC50 for binding affinity to CA-SP1 P373S mutant in HIV-1 subtype B NL4-3 infected in human MT2 cells in absence | 2018 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9 | The design, synthesis and structure-activity relationships associated with C28 amine-based betulinic acid derivatives as inhibitors of HIV-1 maturation. |
| AID736134 | Inhibition of HIV1 NL4.3 CA-SP1 cleavage infected in 293T cells after 2 days by Western blot analysis | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Synthesis and biological evaluation of a new derivative of bevirimat that targets the Gag CA-SP1 cleavage site. |
| AID1672249 | Binding affinity to HIV-1 CA-SP1 cleavage site of Gag-Pol protein harboring V370A mutant assessed as inhibition of HIV-1 maturation | 2019 | ACS medicinal chemistry letters, Mar-14, Volume: 10, Issue:3 | Second Generation Inhibitors of HIV-1 Maturation. |
| AID369767 | Toxicity in healthy human assessed as adverse event occurrence at 100 mg, po administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | Safety and pharmacokinetics of Bevirimat (PA-457), a novel inhibitor of human immunodeficiency virus maturation, in healthy volunteers. |
| AID350984 | Apparent oral clearance in HIV1 infected human at 150 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID1708701 | Cmax in rat at 5 mg/kg, po measured after 24 hrs | 2021 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 36 | Design and exploration of C-3 benzoic acid bioisosteres and alkyl replacements in the context of GSK3532795 (BMS-955176) that exhibit broad spectrum HIV-1 maturation inhibition. |
| AID271056 | Therapeutic index, IC50 for H9/EC50 for HIV1 NL4-3 | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Anti-AIDS agents 69. Moronic acid and other triterpene derivatives as novel potent anti-HIV agents. |
| AID369604 | Dose normalized AUC (0 to infinity) in healthy human plasma at 250 mg, po administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | Safety and pharmacokinetics of Bevirimat (PA-457), a novel inhibitor of human immunodeficiency virus maturation, in healthy volunteers. |
| AID78783 | Toxic concentration on HIV-1 mock infected H9 lymphocyte cells | 1996 | Journal of medicinal chemistry, Mar-01, Volume: 39, Issue:5 | Betulinic acid and dihydrobetulinic acid derivatives as potent anti-HIV agents. |
| AID1391875 | Binding affinity to CA-SP1 P373S/V362I double mutant in HIV-1 subtype B NL4-3 infected in human MT2 cells assessed as inhibition of viral maturation by measuring virus yield after 4 to 5 days in presence of 10% FBS by luciferase reporter gene assay | 2018 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9 | The design, synthesis and structure-activity relationships associated with C28 amine-based betulinic acid derivatives as inhibitors of HIV-1 maturation. |
| AID1708696 | Metabolic stability in rat liver microsomes assessed as half life | 2021 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 36 | Design and exploration of C-3 benzoic acid bioisosteres and alkyl replacements in the context of GSK3532795 (BMS-955176) that exhibit broad spectrum HIV-1 maturation inhibition. |
| AID369587 | Half life in healthy human plasma at 25 mg, po administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | Safety and pharmacokinetics of Bevirimat (PA-457), a novel inhibitor of human immunodeficiency virus maturation, in healthy volunteers. |
| AID555843 | Antiviral activity against HIV1 PA100 harboring SP1 mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID246296 | Concentration required to inhibit 50% of HIV-1 (human immunodeficiency virus-1) replication | 2004 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 14, Issue:23 | 3-O-Glutaryl-dihydrobetulin and related monoacyl derivatives as potent anti-HIV agents. |
| AID532264 | Antiviral activity against Human immunodeficiency virus 1 isolate 35 harboring Gag-capsid G357S mutant gene and Gag-SP1 V370A, T371Q, N372S, T375N and I376M mutant gene infected in human MT-2 cells by XTT assay relative to wild-type | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID621520 | Inhibition of human 20S proteasome chymotrypsin-like activity using Suc-Leu-Leu-Val-Tyr-AMC fluorogenic substrate by fluorimetry | 2011 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19 | New betulinic acid derivatives as potent proteasome inhibitors. |
| AID728089 | Antiviral activity against 0.001 MOI bevirimat-resistant Human immunodeficiency virus 1 NL4-3 harboring gag V370 deletion mutant infected in human MT4 cells assessed as inhibition of viral replication measured 4 days post infection by ELISA | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5 | New betulinic acid derivatives for bevirimat-resistant human immunodeficiency virus type-1. |
| AID81587 | Inhibitory activity against HIV-1-induced syncytia determined by fusion assay | 1996 | Journal of medicinal chemistry, Mar-01, Volume: 39, Issue:5 | Betulinic acid and dihydrobetulinic acid derivatives as potent anti-HIV agents. |
| AID736136 | Selectivity index, ratio of CC50 for human MAGIC-5B cells to IC50 for HIV1 NL4.3 | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Synthesis and biological evaluation of a new derivative of bevirimat that targets the Gag CA-SP1 cleavage site. |
| AID555840 | Antiviral activity against HIV1 NL4.3 harboring SP1 A1V mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID555863 | Antiviral activity against HIV1 HXB2 harboring SP1 mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID1313369 | Binding affinity to gag polyprotein Q369H mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6 | Discovery of BMS-955176, a Second Generation HIV-1 Maturation Inhibitor with Broad Spectrum Antiviral Activity. |
| AID1471103 | Inhibition of bevirimat-resistant HIV-1 clade B isolate CC1/85 CA-SP1 V370A mutant infected in human PBMC measured after 7 days by scintillation counting method | 2017 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12 | Discovery of a novel and potent class of anti-HIV-1 maturation inhibitors with improved virology profile against gag polymorphisms. |
| AID369599 | Cmax in heathy human plasma after 100 mg oral dose, normalised for 70 kg subject | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | Safety and pharmacokinetics of Bevirimat (PA-457), a novel inhibitor of human immunodeficiency virus maturation, in healthy volunteers. |
| AID1228703 | Cytotoxicity against mock-infected human MT2 cells assessed as reduction in cell viability incubated for 48 hrs by cell-titer Glo assay | 2015 | Journal of natural products, May-22, Volume: 78, Issue:5 | Isolation, Structural Modification, and HIV Inhibition of Pentacyclic Lupane-Type Triterpenoids from Cassine xylocarpa and Maytenus cuzcoina. |
| AID1391914 | Half life in human liver microsomes at 0.5 uM in presence of NADPH by LC-MS/MS method | 2018 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9 | The design, synthesis and structure-activity relationships associated with C28 amine-based betulinic acid derivatives as inhibitors of HIV-1 maturation. |
| AID532674 | Antiviral activity against antiretroviral-pretreated Human immunodeficiency virus 1 isolate 22 infected in human MT-2 cells by XTT assay relative to wild-type | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID1520505 | Antiviral activity against HIV1 NL4-3 infected in human MT4 cells by luciferase reporter gene assay | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Discovery and synthesis of novel beesioside I derivatives with potent anti-HIV activity. |
| AID532266 | Antiviral activity against antiretroviral-pretreated PI-resistant Human immunodeficiency virus 1 isolate 23 harboring Gag-capsid G357S and V362I mutant gene, Gag-SP-1 V370A and T375A mutant gene and deletion at T371 in Gag-SP-1 infected in human MT-2 cell | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID1708698 | AUC (0 to 24) in rat at 5 mg/kg, po measured after 24 hrs | 2021 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 36 | Design and exploration of C-3 benzoic acid bioisosteres and alkyl replacements in the context of GSK3532795 (BMS-955176) that exhibit broad spectrum HIV-1 maturation inhibition. |
| AID1708703 | Volume of distribution at steady state in rat at 1 mg/kg, iv | 2021 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 36 | Design and exploration of C-3 benzoic acid bioisosteres and alkyl replacements in the context of GSK3532795 (BMS-955176) that exhibit broad spectrum HIV-1 maturation inhibition. |
| AID555831 | Antiviral activity against HIV1 NL4.3 harboring SP1 T8delta mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID532256 | Antiviral activity against antiretroviral-pretreated PI-resistant Human immunodeficiency virus 1 isolate 27 harboring Gag-SP-1 S373P mutant gene deletion at T371 in Gag-SP-1 infected in human MT-2 cells by XTT assay relative to wild-type | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID369589 | AUC (0 to infinity) in healthy human plasma at 50 mg, po administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | Safety and pharmacokinetics of Bevirimat (PA-457), a novel inhibitor of human immunodeficiency virus maturation, in healthy volunteers. |
| AID532673 | Antiviral activity against Human immunodeficiency virus 1 LAI infected in human MT-2 cells by XTT-assay | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID1708700 | Tmax in rat at 5 mg/kg, po measured after 24 hrs | 2021 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 36 | Design and exploration of C-3 benzoic acid bioisosteres and alkyl replacements in the context of GSK3532795 (BMS-955176) that exhibit broad spectrum HIV-1 maturation inhibition. |
| AID351000 | Antiviral activity against HIV1 infected in human assessed as rate at which virus infects CD4 cells at 250 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID351006 | Antiviral activity against HIV1 infected in human assessed as clearance rate of virions at 250 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID350992 | Half life in HIV1 infected human at 75 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID555845 | Antiviral activity against HIV1 PA105 harboring SP1 mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID556036 | Antiviral activity against HIV1 HXB2 harboring SP1 Q6H /V7A/T8delta mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID555841 | Antiviral activity against HIV1 NL4.3 harboring SP1 L231M mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID492518 | Cytotoxicity against human H9 cells after 4 days by coulter counter | 2010 | Journal of natural products, Mar-26, Volume: 73, Issue:3 | Discovery and development of natural product-derived chemotherapeutic agents based on a medicinal chemistry approach. |
| AID369606 | Cmax in healthy human plasma after 250 mg oral dose, normalised for 70 kg subject | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | Safety and pharmacokinetics of Bevirimat (PA-457), a novel inhibitor of human immunodeficiency virus maturation, in healthy volunteers. |
| AID1313362 | Cytotoxicity against human MT2 cells | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6 | Discovery of BMS-955176, a Second Generation HIV-1 Maturation Inhibitor with Broad Spectrum Antiviral Activity. |
| AID1313390 | Antiviral activity against HIV1 infected in patient assessed as viral load reduction at 150 to 250 mg administered po qd for 10 days measured on day 11 | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6 | Discovery of BMS-955176, a Second Generation HIV-1 Maturation Inhibitor with Broad Spectrum Antiviral Activity. |
| AID532258 | Antiviral activity against antiretroviral-pretreated PI-resistant Human immunodeficiency virus 1 isolate 3 harboring Gag-capsid G357S mutant gene, Gag-Sp-1 V370A and N372H mutant gene and deletion at T371 in Gag-SP-1 infected in human MT-2 cells by XTT as | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID473141 | Cytotoxicity against human MT2 cells by XTT assay | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Anti-AIDS agents 81. Design, synthesis, and structure-activity relationship study of betulinic acid and moronic acid derivatives as potent HIV maturation inhibitors. |
| AID532243 | Antiviral activity against Human immunodeficiency virus 1 isolate 32 harboring Gag-SP1 V370I and N372G mutant gene infected in human MT-2 cells by XTT assay relative to wild-type | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID271055 | Antiviral activity against HIV1 NL4-3 in MT4 cells | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Anti-AIDS agents 69. Moronic acid and other triterpene derivatives as novel potent anti-HIV agents. |
