antiretroviral

Ancriviroc (SCH-351125) is an oxime-piperidine compound with strong antiretroviral activity and an orally bioavailable small molecule chemokine receptor CCR5 antagonist (Kd value 9.27nM) that enters HIV-1 through the CCR5 co-receptor and is used to study HIV-1.

Apricitabine (SPD754) is a highly selective and orally active HIV-1 reverse transcriptase inhibitor (Ki=0.08 μM), the (-) enantiomer of 2′-deoxy-3′-oxy-4′-thiocytidine (dOTC) . Apricitabine inhibits DNA polymerase α, β and γ with Ki values of 300 μM, 12 μM and 112.25 μM, respectively. Apricitabine has shown good antiretroviral therapeutic efficacy in antiretroviral HIV-infected patients, with good tolerability and low selective resistance.

DNA polymerase-IN-1, a DNA polymerase inhibitor, exhibited antiproliferative activity against tumor cells with a half-inhibitory concentration (IC50) of 20.7 μM. DNA polymerase-IN-1 inhibited Taq DNA polymerase with an IC50 of less than 250 μM. DNA polymerase-IN-1 was shown to inhibit Taq DNA polymerase by RT- DNA polymerase-IN-1 showed antiretroviral activity in vitro by RT-PCR assay and can be used to study oxidative damage and colorectal cancer.

Nevirapine (NVP) is a benzodiazepine non-nucleoside reverse transcriptase inhibitor. In combination with other antiretroviral drugs, nevirapine reduces HIV viral loads and increases CD4 counts, thereby retarding or preventing the damage to the immune system and reducing the risk of developing AIDS.

Cabotegravir (S GSK1265744) (GSK744, GSK1265744) is a long-acting HIV integrase inhibitor and inhibits the HIV-1 integrase catalyzed strand transfer reaction (IC50: 3.0 nM).

Stavudine (BMY-27857), a nucleoside reverse transcriptase inhibitor analog of thymidine, has activity against HIV.

Didanosine (ddI) is a nucleoside reverse transcriptase inhibitor analog of adenosine (IC50: 0.49 μM).

Tenofovir alafenamide (GS-7340) is a nucleotide reverse transcriptase inhibitor (NRTI) and a novel ester prodrug of the antiretroviral tenofovir.

Bavtavirine is a potent non-nucleoside reverse transcriptase inhibitor (NNRTIs) that inhibits HIV replication by inhibiting HIV-1 reverse transcriptase activity and preventing the transcription of viral RNA into DNA for use in Highly Active Antiretroviral Therapy (HAART) programs and HIV disease studies

Lenacapavir (GS-6207) is the first HIV-1 capsid inhibitor approved by the U.S. Food and Drug Administration, the European Medicines Agency, and Health Canada for the treatment of MDR HIV-1 infection.[3]

Betulinic acid (ALS-357) is a pentacyclic lupane-type triterpene derivative of betulin (isolated from the bark of Betula alba, the common white birch) which has antiretroviral, antimalarial, and anti-inflammatory properties, as well as a more recently discovered potential as an anticancer agent, by inhibition of topoisomerase.

Nelfinavir (AG1341) is an antiretroviral drug used in the treatment of the human immunodeficiency virus (HIV) (Ki=2 nM). Nelfinavir is a broad-spectrum, anticancer agent.

Fosamprenavir (Amprenavir phosphate; GW 433908) is a phosphate ester prodrug of the antiretroviral protease inhibitor Amprenavir, offering improved solubility over the parent molecule and exhibiting anti-HIV infection effects [1].

Lenacapavir, also known as GS-6207, is an HIV