| AID728092 | Antiviral activity against 0.001 MOI wild type Human immunodeficiency virus 1 NL4-3 infected in human MT4 cells assessed as inhibition of viral replication measured 4 days post infection by ELISA | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5 | New betulinic acid derivatives for bevirimat-resistant human immunodeficiency virus type-1. |
| AID1285297 | Ratio of EC50 for HIV1 NLRepRlucP373S infected in human MT2 cells in presence of HSA to EC50 for HIV1 NLRepRlucP373S infected in human MT2 cells in absence of HSA | 2016 | Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8 | C-3 benzoic acid derivatives of C-3 deoxybetulinic acid and deoxybetulin as HIV-1 maturation inhibitors. |
| AID1391862 | Binding affinity to CA-SP1 P373S/V370A double mutant in HIV-1 subtype B NL4-3 infected in human MT2 cells assessed as inhibition of viral maturation by measuring virus yield after 4 to 5 days in presence of 10% FBS by luciferase reporter gene assay | 2018 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9 | The design, synthesis and structure-activity relationships associated with C28 amine-based betulinic acid derivatives as inhibitors of HIV-1 maturation. |
| AID350157 | Cytotoxicity against human MT2 cells by XTT assay | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10 | Anti-AIDS agents. 78. Design, synthesis, metabolic stability assessment, and antiviral evaluation of novel betulinic acid derivatives as potent anti-human immunodeficiency virus (HIV) agents. |
| AID1291863 | Antiviral activity against wild type HIV1 NL4-3 habouring Gag protein V370A mutant infected in human MT2 cells after 4 to 5 days by dual-luciferase reporter gene assay | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Inhibitors of HIV-1 maturation: Development of structure-activity relationship for C-28 amides based on C-3 benzoic acid-modified triterpenoids. |
| AID351176 | Antiviral activity against HIV1 infected in human assessed as inhibition of viral replication at 150 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID1313371 | Binding affinity to gag polyprotein V370A/T371 deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6 | Discovery of BMS-955176, a Second Generation HIV-1 Maturation Inhibitor with Broad Spectrum Antiviral Activity. |
| AID532447 | Antiviral activity against antiretroviral-pretreated Human immunodeficiency virus 1 isolate 12 harboring Gag-capsid G357S and V362I mutant gene infected in human MT-2 cells by XTT assay relative to wild-type | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID562702 | Antiviral activity against HIV1 harboring capsid I201V mutant protein infected in human HeLa cells assessed as decrease in viral infection after 72 hrs by beta-galactosidase reporter gene assay | 2009 | Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12 | New small-molecule inhibitor class targeting human immunodeficiency virus type 1 virion maturation. |
| AID1520507 | Therapeutic index, ratio of CC50 for human MT4 cells to EC50 for HIV1 NL4-3 infected in human MT4 cells | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Discovery and synthesis of novel beesioside I derivatives with potent anti-HIV activity. |
| AID583853 | Antiviral activity against HIV1 NL4-3 infected in human MT2 cells assessed as inhibition of virus-induced cell death at 0.05 multiplicities of infection after 6 days | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10 | Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. |
| AID1672279 | Binding affinity to HIV-1 CA-SP1 cleavage site of Gag-Pol protein harboring V370M mutant assessed as inhibition of HIV-1 maturation | 2019 | ACS medicinal chemistry letters, Mar-14, Volume: 10, Issue:3 | Second Generation Inhibitors of HIV-1 Maturation. |
| AID350158 | Therapeutic index, ratio of CC50 for human MT2 cells to EC50 for HIV1 3B | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10 | Anti-AIDS agents. 78. Design, synthesis, metabolic stability assessment, and antiviral evaluation of novel betulinic acid derivatives as potent anti-human immunodeficiency virus (HIV) agents. |
| AID562701 | Antiviral activity against wild type HIV1 infected in human HeLa cells assessed as decrease in viral infection after 72 hrs by beta-galactosidase reporter gene assay | 2009 | Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12 | New small-molecule inhibitor class targeting human immunodeficiency virus type 1 virion maturation. |
| AID1285305 | AUC(0 to 6 hrs) in rat at 5 mg/kg, po by LC-MS/MS | 2016 | Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8 | C-3 benzoic acid derivatives of C-3 deoxybetulinic acid and deoxybetulin as HIV-1 maturation inhibitors. |
| AID1313372 | Binding affinity to gag polyprotein V371A deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6 | Discovery of BMS-955176, a Second Generation HIV-1 Maturation Inhibitor with Broad Spectrum Antiviral Activity. |
| AID1471113 | Inhibition of HIV1 Gag CA-SP1 cleavage infected in human PBMC at 10 uM measured after 8 days post infection by Western blot analysis | 2017 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12 | Discovery of a novel and potent class of anti-HIV-1 maturation inhibitors with improved virology profile against gag polymorphisms. |
| AID350982 | Distributional clearance in HIV1 infected human at 250 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID371950 | Cytotoxicity against human Raji cells assessed as cell viability at 500 molar ratio after 48 hrs by trypan blue staining method | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13 | Cancer preventive agents 9. Betulinic acid derivatives as potent cancer chemopreventive agents. |
| AID378286 | Antiviral activity against HIV1 3B isolate replication in human H9 cells assessed as decrease in viral p24 level after 4 days | 2000 | Journal of natural products, Dec, Volume: 63, Issue:12 | Anti-AIDS agents 38. Anti-HIV activity of 3-O-acyl ursolic acid derivatives. |
| AID271057 | Cytotoxicity against human MT4 cells at 5 uM | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Anti-AIDS agents 69. Moronic acid and other triterpene derivatives as novel potent anti-HIV agents. |
| AID555855 | Antiviral activity against HIV1 PA102 harboring SP1 mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID369607 | Tmax in healthy human plasma at 250 mg, po administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | Safety and pharmacokinetics of Bevirimat (PA-457), a novel inhibitor of human immunodeficiency virus maturation, in healthy volunteers. |
| AID673428 | Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells assessed as reduction of viral p24 level cells by fluorescence assay relative to wild type HIV1 NL4-3 after 4 days by ELISA | 2012 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 22, Issue:16 | Synthesis of betulinic acid derivatives as entry inhibitors against HIV-1 and bevirimat-resistant HIV-1 variants. |
| AID350987 | Tlag in HIV1 infected human at 150 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID1471098 | Inhibition of wild type HIV-1 clade B NL4-3 Gag polyprotein SP1 infected in human MT4 cells | 2017 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12 | Discovery of a novel and potent class of anti-HIV-1 maturation inhibitors with improved virology profile against gag polymorphisms. |
| AID369603 | AUC (0 to infinity) in healthy human plasma at 250 mg, po administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | Safety and pharmacokinetics of Bevirimat (PA-457), a novel inhibitor of human immunodeficiency virus maturation, in healthy volunteers. |
| AID555828 | Antiviral activity against HIV1 HXB2 harboring SP1 T8N mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID1391865 | AUC (0 to 6 hrs) in Sprague-Dawley rat at 5 mg/kg, po via gavage by LC-MS/MS analysis | 2018 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9 | The design, synthesis and structure-activity relationships associated with C28 amine-based betulinic acid derivatives as inhibitors of HIV-1 maturation. |
| AID351179 | Antiviral activity against HIV1 infected in human assessed as maximum rate of viral replication measured as logarithmic viral copies at 150 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID1706910 | Protein binding in human serum albumin | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Triterpenoid-Mediated Inhibition of Virus-Host Interaction: Is Now the Time for Discovering Viral Entry/Release Inhibitors from Nature? |
| AID1265942 | Antiviral activity against HIV-1 NL4-3 infected in MT4 cells assessed inhibition of viral replication measured on day 4 postinfection by ELISA | 2016 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 26, Issue:1 | Fluorinated betulinic acid derivatives and evaluation of their anti-HIV activity. |
| AID350993 | Half life in HIV1 infected human at 150 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID501755 | Cytotoxicity against human MT4 cells after 4 days | 2010 | Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17 | Conjugates of betulin derivatives with AZT as potent anti-HIV agents. |
| AID369611 | Drug concentration in healthy human urine assessed as conjugated drug level at 250 mg, po administered as single dose after 48 hrs | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | Safety and pharmacokinetics of Bevirimat (PA-457), a novel inhibitor of human immunodeficiency virus maturation, in healthy volunteers. |
| AID369586 | Tmax in healthy human plasma at 25 mg, po administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | Safety and pharmacokinetics of Bevirimat (PA-457), a novel inhibitor of human immunodeficiency virus maturation, in healthy volunteers. |
| AID555838 | Antiviral activity against HIV1 NL4.3 harboring SP1 Q6A mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID371944 | Inhibition of TPA-induced EBV-early antigen activation in human Raji cells assessed as EA induction at 1000 molar ratio after 48 hrs relative to TPA | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13 | Cancer preventive agents 9. Betulinic acid derivatives as potent cancer chemopreventive agents. |
| AID1291871 | Total AUC in cannula implanted rat at 5 mg/kg administered through oral gavage after 24 hrs by LC-MS/MS analysis | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Inhibitors of HIV-1 maturation: Development of structure-activity relationship for C-28 amides based on C-3 benzoic acid-modified triterpenoids. |
| AID351002 | Antiviral activity against HIV1 infected in human assessed as death rate constant of infected CD4 cells at 150 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID350976 | Antiviral activity against HIV1 infected in human assessed as logarithmic reduction in HIV RNA copies at 250 mg, po relative to baseline | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID532249 | Antiviral activity against Human immunodeficiency virus 1 isolate 36 harboring Gag-SP1 Q371T, A374N and T375A mutant gene infected in human MT-2 cells by XTT assay relative to wild-type | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID532667 | Antiviral activity against Human immunodeficiency virus 1 isolate 7 harboring Gap-SP-1 V362I mutant infected in human MT-2 cells by XTT-assay relative to wild-type | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID532451 | Antiviral activity against antiretroviral-pretreated PI-resistant Human immunodeficiency virus 1 isolate 29 harboring Gag-SP-1 T375A mutant gene infected in human MT-2 cells by XTT assay relative to wild-type | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID79309 | Anti-HIV activity against acutely infected H9 lymphocytes. Activity expressed as concentration of compound toxic to 50% of mock-infected H9 cells. | 1998 | Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23 | Anti-AIDS agents. 34. Synthesis and structure-activity relationships of betulin derivatives as anti-HIV agents. |
| AID1672250 | Aqueous solubility of the compound | 2019 | ACS medicinal chemistry letters, Mar-14, Volume: 10, Issue:3 | Second Generation Inhibitors of HIV-1 Maturation. |
| AID371947 | Inhibition of TPA-induced EBV-early antigen activation in human Raji cells assessed as EA induction at 10 molar ratio after 48 hrs relative to TPA | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13 | Cancer preventive agents 9. Betulinic acid derivatives as potent cancer chemopreventive agents. |
| AID1285304 | Oral bioavailability in rat at 5 mg/kg by LC-MS/MS | 2016 | Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8 | C-3 benzoic acid derivatives of C-3 deoxybetulinic acid and deoxybetulin as HIV-1 maturation inhibitors. |
| AID549500 | Antiviral activity against Human immunodeficiency virus 1 NL4-3 infected in MT4 lymphocytes assessed as p24 antigen level by ELISA | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1 | Efficient synthesis and biological evaluation of epiceanothic acid and related compounds. |
| AID351008 | Antiviral activity against HIV1 infected in human assessed as number of new virions produced by infected CD4 cell at 150 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID1706911 | Aqueous solubility of compound | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Triterpenoid-Mediated Inhibition of Virus-Host Interaction: Is Now the Time for Discovering Viral Entry/Release Inhibitors from Nature? |
| AID1285311 | Protein binding of the compound in plasma (unknown origin) | 2016 | Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8 | C-3 benzoic acid derivatives of C-3 deoxybetulinic acid and deoxybetulin as HIV-1 maturation inhibitors. |
| AID1327729 | Antiviral activity against bevirimat-resistant HIV1 NL4-3 harboring GagV370A mutant infected in human MT4 cells by p24 ELISA | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19 | Incorporation of Privileged Structures into Bevirimat Can Improve Activity against Wild-Type and Bevirimat-Resistant HIV-1. |
| AID271062 | Cytotoxicity against COS-TZM fused cells | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Anti-AIDS agents 69. Moronic acid and other triterpene derivatives as novel potent anti-HIV agents. |
| AID532263 | Antiviral activity against Human immunodeficiency virus 1 isolate 34 harboring Gag-capsid G357S mutant gene and Gag-SP1 V370A, N372T, S373P and T375A mutant gene infected in human MT-2 cells by XTT assay relative to wild-type | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID1285296 | Antiviral activity against wild type HIV1 NLRepRlucP373S infected in human MT2 cells after 4 to 5 days in presence of 15 mg/ml HSA by luciferase report gene based multiple cycle drug susceptibility assay | 2016 | Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8 | C-3 benzoic acid derivatives of C-3 deoxybetulinic acid and deoxybetulin as HIV-1 maturation inhibitors. |
| AID549502 | Therapeutic index, ratio of IC50 for human lymphocytes to EC50 for Human immunodeficiency virus 1 NL4-3 | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1 | Efficient synthesis and biological evaluation of epiceanothic acid and related compounds. |
| AID1291865 | Antiviral activity against wild type BVM-resistant HIV1 NL4-3 habouring Gag protein V370M mutant infected in human MT2 cells after 4 to 5 days by dual-luciferase reporter gene assay | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Inhibitors of HIV-1 maturation: Development of structure-activity relationship for C-28 amides based on C-3 benzoic acid-modified triterpenoids. |
| AID1708695 | Metabolic stability in human liver microsomes assessed as half life | 2021 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 36 | Design and exploration of C-3 benzoic acid bioisosteres and alkyl replacements in the context of GSK3532795 (BMS-955176) that exhibit broad spectrum HIV-1 maturation inhibition. |
| AID1672277 | Binding affinity to HIV-1 CA-SP1 cleavage site of Gag-Pol protein harboring V362I mutant assessed as inhibition of HIV-1 maturation | 2019 | ACS medicinal chemistry letters, Mar-14, Volume: 10, Issue:3 | Second Generation Inhibitors of HIV-1 Maturation. |
| AID555832 | Antiviral activity against HIV1 NL4.3 harboring SP1 V7M mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID1313360 | Binding affinity to gag polyprotein V370A mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6 | Discovery of BMS-955176, a Second Generation HIV-1 Maturation Inhibitor with Broad Spectrum Antiviral Activity. |
| AID369590 | Dose normalized AUC (0 to infinity) in healthy human plasma at 50 mg, po administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | Safety and pharmacokinetics of Bevirimat (PA-457), a novel inhibitor of human immunodeficiency virus maturation, in healthy volunteers. |
| AID1391874 | Binding affinity to CA-SP1 P373S/T371A double mutant in HIV-1 subtype B NL4-3 infected in human MT2 cells assessed as inhibition of viral maturation by measuring virus yield after 4 to 5 days in presence of 10% FBS by luciferase reporter gene assay | 2018 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9 | The design, synthesis and structure-activity relationships associated with C28 amine-based betulinic acid derivatives as inhibitors of HIV-1 maturation. |
| AID1672255 | Cmax in rat at 5 mg/kg, po or 1 mg/kg, iv | 2019 | ACS medicinal chemistry letters, Mar-14, Volume: 10, Issue:3 | Second Generation Inhibitors of HIV-1 Maturation. |
| AID532251 | Antiviral activity against antiretroviral-pretreated PI-resistant Human immunodeficiency virus 1 isolate 5 harboring Gag-SP1 Q369H and T375N mutant gene infected in human MT-2 cells by XTT assay relative to wild-type | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID1285308 | Clearance in cannula implanted rat at 1 mg/kg, iv by LC-MS/MS | 2016 | Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8 | C-3 benzoic acid derivatives of C-3 deoxybetulinic acid and deoxybetulin as HIV-1 maturation inhibitors. |
| AID555847 | Antiviral activity against HIV1 PA111 harboring SP1 mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID351001 | Antiviral activity against HIV1 infected in human assessed as death rate constant of infected CD4 cells at 75 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID399882 | Antiviral activity against HIV | 2004 | Journal of natural products, Feb, Volume: 67, Issue:2 | Current developments in the discovery and design of new drug candidates from plant natural product leads. |
| AID1327733 | Inhibition of wild type HIV1 NL4-3 Env-mediated cell-cell fusion between viral envelope expressing virus-infected African green monkey COS cells to human TZM-bl cells incubated overnight by luciferase reporter gene assay | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19 | Incorporation of Privileged Structures into Bevirimat Can Improve Activity against Wild-Type and Bevirimat-Resistant HIV-1. |
| AID532262 | Antiviral activity against Human immunodeficiency virus 1 isolate 33 harboring Gag-SP1 S368G, V370M and S373T mutant gene infected in human MT-2 cells by XTT assay relative to wild-type | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID532252 | Antiviral activity against Human immunodeficiency virus 1 isolate 37 harboring Gag-capsid G357S mutant gene and Gag-SP1 I376V mutant gene infected in human MT-2 cells by XTT assay relative to wild-type | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID369608 | Half life in healthy human plasma at 250 mg, po administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | Safety and pharmacokinetics of Bevirimat (PA-457), a novel inhibitor of human immunodeficiency virus maturation, in healthy volunteers. |
| AID532672 | Antiviral activity against Human immunodeficiency virus 1 isolates harboring Gag-SP-1 V370A mutant gene relative to wild-type | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID371946 | Inhibition of TPA-induced EBV-early antigen activation in human Raji cells assessed as EA induction at 100 molar ratio after 48 hrs relative to TPA | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13 | Cancer preventive agents 9. Betulinic acid derivatives as potent cancer chemopreventive agents. |
| AID1291864 | Antiviral activity against wild type HIV1 NL4-3 habouring Gag protein delta V370 infected in human MT2 cells after 4 to 5 days by dual-luciferase reporter gene assay | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Inhibitors of HIV-1 maturation: Development of structure-activity relationship for C-28 amides based on C-3 benzoic acid-modified triterpenoids. |
| AID532259 | Antiviral activity against antiretroviral-pretreated PI-resistant Human immunodeficiency virus 1 isolate 6 harboring Gag-SP-1 V370A,S373A and A374T mutant gene infected in human MT-2 cells by XTT assay relative to wild-type | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID248082 | Concentration required to produce 50% toxicity against mock-infected H9 cells | 2004 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 14, Issue:23 | 3-O-Glutaryl-dihydrobetulin and related monoacyl derivatives as potent anti-HIV agents. |
| AID1672281 | Binding affinity to HIV-1 CA-SP1 cleavage site of Gag-Pol protein harboring Thr371Ala mutant assessed as inhibition of HIV-1 maturation | 2019 | ACS medicinal chemistry letters, Mar-14, Volume: 10, Issue:3 | Second Generation Inhibitors of HIV-1 Maturation. |
| AID549501 | Cytotoxicity against human MT4 lymphocytes after 48 hrs by MTT assay | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1 | Efficient synthesis and biological evaluation of epiceanothic acid and related compounds. |
| AID621522 | Inhibition of human 20S proteasome caspase-like activity using (Z)-LLE-bNA fluorogenic substrate by fluorimetry | 2011 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19 | New betulinic acid derivatives as potent proteasome inhibitors. |
| AID1291860 | Bioavailability in cannula implanted rat at 5 mg/kg administered through oral gavage after 24 hrs by LC-MS/MS analysis | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Inhibitors of HIV-1 maturation: Development of structure-activity relationship for C-28 amides based on C-3 benzoic acid-modified triterpenoids. |
| AID555865 | Antiviral activity against HIV1 HXB2 harboring SP1 Q6H/V7A mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID532448 | Antiviral activity against Human immunodeficiency virus 1 isolate 39 harboring Gag-capsid G357S and V362I mutant gene and Gag-SP-1 T375A mutant gene infected in human MT-2 cells by XTT assay relative to wild-type | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID351180 | Antiviral activity against HIV1 infected in human assessed as maximum rate of viral replication measured as logarithmic viral copies at 250 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID1672256 | Clearance in rat at 5 mg/kg, po or 1 mg/kg, iv | 2019 | ACS medicinal chemistry letters, Mar-14, Volume: 10, Issue:3 | Second Generation Inhibitors of HIV-1 Maturation. |
| AID1708689 | Antiviral activity against wild type HIV-1 NL4-3 harbouring Gag V370A mutant infected in MT-2 cells assessed as inhibition of viral replication in presence of 10% of fetal bovine serum by luciferase reporter gene based multicycle replication assay | 2021 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 36 | Design and exploration of C-3 benzoic acid bioisosteres and alkyl replacements in the context of GSK3532795 (BMS-955176) that exhibit broad spectrum HIV-1 maturation inhibition. |
| AID369588 | Apparent oral clearance in healthy human plasma at 25 mg, po administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | Safety and pharmacokinetics of Bevirimat (PA-457), a novel inhibitor of human immunodeficiency virus maturation, in healthy volunteers. |
| AID728085 | Antiviral activity against bevirimat-resistant Human immunodeficiency virus 1 NL4-3 harboring gag V370A mutant infected in human 293T cells assessed as inhibition of CA-SP1 cleavage measured 2 days post infection by Western blotting analysis | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5 | New betulinic acid derivatives for bevirimat-resistant human immunodeficiency virus type-1. |
| AID350997 | Antiviral activity against HIV1 infected in human assessed as death rate constant of uninfected CD4 cells at 250 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID1726076 | Antiviral activity against HIV 1 NL4-3 infected in human MT4 cells assessed as reduction in viral replication and measured on day 3 post infection by Nano-glo luciferase reporter assay | 2020 | ACS medicinal chemistry letters, Nov-12, Volume: 11, Issue:11 | Novel Betulinic Acid-Nucleoside Hybrids with Potent Anti-HIV Activity. |
| AID1672253 | Binding affinity to HIV-1 CA-SP1 cleavage site of Gag-pol protein harboring deltaV370 mutant assessed as inhibition of HIV-1 maturation | 2019 | ACS medicinal chemistry letters, Mar-14, Volume: 10, Issue:3 | Second Generation Inhibitors of HIV-1 Maturation. |
| AID673431 | Antiviral activity against bevirimat-resistant HIV1 NL4-3 harboring QVT motif of Gag SP1 deltaV370 mutant infected in human MT4 cells assessed as reduction of viral p24 level cells by fluorescence assay relative to wild type HIV1 NL4-3 after 4 days by ELI | 2012 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 22, Issue:16 | Synthesis of betulinic acid derivatives as entry inhibitors against HIV-1 and bevirimat-resistant HIV-1 variants. |
| AID728088 | Antiviral activity against 0.001 MOI bevirimat-resistant Human immunodeficiency virus 1 NL4-3 harboring gag T371 deletion mutant infected in human MT4 cells assessed as inhibition of viral replication measured 4 days post infection by ELISA | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5 | New betulinic acid derivatives for bevirimat-resistant human immunodeficiency virus type-1. |
| AID1285298 | Antiviral activity against HIV1 containing gag V370A mutant infected in human MT2 cells after 4 to 5 days by luciferase report gene based multiple cycle drug susceptibility assay | 2016 | Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8 | C-3 benzoic acid derivatives of C-3 deoxybetulinic acid and deoxybetulin as HIV-1 maturation inhibitors. |
| AID1391869 | Ratio of EC50 for binding affinity to CA-SP1 P373S mutant in HIV-1 subtype B NL4-3 infected in human MT2 cells in presence of 40% human serum to EC50 for binding affinity to CA-SP1 P373S mutant in HIV-1 subtype B NL4-3 infected in human MT2 cells in absen | 2018 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9 | The design, synthesis and structure-activity relationships associated with C28 amine-based betulinic acid derivatives as inhibitors of HIV-1 maturation. |
| AID728087 | Antiviral activity against 0.001 MOI bevirimat-resistant Human immunodeficiency virus 1 NL4-3 harboring gag V362I mutant infected in human MT4 cells assessed as inhibition of viral replication measured 4 days post infection by ELISA | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5 | New betulinic acid derivatives for bevirimat-resistant human immunodeficiency virus type-1. |
| AID350985 | Apparent oral clearance in HIV1 infected human at 250 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID234032 | Therapeutic Index (IC50/EC50) of the compound | 2001 | Bioorganic & medicinal chemistry letters, Jan-22, Volume: 11, Issue:2 | 3,28-Di-O-(dimethylsuccinyl)-betulin isomers as anti-HIV agents. |
| AID473139 | Antiviral activity against HIV1 3B infected in human MT2 cells assessed as inhibition of viral replication treated 1 day after infection measured on after 4 days postinfection by p24 antigen ELISA | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Anti-AIDS agents 81. Design, synthesis, and structure-activity relationship study of betulinic acid and moronic acid derivatives as potent HIV maturation inhibitors. |
| AID532666 | Antiviral activity against Human immunodeficiency virus 1 isolate 6 harboring Gag-SP-1 S373 and A374 mutant infected in human MT-2 cells by XTT-assay relative to wild-type | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID1726077 | Cytotoxicity against human MT4 cells treated for 3 days measured by Celltiter-glo luminescent assay | 2020 | ACS medicinal chemistry letters, Nov-12, Volume: 11, Issue:11 | Novel Betulinic Acid-Nucleoside Hybrids with Potent Anti-HIV Activity. |
| AID369593 | Tmax in healthy human plasma at 50 mg, po administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | Safety and pharmacokinetics of Bevirimat (PA-457), a novel inhibitor of human immunodeficiency virus maturation, in healthy volunteers. |
| AID1291870 | AUC (0 to 6 hrs) in cannula implanted rat at 5 mg/kg administered through oral gavage after 24 hrs by LC-MS/MS analysis | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Inhibitors of HIV-1 maturation: Development of structure-activity relationship for C-28 amides based on C-3 benzoic acid-modified triterpenoids. |
| AID1327728 | Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells by p24 ELISA | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19 | Incorporation of Privileged Structures into Bevirimat Can Improve Activity against Wild-Type and Bevirimat-Resistant HIV-1. |
| AID1327735 | Half life in human liver microsomes at 1 uM in presence of NADPH by LC/MS/MS analysis | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19 | Incorporation of Privileged Structures into Bevirimat Can Improve Activity against Wild-Type and Bevirimat-Resistant HIV-1. |
| AID532244 | Antiviral activity against antiretroviral-pretreated PI-resistant Human immunodeficiency virus 1 isolate 7 infected in human MT-2 cells by XTT assay relative to wild-type | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID1285295 | Antiviral activity against wild type HIV1 NLRepRlucP373S infected in human MT2 cells after 4 to 5 days by luciferase report gene based multiple cycle drug susceptibility assay | 2016 | Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8 | C-3 benzoic acid derivatives of C-3 deoxybetulinic acid and deoxybetulin as HIV-1 maturation inhibitors. |
| AID555851 | Antiviral activity against HIV1 PA114 harboring SP1 mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID1391864 | Cytotoxicity against human MT2 cells | 2018 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9 | The design, synthesis and structure-activity relationships associated with C28 amine-based betulinic acid derivatives as inhibitors of HIV-1 maturation. |
| AID555858 | Antiviral activity against HIV1 PA113 harboring SP1 mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID736138 | Antiviral activity against HIV1 NL4.3 infected in MAGIC-5B cells after 48 hrs by beta-galactosidase reporter gene assay | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Synthesis and biological evaluation of a new derivative of bevirimat that targets the Gag CA-SP1 cleavage site. |
| AID532265 | Antiviral activity against Human immunodeficiency virus 1 isolate 38 harboring Gag-SP1 V370A, N372S/G, S373P/T/Q/K, A374A/G/T/S, T375A and I376M mutant gene infected in human MT-2 cells by XTT assay relative to wild-type | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID350969 | Antiviral activity against HIV1 assessed as inhibition of release of CA/p24 from CA-SP1/p25 at 37.8 nM by MAGI assay | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID555854 | Antiviral activity against HIV1 PA107 harboring SP1 mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID492517 | Antiviral activity against HIV1 infected in human H9 cells after 4 days by p24 antigen ELISA | 2010 | Journal of natural products, Mar-26, Volume: 73, Issue:3 | Discovery and development of natural product-derived chemotherapeutic agents based on a medicinal chemistry approach. |
| AID310349 | Antiviral activity against HIV1 | 2007 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23 | Anti-AIDS agents 73: structure-activity relationship study and asymmetric synthesis of 3-O-monomethylsuccinyl-betulinic acid derivatives. |
| AID736131 | Antiviral activity against HIV1 NL4.3 infected in 293T cells assessed as acentric core at 5 ug/ml after 2 days by electron microscopic analysis | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Synthesis and biological evaluation of a new derivative of bevirimat that targets the Gag CA-SP1 cleavage site. |
| AID583854 | Antiviral activity against HIV1 NL4-3 infected in human MT2 cells assessed as inhibition of virus-induced cell death at 0.5 multiplicities of infection after 6 days | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10 | Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. |
| AID1708687 | Antiviral activity against wild type HIV-1 NL4-3 harbouring Gag AV370 mutant infected in MT-2 cells assessed as inhibition of viral replication in presence of 10% of fetal bovine serum by luciferase reporter gene based multicycle replication assay | 2021 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 36 | Design and exploration of C-3 benzoic acid bioisosteres and alkyl replacements in the context of GSK3532795 (BMS-955176) that exhibit broad spectrum HIV-1 maturation inhibition. |
| AID532246 | Antiviral activity against antiretroviral-pretreated Human immunodeficiency virus 1 isolate 21 harboring Gag-SP1 I375V mutant gene infected in human MT-2 cells by XTT assay relative to wild-type | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID1313358 | Binding affinity to gag polyprotein in wild type HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum/40% human serum by dual-luciferase reporter assay | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6 | Discovery of BMS-955176, a Second Generation HIV-1 Maturation Inhibitor with Broad Spectrum Antiviral Activity. |
| AID371951 | Cytotoxicity against human Raji cells assessed as cell viability at 100 molar ratio after 48 hrs by trypan blue staining method | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13 | Cancer preventive agents 9. Betulinic acid derivatives as potent cancer chemopreventive agents. |
| AID1672275 | Protein binding in human serum | 2019 | ACS medicinal chemistry letters, Mar-14, Volume: 10, Issue:3 | Second Generation Inhibitors of HIV-1 Maturation. |
| AID369582 | Dose normalized AUC (0 to infinity) in healthy human plasma at 25 mg, po administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | Safety and pharmacokinetics of Bevirimat (PA-457), a novel inhibitor of human immunodeficiency virus maturation, in healthy volunteers. |
| AID371948 | Inhibition of TPA-induced EBV-early antigen activation in human Raji cells assessed as EA induction after 48 hrs relative to TPA | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13 | Cancer preventive agents 9. Betulinic acid derivatives as potent cancer chemopreventive agents. |
| AID706458 | Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as p24 antigen level after 4 days by ELISA | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18 | Anti-AIDS agents 90. novel C-28 modified bevirimat analogues as potent HIV maturation inhibitors. |
| AID555869 | Antiviral activity against HIV1 HXB2 harboring SP1 V7A/T8delta mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID1672280 | Binding affinity to HIV-1 CA-SP1 cleavage site of Gag-Pol protein harboring deltaV370/Thr371Ala mutant assessed as inhibition of HIV-1 maturation | 2019 | ACS medicinal chemistry letters, Mar-14, Volume: 10, Issue:3 | Second Generation Inhibitors of HIV-1 Maturation. |
| AID351003 | Antiviral activity against HIV1 infected in human assessed as death rate constant of infected CD4 cells at 250 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID532449 | Antiviral activity against antiretroviral-pretreated PI-resistant Human immunodeficiency virus 1 isolate 2 harboring Gag-capsid G357S mutant gene and Gag-Sp-1 N372A, A374T and T375N mutant gene infected in human MT-2 cells by XTT assay relative to wild-ty | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID244675 | Therapeutic index expressed as ratio of IC50 for 50% toxicity to EC50 for 50% inhibition | 2004 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 14, Issue:23 | 3-O-Glutaryl-dihydrobetulin and related monoacyl derivatives as potent anti-HIV agents. |
| AID369585 | Cmax in healthy human plasma at 25 mg, po administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | Safety and pharmacokinetics of Bevirimat (PA-457), a novel inhibitor of human immunodeficiency virus maturation, in healthy volunteers. |
| AID736129 | Antiviral activity against HIV infected in H9 cells | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Synthesis and biological evaluation of a new derivative of bevirimat that targets the Gag CA-SP1 cleavage site. |
| AID369596 | AUC (0 to infinity) in healthy human plasma at 100 mg, po administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | Safety and pharmacokinetics of Bevirimat (PA-457), a novel inhibitor of human immunodeficiency virus maturation, in healthy volunteers. |
| AID555829 | Antiviral activity against HIV1 NL4.3 harboring SP1 T8A mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID1391915 | Half life in mouse liver microsomes at 0.5 uM in presence of NADPH by LC-MS/MS method | 2018 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9 | The design, synthesis and structure-activity relationships associated with C28 amine-based betulinic acid derivatives as inhibitors of HIV-1 maturation. |
| AID271051 | Cytotoxicity against human H9 lymphocytes | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Anti-AIDS agents 69. Moronic acid and other triterpene derivatives as novel potent anti-HIV agents. |
| AID532661 | Antiviral activity against Human immunodeficiency virus 1 isolate 29 harboring Gag-capsid I138M, A146P, R286K and A326S mutant gene and protease L10F, I13V, V32I, M36L, S37N, M46I, I47V, I62V, L63P, A71I, I72V and V82A mutant gene infected in human MT-2 c | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID1069002 | Chemopreventive activity in human Raji cells assessed as inhibition of TPA-induced EBV-early antigen activation by measuring EBV-EA positive cells at 10 molar ratio/20 ng/ml of TPA after 48 hrs by immunofluorescence analysis | 2014 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3 | A-ring modified betulinic acid derivatives as potent cancer preventive agents. |
| AID555848 | Antiviral activity against HIV1 PA108 harboring SP1 mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID310350 | Cytotoxicity against MT2 cells by XTT assay | 2007 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23 | Anti-AIDS agents 73: structure-activity relationship study and asymmetric synthesis of 3-O-monomethylsuccinyl-betulinic acid derivatives. |
| AID1733115 | Antiviral activity against HIV-1 NL4-3 infected in human MT4 cells assessed as reduction in p24 gag protein incubated for 4 days by ELISA | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | Design, synthesis, and structure activity relationship analysis of new betulinic acid derivatives as potent HIV inhibitors. |
| AID1471102 | Inhibition of bevirimat-resistant HIV-1 clade B isolate ASJM108 Gag V370A mutant infected in human PBMC after 7 days by scintillation counting method | 2017 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12 | Discovery of a novel and potent class of anti-HIV-1 maturation inhibitors with improved virology profile against gag polymorphisms. |
| AID271061 | Inhibition of membrane fusion between HIV1 NL4-3 envelope gene expressing COS cells and TZM cells | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Anti-AIDS agents 69. Moronic acid and other triterpene derivatives as novel potent anti-HIV agents. |
| AID1391863 | Binding affinity to CA-SP1 P373S/V370 deletion mutant in HIV-1 subtype B NL4-3 infected in human MT2 cells assessed as inhibition of viral maturation by measuring virus yield after 4 to 5 days in presence of 10% FBS by luciferase reporter gene assay | 2018 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9 | The design, synthesis and structure-activity relationships associated with C28 amine-based betulinic acid derivatives as inhibitors of HIV-1 maturation. |
| AID1391859 | Binding affinity to CA-SP1 P373S mutant in HIV-1 subtype B NL4-3 infected in human MT2 cells assessed as inhibition of viral maturation by measuring virus yields after 4 to 5 days in presence of 10% FBS by luciferase reporter gene assay | 2018 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9 | The design, synthesis and structure-activity relationships associated with C28 amine-based betulinic acid derivatives as inhibitors of HIV-1 maturation. |
| AID369766 | Toxicity in healthy human assessed as adverse event occurrence at 50 mg, po administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | Safety and pharmacokinetics of Bevirimat (PA-457), a novel inhibitor of human immunodeficiency virus maturation, in healthy volunteers. |
| AID439727 | Antiviral activity against HIV1 NL4-3 infected in human TZM-b1 cells assessed as reduction in luciferase activity after 2 days by luciferase reporter gene assay | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23 | Betulinic acid derivatives as human immunodeficiency virus type 2 (HIV-2) inhibitors. |
| AID673432 | Cytotoxicity against human MT4 assessed as cell viability after 2 days | 2012 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 22, Issue:16 | Synthesis of betulinic acid derivatives as entry inhibitors against HIV-1 and bevirimat-resistant HIV-1 variants. |
| AID350995 | Antiviral activity against HIV1 infected in human assessed as death rate constant of uninfected CD4 cells at 75 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID351178 | Antiviral activity against HIV1 infected in human assessed as maximum rate of viral replication measured as logarithmic viral copies at 75 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID350979 | Volume of distribution at steady state in HIV1 infected human at 250 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID310351 | Therapeutic index, ratio of IC50 for MT2 cells to EC50 for HIV1 | 2007 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23 | Anti-AIDS agents 73: structure-activity relationship study and asymmetric synthesis of 3-O-monomethylsuccinyl-betulinic acid derivatives. |
| AID1069005 | Chemopreventive activity in human Raji cells assessed as inhibition of TPA-induced EBV-early antigen activation by measuring EBV-EA positive cells at 100 molar ratio/20 ng/ml of TPA after 48 hrs by immunofluorescence analysis | 2014 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3 | A-ring modified betulinic acid derivatives as potent cancer preventive agents. |
| AID532260 | Antiviral activity against antiretroviral-pretreated PI-resistant Human immunodeficiency virus 1 isolate 10 harboring deletion at T371 of Gag-SP-1 and Gag-Sp-1 V370I, S373P and I376V mutant gene infected in human MT-2 cells by XTT assay relative to wild-t | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID555835 | Antiviral activity against HIV1 NL4.3 harboring SP1 V7A mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID1291876 | Cytotoxicity against human MT2 cells | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Inhibitors of HIV-1 maturation: Development of structure-activity relationship for C-28 amides based on C-3 benzoic acid-modified triterpenoids. |
| AID1327730 | Resistance index, ratio of IC50 for bevirimat-resistant HIV1 NL4-3 harboring GagV370A mutant infected in human MT4 cells to IC50 for wild type HIV1 NL4-3 infected in human MT4 cells | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19 | Incorporation of Privileged Structures into Bevirimat Can Improve Activity against Wild-Type and Bevirimat-Resistant HIV-1. |
| AID532670 | Antiviral activity against Human immunodeficiency virus 1 isolate 12 harboring Gag-capsid G357S mutant gene and Gag-SP1 V362I mutant infected in human MT-2 cells by XTT-assay relative to wild-type | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID1672283 | Ratio of EC50 for wild type HIV-1 NL4-3 CA-SP1 cleavage site of Gag-Pol protein in presence of human serum albumin to EC50 for wild type HIV-1 NL4-3 CA-SP1 cleavage site of Gag-Pol protein | 2019 | ACS medicinal chemistry letters, Mar-14, Volume: 10, Issue:3 | Second Generation Inhibitors of HIV-1 Maturation. |
| AID369609 | Apparent oral clearance in healthy human plasma at 250 mg, po administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | Safety and pharmacokinetics of Bevirimat (PA-457), a novel inhibitor of human immunodeficiency virus maturation, in healthy volunteers. |
| AID210597 | Therapeutic Index is the average of the IC50 to that of EC50 | 1998 | Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23 | Anti-AIDS agents. 34. Synthesis and structure-activity relationships of betulin derivatives as anti-HIV agents. |
| AID369612 | Protein binding in healthy human plasma at 90% HIV inhibitory drug level | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | Safety and pharmacokinetics of Bevirimat (PA-457), a novel inhibitor of human immunodeficiency virus maturation, in healthy volunteers. |
| AID492519 | Therapeutic index, ratio of IC50 for human H9 cells to EC50 for HIV1 | 2010 | Journal of natural products, Mar-26, Volume: 73, Issue:3 | Discovery and development of natural product-derived chemotherapeutic agents based on a medicinal chemistry approach. |
| AID555861 | Antiviral activity against HIV1 PA115 harboring SP1 mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID706257 | Elimination half life in human | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18 | Anti-AIDS agents 90. novel C-28 modified bevirimat analogues as potent HIV maturation inhibitors. |
| AID706460 | Cytotoxicity against human MT4 cells after 2 days | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18 | Anti-AIDS agents 90. novel C-28 modified bevirimat analogues as potent HIV maturation inhibitors. |
| AID79295 | Anti-HIV activity against acutely infected H9 lymphocytes. Activity expressed as concentration of compound able to suppress HIV replication by 50%. | 1998 | Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23 | Anti-AIDS agents. 34. Synthesis and structure-activity relationships of betulin derivatives as anti-HIV agents. |
| AID369765 | Toxicity in healthy human assessed as adverse event occurrence at 25 mg, po administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | Safety and pharmacokinetics of Bevirimat (PA-457), a novel inhibitor of human immunodeficiency virus maturation, in healthy volunteers. |
| AID351005 | Antiviral activity against HIV1 infected in human assessed as clearance rate of virions at 150 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID555830 | Antiviral activity against HIV1 HXB2 harboring SP1 T8delta mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID562870 | Selectivity ratio of EC50 for HIV1 harboring spacer peptide A1V mutant protein infected in human HeLa cells to EC50 for wild type HIV1 infected in human HeLa cells | 2009 | Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12 | New small-molecule inhibitor class targeting human immunodeficiency virus type 1 virion maturation. |
| AID1471101 | Inhibition of bevirimat-resistant HIV1 clade B NL4-3 CA-SP1 T371A mutant infected in human MT4 cells | 2017 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12 | Discovery of a novel and potent class of anti-HIV-1 maturation inhibitors with improved virology profile against gag polymorphisms. |
| AID378287 | Cytotoxicity against mock-infected human H9 cells | 2000 | Journal of natural products, Dec, Volume: 63, Issue:12 | Anti-AIDS agents 38. Anti-HIV activity of 3-O-acyl ursolic acid derivatives. |
| AID1471099 | Inhibition of bevirimat-resistant HIV1 clade B NL4-3 CA-SP1 Q369H mutant infected in human MT4 cells | 2017 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12 | Discovery of a novel and potent class of anti-HIV-1 maturation inhibitors with improved virology profile against gag polymorphisms. |
| AID1291867 | Antiviral activity against wild type BVM-resistant HIV1 NL4-3 habouring Gag protein delta T371 infected in human MT2 cells after 4 to 5 days by dual-luciferase reporter gene assay | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Inhibitors of HIV-1 maturation: Development of structure-activity relationship for C-28 amides based on C-3 benzoic acid-modified triterpenoids. |
| AID350991 | Absorption rate constant in HIV1 infected human at 250 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID350980 | Distributional clearance in HIV1 infected human at 75 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID1708688 | Antiviral activity against wild type HIV-1 NL4-3 infected in MT-2 cells assessed as inhibition of viral replication in presence of 10% of fetal bovine serum by luciferase reporter gene based multicycle replication assay | 2021 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 36 | Design and exploration of C-3 benzoic acid bioisosteres and alkyl replacements in the context of GSK3532795 (BMS-955176) that exhibit broad spectrum HIV-1 maturation inhibition. |
| AID1672251 | Protein binding in human plasma | 2019 | ACS medicinal chemistry letters, Mar-14, Volume: 10, Issue:3 | Second Generation Inhibitors of HIV-1 Maturation. |
| AID350999 | Antiviral activity against HIV1 infected in human assessed as rate at which virus infects CD4 cells at 150 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID351185 | Toxicity in HIV1 infected human assessed as mortality at 75 to 250 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID1391913 | Half life in rat liver microsomes at 0.5 uM in presence of NADPH by LC-MS/MS method | 2018 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9 | The design, synthesis and structure-activity relationships associated with C28 amine-based betulinic acid derivatives as inhibitors of HIV-1 maturation. |
| AID1228704 | Antiviral activity against HIV1 NL4.3-Ren infected in human MT2 cells assessed as inhibition of viral growth measured 48 hrs post infection by luminometry | 2015 | Journal of natural products, May-22, Volume: 78, Issue:5 | Isolation, Structural Modification, and HIV Inhibition of Pentacyclic Lupane-Type Triterpenoids from Cassine xylocarpa and Maytenus cuzcoina. |
| AID1708702 | Clearance in rat at 1 mg/kg, iv measured after 24 hrs | 2021 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 36 | Design and exploration of C-3 benzoic acid bioisosteres and alkyl replacements in the context of GSK3532795 (BMS-955176) that exhibit broad spectrum HIV-1 maturation inhibition. |
| AID350973 | Effect of CD4 cell count in HIV1 infected human at 250 mg, po after 10 days | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID555867 | Antiviral activity against HIV1 HXB2 harboring SP1 Q6H/T8delta mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID555860 | Antiviral activity against HIV1 PA112 harboring SP1 mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID350998 | Antiviral activity against HIV1 infected in human assessed as rate at which virus infects CD4 cells at 75 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID555849 | Antiviral activity against HIV1 PA119 harboring SP1 mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID1708690 | Cytotoxicity against human MT2 cells | 2021 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 36 | Design and exploration of C-3 benzoic acid bioisosteres and alkyl replacements in the context of GSK3532795 (BMS-955176) that exhibit broad spectrum HIV-1 maturation inhibition. |
| AID1313370 | Binding affinity to gag polyprotein V370M mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6 | Discovery of BMS-955176, a Second Generation HIV-1 Maturation Inhibitor with Broad Spectrum Antiviral Activity. |
| AID532659 | Antiviral activity against Human immunodeficiency virus 1 isolate 2 harboring Gag-capsid A146P, S173A, V215L, E230D, N252S, L268M and A340G mutant gene and protease L10I, I15V, K20R, M36I, S37N, M46I, L63P, V82A, N83H, I84V, I85T and L90M mutant gene infe | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID351183 | Antiviral activity against HIV1 infected in human assessed as growth/production of uninfected CD4 cells at 250 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID728086 | Antiviral activity against wild type Human immunodeficiency virus 1 NL4-3 infected in human 293T cells assessed as inhibition of CA-SP1 cleavage measured 2 days post infection by Western blotting analysis | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5 | New betulinic acid derivatives for bevirimat-resistant human immunodeficiency virus type-1. |
| AID501756 | Therapeutic index, ratio of IC50 for human MT4 cells to EC50 for HIV1 NL4-3 | 2010 | Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17 | Conjugates of betulin derivatives with AZT as potent anti-HIV agents. |
| AID1708697 | Oral bioavailability in rat measured at 5 mg/kg up to 24 hrs | 2021 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 36 | Design and exploration of C-3 benzoic acid bioisosteres and alkyl replacements in the context of GSK3532795 (BMS-955176) that exhibit broad spectrum HIV-1 maturation inhibition. |
| AID532247 | Antiviral activity against antiretroviral-pretreated PI-resistant Human immunodeficiency virus 1 isolate 26 harboring Gag-SP1 N372S, S373P and T375N mutant gene infected in human MT-2 cells by XTT assay relative to wild-type | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID1391858 | AUC (0 to 24 hrs) in Sprague-Dawley rat at 5 mg/kg, po via gavage by LC-MS/MS analysis | 2018 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9 | The design, synthesis and structure-activity relationships associated with C28 amine-based betulinic acid derivatives as inhibitors of HIV-1 maturation. |
| AID736133 | Antiviral activity against HIV1 NL4.3 infected in 293T cells assessed as aberrant core at 5 ug/ml after 2 days by electron microscopic analysis | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Synthesis and biological evaluation of a new derivative of bevirimat that targets the Gag CA-SP1 cleavage site. |
| AID532662 | Antiviral activity against Human immunodeficiency virus 1 isolate 1 harboring Gag-SP-1 S368, V370 and deletion at T371 in Gag-SP-1 mutant infected in human MT-2 cells by XTT-assay relative to wild-type | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID1285309 | Volume of distribution in steady state in cannula implanted rat at 1 mg/kg, iv by LC-MS/MS | 2016 | Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8 | C-3 benzoic acid derivatives of C-3 deoxybetulinic acid and deoxybetulin as HIV-1 maturation inhibitors. |
| AID621523 | Antiviral activity against drug-resistant HIV1 isolate | 2011 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19 | New betulinic acid derivatives as potent proteasome inhibitors. |
| AID369610 | Drug concentration in healthy human urine assessed as unconjugated drug level at 250 mg, po administered as single dose after 48 hrs | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | Safety and pharmacokinetics of Bevirimat (PA-457), a novel inhibitor of human immunodeficiency virus maturation, in healthy volunteers. |
| AID350971 | Effect of CD4 cell count in HIV1 infected human at 75 mg, po after 10 days | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID1313373 | Binding affinity to gag polyprotein T371 deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6 | Discovery of BMS-955176, a Second Generation HIV-1 Maturation Inhibitor with Broad Spectrum Antiviral Activity. |
| AID351175 | Antiviral activity against HIV1 infected in human assessed as inhibition of viral replication at 75 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID1471105 | Ratio of compound effect in presence of 40% human serum to compound effect in absence of serum for antiviral activity against HIV1 by cell based assay | 2017 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12 | Discovery of a novel and potent class of anti-HIV-1 maturation inhibitors with improved virology profile against gag polymorphisms. |
| AID350990 | Absorption rate constant in HIV1 infected human at 150 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID1228705 | Selectivity index, ratio of CC50 for mock-infected human MT2 cells to IC50 for HIV1 NL4.3-Ren infected in human MT2 cells | 2015 | Journal of natural products, May-22, Volume: 78, Issue:5 | Isolation, Structural Modification, and HIV Inhibition of Pentacyclic Lupane-Type Triterpenoids from Cassine xylocarpa and Maytenus cuzcoina. |
| AID350983 | Apparent oral clearance in HIV1 infected human at 75 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID271059 | Antiviral activity against HIV1 PI-R replication in human MT4 cells | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Anti-AIDS agents 69. Moronic acid and other triterpene derivatives as novel potent anti-HIV agents. |
| AID555833 | Antiviral activity against HIV1 HXB2 harboring SP1 V7M mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID532664 | Antiviral activity against Human immunodeficiency virus 1 isolate 6 harboring Gag-SP-1 V370, S373 and A374 mutant infected in human MT-2 cells by XTT-assay relative to wild-type | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID555844 | Antiviral activity against HIV1 PA109 harboring SP1 mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID1391860 | Binding affinity to CA-SP1 P373S mutant in HIV-1 subtype B NL4-3 infected in human MT2 cells assessed as inhibition of viral maturation by measuring virus yields after 4 to 5 days in presence of 10% FBS/15 mg/ml HSA by luciferase reporter gene assay | 2018 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9 | The design, synthesis and structure-activity relationships associated with C28 amine-based betulinic acid derivatives as inhibitors of HIV-1 maturation. |
| AID371949 | Cytotoxicity against human Raji cells assessed as cell viability at 1000 molar ratio after 48 hrs by trypan blue staining method | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13 | Cancer preventive agents 9. Betulinic acid derivatives as potent cancer chemopreventive agents. |
| AID1520506 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 3 days by CellTiter-Glo luminescent assay | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Discovery and synthesis of novel beesioside I derivatives with potent anti-HIV activity. |
| AID351174 | Antiviral activity against HIV1 infected in human assessed as number of new virions produced by infected CD4 cells at 250 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID1313368 | Binding affinity to gag polyprotein V3621 mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6 | Discovery of BMS-955176, a Second Generation HIV-1 Maturation Inhibitor with Broad Spectrum Antiviral Activity. |
| AID78942 | Inhibitory activity against HIV-1 replication in mock infected H9 cells | 1996 | Journal of medicinal chemistry, Mar-01, Volume: 39, Issue:5 | Betulinic acid and dihydrobetulinic acid derivatives as potent anti-HIV agents. |
| AID1672278 | Binding affinity to HIV-1 CA-SP1 cleavage site of Gag-Pol protein harboring G369H mutant assessed as inhibition of HIV-1 maturation | 2019 | ACS medicinal chemistry letters, Mar-14, Volume: 10, Issue:3 | Second Generation Inhibitors of HIV-1 Maturation. |
| AID556037 | Antiviral activity against HIV1 HXB2 harboring SP1 Q6H /V7A/T8N mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID271063 | Antiviral activity against HIV1 FHR2 replication in MT4 cells at 5 uM | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Anti-AIDS agents 69. Moronic acid and other triterpene derivatives as novel potent anti-HIV agents. |
| AID1069001 | Chemopreventive activity in human Raji cells assessed as molar ratio of compound required to inhibit 50% of control of inhibition of TPA-induced EBV-early antigen activation after 48 hrs by immunofluorescence analysis | 2014 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3 | A-ring modified betulinic acid derivatives as potent cancer preventive agents. |
| AID350994 | Half life in HIV1 infected human at 250 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID562703 | Antiviral activity against HIV1 harboring spacer peptide A1V mutant protein infected in human HeLa cells assessed as decrease in viral infection after 72 hrs by beta-galactosidase reporter gene assay | 2009 | Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12 | New small-molecule inhibitor class targeting human immunodeficiency virus type 1 virion maturation. |
| AID351182 | Antiviral activity against HIV1 infected in human assessed as growth/production of uninfected CD4 cells at 150 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID1069004 | Chemopreventive activity in human Raji cells assessed as inhibition of TPA-induced EBV-early antigen activation by measuring EBV-EA positive cells at 1000 molar ratio/20 ng/ml of TPA after 48 hrs by immunofluorescence analysis relative to control | 2014 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3 | A-ring modified betulinic acid derivatives as potent cancer preventive agents. |
| AID532253 | Antiviral activity against antiretroviral-pretreated PI-resistant Human immunodeficiency virus 1 isolate 9 harboring Gag-SP1 T375N and I376V mutant gene infected in human MT-2 cells by XTT assay relative to wild-type | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID1265943 | Cytotoxicity against human MT4 cells by cell-titer Glo assay | 2016 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 26, Issue:1 | Fluorinated betulinic acid derivatives and evaluation of their anti-HIV activity. |
| AID1454744 | Antiviral activity against Human immunodeficiency virus assessed as reduction in maturation | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Natural-Products-Inspired Use of the gem-Dimethyl Group in Medicinal Chemistry. |
| AID532254 | Antiviral activity against Human immunodeficiency virus 1 isolate 30 infected in human MT-2 cells by XTT assay relative to wild-type | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID1327731 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 2 days by CytoTox-Glo assay | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19 | Incorporation of Privileged Structures into Bevirimat Can Improve Activity against Wild-Type and Bevirimat-Resistant HIV-1. |
| AID555842 | Antiviral activity against HIV1 NL4.3 harboring SP1 mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID271058 | Antiviral activity against HIV1 NL4-3 replication in human MT4 cells | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Anti-AIDS agents 69. Moronic acid and other triterpene derivatives as novel potent anti-HIV agents. |
| AID350974 | Antiviral activity against HIV1 infected in human assessed as logarithmic reduction in HIV RNA copies at 75 mg, po relative to baseline | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID369583 | AUC (0 to infinity) in healthy human plasma at 25 mg, po administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | Safety and pharmacokinetics of Bevirimat (PA-457), a novel inhibitor of human immunodeficiency virus maturation, in healthy volunteers. |
| AID555864 | Antiviral activity against HIV1 clinical isolates | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID555839 | Antiviral activity against HIV1 NL4.3 harboring SP1 Q6H mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID1285299 | Cytotoxicity against human MT2 cells assessed as cell viability by redox dye assay | 2016 | Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8 | C-3 benzoic acid derivatives of C-3 deoxybetulinic acid and deoxybetulin as HIV-1 maturation inhibitors. |
| AID736132 | Antiviral activity against HIV1 NL4.3 infected in 293T cells assessed as spherical core at 5 ug/ml after 2 days by electron microscopic analysis | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Synthesis and biological evaluation of a new derivative of bevirimat that targets the Gag CA-SP1 cleavage site. |
| AID1313363 | AUC (0 to 24 hrs) in rat at 5 mg/kg, po | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6 | Discovery of BMS-955176, a Second Generation HIV-1 Maturation Inhibitor with Broad Spectrum Antiviral Activity. |
| AID1672248 | Binding affinity to wild type HIV-1 NL4-3 CA-SP1 cleavage site of Gag-Pol protein assessed as inhibition of HIV-1 maturation | 2019 | ACS medicinal chemistry letters, Mar-14, Volume: 10, Issue:3 | Second Generation Inhibitors of HIV-1 Maturation. |
| AID1391868 | Binding affinity to CA-SP1 P373S mutant in HIV-1 subtype B NL4-3 infected in human MT2 cells assessed as inhibition of viral maturation by measuring virus yield after 4 to 5 days in presence of 10% FBS/40% human serum by luciferase reporter gene assay | 2018 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9 | The design, synthesis and structure-activity relationships associated with C28 amine-based betulinic acid derivatives as inhibitors of HIV-1 maturation. |
| AID371952 | Cytotoxicity against human Raji cells assessed as cell viability at 10 molar ratio after 48 hrs by trypan blue staining method | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13 | Cancer preventive agents 9. Betulinic acid derivatives as potent cancer chemopreventive agents. |
| AID350988 | Tlag in HIV1 infected human at 250 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID369598 | Cmax in healthy human plasma at 100 mg, po administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | Safety and pharmacokinetics of Bevirimat (PA-457), a novel inhibitor of human immunodeficiency virus maturation, in healthy volunteers. |
| AID532261 | Antiviral activity against Human immunodeficiency virus 1 isolate 31 harboring Gag-SP1 V370A, T371S, N372A/T, A374N/T and I376V mutant gene infected in human MT-2 cells by XTT assay relative to wild-type | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID555834 | Antiviral activity against HIV1 HXB2 harboring SP1 V7A mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID555846 | Antiviral activity against HIV1 PA106 harboring SP1 mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID351184 | Half life in po dosed human | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID350996 | Antiviral activity against HIV1 infected in human assessed as death rate constant of uninfected CD4 cells at 150 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID1471100 | Inhibition of bevirimat-resistant HIV1 clade B NL4-3 CA-SP1 V370A mutant infected in human MT4 cells | 2017 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12 | Discovery of a novel and potent class of anti-HIV-1 maturation inhibitors with improved virology profile against gag polymorphisms. |
| AID371945 | Inhibition of TPA-induced EBV-early antigen activation in human Raji cells assessed as EA induction at 500 molar ratio after 48 hrs relative to TPA | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13 | Cancer preventive agents 9. Betulinic acid derivatives as potent cancer chemopreventive agents. |
| AID532257 | Antiviral activity against antiretroviral-pretreated PI-resistant Human immunodeficiency virus 1 isolate 1 harboring Gag-Sp-1 S368C, V370A and A374N mutant gene deletion at T371 in Gag-SP-1 infected in human MT-2 cells by XTT assay relative to wild-type | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID1291866 | Antiviral activity against wild type BVM-resistant HIV1 NL4-3 habouring Gag protein T371A mutant infected in human MT2 cells after 4 to 5 days by dual-luciferase reporter gene assay | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Inhibitors of HIV-1 maturation: Development of structure-activity relationship for C-28 amides based on C-3 benzoic acid-modified triterpenoids. |
| AID271052 | Antiviral activity against HIV1 3B in H9 lymphocytes | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Anti-AIDS agents 69. Moronic acid and other triterpene derivatives as novel potent anti-HIV agents. |
| AID555868 | Antiviral activity against HIV1 HXB2 harboring SP1 Q6H/T8N mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID369602 | Apparent oral clearance in healthy human plasma at 100 mg, po administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | Safety and pharmacokinetics of Bevirimat (PA-457), a novel inhibitor of human immunodeficiency virus maturation, in healthy volunteers. |
| AID1471104 | Inhibition of bevirimat-resistant HIV-1 clade A isolate I-2496 V370A mutant infected in human PBMC after 7 days by scintillation counting method | 2017 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12 | Discovery of a novel and potent class of anti-HIV-1 maturation inhibitors with improved virology profile against gag polymorphisms. |
| AID1391866 | Plasma concentration in Sprague-Dawley rat at 5 mg/kg, po via gavage after 24 hrs by LC-MS/MS analysis | 2018 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9 | The design, synthesis and structure-activity relationships associated with C28 amine-based betulinic acid derivatives as inhibitors of HIV-1 maturation. |
| AID621521 | Inhibition of human 20S proteasome trypsin-like activity using Bz-VGR-AMC fluorogenic substrate by fluorimetry | 2011 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19 | New betulinic acid derivatives as potent proteasome inhibitors. |
| AID532671 | Antiviral activity against Human immunodeficiency virus 1 isolates harboring deletion at T371 in Gag-SP-1 relative to wild-type | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID532245 | Antiviral activity against antiretroviral-pretreated Human immunodeficiency virus 1 isolate 8 infected in human MT-2 cells by XTT assay relative to wild-type | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID1291872 | Cmax in cannula implanted rat at 5 mg/kg administered through oral gavage after 24 hrs by LC-MS/MS analysis | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Inhibitors of HIV-1 maturation: Development of structure-activity relationship for C-28 amides based on C-3 benzoic acid-modified triterpenoids. |
| AID532248 | Antiviral activity against antiretroviral-pretreated PI-resistant Human immunodeficiency virus 1 isolate 28 infected in human MT-2 cells by XTT assay relative to wild-type | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID706256 | Antiviral activity against HIV1 infected in human TZM-bl cells assessed as reduction of viral entry after 48 hrs by luciferase reporter gene assay | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18 | Anti-AIDS agents 90. novel C-28 modified bevirimat analogues as potent HIV maturation inhibitors. |
| AID79116 | Evaluated for the anti-HIV activity against HIV-1 replication in H9 lymphocyte cells | 2001 | Bioorganic & medicinal chemistry letters, Jan-22, Volume: 11, Issue:2 | 3,28-Di-O-(dimethylsuccinyl)-betulin isomers as anti-HIV agents. |
| AID369601 | Half life in healthy human plasma at 100 mg, po administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | Safety and pharmacokinetics of Bevirimat (PA-457), a novel inhibitor of human immunodeficiency virus maturation, in healthy volunteers. |
| AID350989 | Absorption rate constant in HIV1 infected human at 75 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID350975 | Antiviral activity against HIV1 infected in human assessed as logarithmic reduction in HIV RNA copies at 150 mg, po relative to baseline | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID1069003 | Chemopreventive activity in human Raji cells assessed as inhibition of TPA-induced EBV-early antigen activation by measuring EBV-EA positive cells at 500 molar ratio/20 ng/ml of TPA after 48 hrs by immunofluorescence analysis | 2014 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3 | A-ring modified betulinic acid derivatives as potent cancer preventive agents. |
| AID1313361 | Binding affinity to gag polyprotein V370A deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6 | Discovery of BMS-955176, a Second Generation HIV-1 Maturation Inhibitor with Broad Spectrum Antiviral Activity. |
| AID439730 | Selectivity index, ratio of TC50 for human TZM-b1 cells to IC50 for HIV2 KR X3 infected in human TZM-b1 cells | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23 | Betulinic acid derivatives as human immunodeficiency virus type 2 (HIV-2) inhibitors. |
| AID673430 | Antiviral activity against bevirimat-resistant HIV1 NL4-3 harboring QVT motif of Gag SP1 deltaT371 mutant infected in human MT4 cells assessed as reduction of viral p24 level cells by fluorescence assay relative to wild type HIV1 NL4-3 after 4 days by ELI | 2012 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 22, Issue:16 | Synthesis of betulinic acid derivatives as entry inhibitors against HIV-1 and bevirimat-resistant HIV-1 variants. |
| AID378288 | Therapeutic index, IC50 for human T-lymphoid H9 cells to EC50 for HIV1 3B isolate | 2000 | Journal of natural products, Dec, Volume: 63, Issue:12 | Anti-AIDS agents 38. Anti-HIV activity of 3-O-acyl ursolic acid derivatives. |
| AID1291862 | Antiviral activity against wild type HIV1 NL4-3 infected in human MT2 cells after 4 to 5 days by dual-luciferase reporter gene assay in presence of human serum albumin | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Inhibitors of HIV-1 maturation: Development of structure-activity relationship for C-28 amides based on C-3 benzoic acid-modified triterpenoids. |
| AID350155 | Antiviral activity against HIV1 3B infected in human MT2 cells assessed as p24 antigen level after 4 days by ELISA | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10 | Anti-AIDS agents. 78. Design, synthesis, metabolic stability assessment, and antiviral evaluation of novel betulinic acid derivatives as potent anti-human immunodeficiency virus (HIV) agents. |
| AID1285314 | Binding affinity to HIV1 Gag polyprotein assessed as protease-mediated p25-Spacer peptide 1 cleavage in HEK293T cells by measuring p4/p25 ratio at 1 to 3 uM by Western blot analysis | 2016 | Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8 | C-3 benzoic acid derivatives of C-3 deoxybetulinic acid and deoxybetulin as HIV-1 maturation inhibitors. |
| AID562704 | Selectivity ratio of EC50 for HIV1 harboring capsid I201V mutant protein infected in human HeLa cells to EC50 for wild type HIV1 infected in human HeLa cells | 2009 | Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12 | New small-molecule inhibitor class targeting human immunodeficiency virus type 1 virion maturation. |
| AID1327734 | Antiinfective activity against wild type HIV1 NL4-3 assessed as inhibition of viral infection by measuring viral infection level in human TZM-bl cells at 2 uM after 48 hrs by luciferase reporter gene assay (Rvb = 100%) | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19 | Incorporation of Privileged Structures into Bevirimat Can Improve Activity against Wild-Type and Bevirimat-Resistant HIV-1. |
| AID555837 | Antiviral activity against HIV1 HXB2 harboring SP1 Q6H mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID706457 | Therapeutic index, ratio of CC50 for human MT4 cells to IC50 for HIV-1 NL4-3 | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18 | Anti-AIDS agents 90. novel C-28 modified bevirimat analogues as potent HIV maturation inhibitors. |
| AID1285306 | Cmax in rat at 5 mg/kg, po by LC-MS/MS | 2016 | Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8 | C-3 benzoic acid derivatives of C-3 deoxybetulinic acid and deoxybetulin as HIV-1 maturation inhibitors. |
| AID736137 | Cytotoxicity against human MAGIC-5B cells after 48 hrs by MTT assay | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Synthesis and biological evaluation of a new derivative of bevirimat that targets the Gag CA-SP1 cleavage site. |
| AID532660 | Antiviral activity against Human immunodeficiency virus 1 isolate 4 harboring Gag-capsid A146P, V159I, V215L, I223G/V, P255A, E312D and G357S mutant gene and protease L10R, S37N, M46L, I62V, L63P, A71V, V82T, L90M and I93L mutant gene infected in human MT | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID555856 | Antiviral activity against HIV1 PA104 harboring SP1 mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID555862 | Antiviral activity against HIV1 PA110 harboring SP1 mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID1672252 | Binding affinity to wild type HIV-1 NL4-3 CA-SP1 cleavage site of Gag-Pol protein assessed as inhibition of HIV-1 maturation in presence of human serum albumin | 2019 | ACS medicinal chemistry letters, Mar-14, Volume: 10, Issue:3 | Second Generation Inhibitors of HIV-1 Maturation. |
| AID369768 | Toxicity in healthy human assessed as adverse event occurrence at 250 mg, po administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | Safety and pharmacokinetics of Bevirimat (PA-457), a novel inhibitor of human immunodeficiency virus maturation, in healthy volunteers. |
| AID555853 | Antiviral activity against HIV1 PA101 harboring SP1 mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID728090 | Cytotoxicity against human MT4 cells for 4 days | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5 | New betulinic acid derivatives for bevirimat-resistant human immunodeficiency virus type-1. |
| AID532668 | Antiviral activity against Human immunodeficiency virus 1 isolate 8 harboring Gag-SP1 V362I mutant infected in human MT-2 cells by XTT-assay relative to wild-type | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID350986 | Tlag in HIV1 infected human at 75 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID473142 | Therapeutic index, IC50 for human MT2 cells to EC50 for HIV1 3B | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Anti-AIDS agents 81. Design, synthesis, and structure-activity relationship study of betulinic acid and moronic acid derivatives as potent HIV maturation inhibitors. |
| AID351186 | Stability in human plasma | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID555850 | Antiviral activity against HIV1 PA118 harboring SP1 mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID350970 | Toxicity in HIV1 infected human assessed as incidence of adverse effect at 75 to 250 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID673429 | Antiviral activity against bevirimat-resistant HIV1 NL4-3 harboring QVT motif of Gag SP1 V370A mutant infected in human MT4 cells assessed as reduction of viral p24 level cells by fluorescence assay relative to wild type HIV1 NL4-3 after 4 days by ELISA | 2012 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 22, Issue:16 | Synthesis of betulinic acid derivatives as entry inhibitors against HIV-1 and bevirimat-resistant HIV-1 variants. |
| AID556035 | Antiviral activity against HIV1 HXB2 harboring SP1 V7A/T8N mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID1733116 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 2 days by CytoTox-Glo cytotoxicity assay | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | Design, synthesis, and structure activity relationship analysis of new betulinic acid derivatives as potent HIV inhibitors. |
| AID351004 | Antiviral activity against HIV1 infected in human assessed as clearance rate of virions at 75 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID351181 | Antiviral activity against HIV1 infected in human assessed as growth/production of uninfected CD4 cells at 75 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID532450 | Antiviral activity against antiretroviral-pretreated PI-resistant Human immunodeficiency virus 1 isolate 4 harboring Gag-SP-1 S373A, A374G and T375A mutant gene infected in human MT-2 cells by XTT assay relative to wild-type | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID1228702 | Antiviral activity against HIV1 NL4.3-Ren infected in human MT2 cells assessed as inhibition of viral growth at 10 uM measured 48 hrs post infection by luminometry | 2015 | Journal of natural products, May-22, Volume: 78, Issue:5 | Isolation, Structural Modification, and HIV Inhibition of Pentacyclic Lupane-Type Triterpenoids from Cassine xylocarpa and Maytenus cuzcoina. |
| AID369592 | Cmax in healthy human plasma after 50 mg oral dose, normalised for 70 kg subject | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | Safety and pharmacokinetics of Bevirimat (PA-457), a novel inhibitor of human immunodeficiency virus maturation, in healthy volunteers. |
| AID271053 | Therapeutic index, IC50 for H9/EC50 for HIV 3B | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Anti-AIDS agents 69. Moronic acid and other triterpene derivatives as novel potent anti-HIV agents. |
| AID350977 | Volume of distribution at steady state in HIV1 infected human at 75 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID555836 | Antiviral activity against HIV1 NL4.3 harboring SP1 V7delta mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID351007 | Antiviral activity against HIV1 infected in human assessed as number of new virions produced by infected CD4 cell at 75 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID1285307 | Tmax in rat at 5 mg/kg, po by LC-MS/MS | 2016 | Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8 | C-3 benzoic acid derivatives of C-3 deoxybetulinic acid and deoxybetulin as HIV-1 maturation inhibitors. |
| AID728091 | Antiviral activity against 0.001 MOI bevirimat-resistant Human immunodeficiency virus 1 NL4-3 harboring gag V370A mutant infected in human MT4 cells assessed as inhibition of viral replication measured 4 days post infection by ELISA | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5 | New betulinic acid derivatives for bevirimat-resistant human immunodeficiency virus type-1. |
| AID532665 | Antiviral activity against Human immunodeficiency virus 1 isolate 6 harboring Gag-SP-1 V370 mutant infected in human MT-2 cells by XTT-assay relative to wild-type | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID369594 | Half life in healthy human plasma at 50 mg, po administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | Safety and pharmacokinetics of Bevirimat (PA-457), a novel inhibitor of human immunodeficiency virus maturation, in healthy volunteers. |
| AID1285310 | Antiviral activity against HIV1 infected in human H9 cells | 2016 | Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8 | C-3 benzoic acid derivatives of C-3 deoxybetulinic acid and deoxybetulin as HIV-1 maturation inhibitors. |
| AID350972 | Effect of CD4 cell count in HIV1 infected human at 150 mg, po after 10 days | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID532446 | Antiviral activity against antiretroviral-pretreated PI-resistant Human immunodeficiency virus 1 isolate 24 harboring Gag-capsid V362I mutant gene, Gag-SP-1 V370A, N372T and T375A mutant gene and deletion at T371 in Gag-SP-1 infected in human MT-2 cells b | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID369591 | Cmax in healthy human plasma at 50 mg, po administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | Safety and pharmacokinetics of Bevirimat (PA-457), a novel inhibitor of human immunodeficiency virus maturation, in healthy volunteers. |
| AID369597 | Dose normalized AUC (0 to infinity) in healthy human plasma at 100 mg, po administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | Safety and pharmacokinetics of Bevirimat (PA-457), a novel inhibitor of human immunodeficiency virus maturation, in healthy volunteers. |
| AID1291861 | Antiviral activity against wild type HIV1 NL4-3 infected in human MT2 cells after 4 to 5 days by dual-luciferase reporter gene assay | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Inhibitors of HIV-1 maturation: Development of structure-activity relationship for C-28 amides based on C-3 benzoic acid-modified triterpenoids. |
| AID555857 | Antiviral activity against HIV1 PA116 harboring SP1 mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID369600 | Tmax in healthy human plasma at 100 mg, po administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | Safety and pharmacokinetics of Bevirimat (PA-457), a novel inhibitor of human immunodeficiency virus maturation, in healthy volunteers. |
| AID1313357 | Binding affinity to gag polyprotein in wild type HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6 | Discovery of BMS-955176, a Second Generation HIV-1 Maturation Inhibitor with Broad Spectrum Antiviral Activity. |
| AID532669 | Antiviral activity against Human immunodeficiency virus 1 LAI Gag-SP1 V362I mutant infected in human MT-2 cells by XTT-assay relative to wild-type | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID501754 | Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of viral replication after 4 days by p24 antigen based ELISA assay | 2010 | Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17 | Conjugates of betulin derivatives with AZT as potent anti-HIV agents. |
| AID369595 | Apparent oral clearance in healthy human plasma at 50 mg, po administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | Safety and pharmacokinetics of Bevirimat (PA-457), a novel inhibitor of human immunodeficiency virus maturation, in healthy volunteers. |
| AID555852 | Antiviral activity against HIV1 PA103 harboring SP1 mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID1291873 | Plasma concentration in cannula implanted rat at 5 mg/kg administered through oral gavage after 24 hrs by LC-MS/MS analysis | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Inhibitors of HIV-1 maturation: Development of structure-activity relationship for C-28 amides based on C-3 benzoic acid-modified triterpenoids. |
| AID532663 | Antiviral activity against Human immunodeficiency virus 1 isolate 3 harboring Gag-capsid N372A and V370 mutant gene and deletion at T371 in Gag-SP-1 infected in human MT-2 cells by XTT-assay relative to wild-type | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID532255 | Antiviral activity against antiretroviral-pretreated PI-resistant Human immunodeficiency virus 1 isolate 25 harboring Gag-capsid G357S mutant gene and Gag-SP-1 V373A mutant gene infected in human MT-2 cells by XTT assay relative to wild-type | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID1726078 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV1 NL4-3 | 2020 | ACS medicinal chemistry letters, Nov-12, Volume: 11, Issue:11 | Novel Betulinic Acid-Nucleoside Hybrids with Potent Anti-HIV Activity. |
| AID350981 | Distributional clearance in HIV1 infected human at 150 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID198242 | Inhibitory activity against HIV-RT | 1996 | Journal of medicinal chemistry, Mar-01, Volume: 39, Issue:5 | Betulinic acid and dihydrobetulinic acid derivatives as potent anti-HIV agents. |
| AID1708699 | AUCtotal in rat at 5 mg/kg, po measured after 24 hrs | 2021 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 36 | Design and exploration of C-3 benzoic acid bioisosteres and alkyl replacements in the context of GSK3532795 (BMS-955176) that exhibit broad spectrum HIV-1 maturation inhibition. |
| AID369605 | Cmax in healthy human plasma at 250 mg, po administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | Safety and pharmacokinetics of Bevirimat (PA-457), a novel inhibitor of human immunodeficiency virus maturation, in healthy volunteers. |
| AID350978 | Volume of distribution at steady state in HIV1 infected human at 150 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID583852 | Antiviral activity against HIV1 NL4-3 infected in human MT2 cells assessed as inhibition of virus-induced cell death at 0.005 multiplicities of infection after 6 days | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10 | Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. |
| AID1291874 | Plasma clearance in cannula implanted rat at 1 mg/kg, iv by LC-MS/MS analysis | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Inhibitors of HIV-1 maturation: Development of structure-activity relationship for C-28 amides based on C-3 benzoic acid-modified triterpenoids. |
| AID351177 | Antiviral activity against HIV1 infected in human assessed as inhibition of viral replication at 250 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection. |
| AID1291875 | Volume of distribution at steady state in cannula implanted rat at 1 mg/kg, iv by LC-MS/MS analysis | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Inhibitors of HIV-1 maturation: Development of structure-activity relationship for C-28 amides based on C-3 benzoic acid-modified triterpenoids. |
| AID555859 | Antiviral activity against HIV1 PA117 harboring SP1 mutant gene relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Susceptibility of human immunodeficiency virus type 1 to the maturation inhibitor bevirimat is modulated by baseline polymorphisms in Gag spacer peptide 1. |
| AID439729 | Cytotoxicity against human TZM-b1 cells after 2 days | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23 | Betulinic acid derivatives as human immunodeficiency virus type 2 (HIV-2) inhibitors. |
| AID532250 | Antiviral activity against antiretroviral-pretreated PI-resistant Human immunodeficiency virus 1 isolate 20 harboring Gag-capsid G357S mutant gene and Gag-SP1 Q369H and I376V mutant gene infected in human MT-2 cells by XTT assay relative to wild-type | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID1672282 | Binding affinity to HIV-1 CA-SP1 cleavage site of Gag-Pol protein harboring deltaThr371 mutant assessed as inhibition of HIV-1 maturation | 2019 | ACS medicinal chemistry letters, Mar-14, Volume: 10, Issue:3 | Second Generation Inhibitors of HIV-1 Maturation. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 2 (1.89) | 18.2507 |
| 2000's | 49 (46.23) | 29.6817 |
| 2010's | 43 (40.57) | 24.3611 |
| 2020's | 12 (11.32) | 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 (28.39) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 5 (4.55%) | 5.53% |
| Reviews | 13 (11.82%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 92 (83.64%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||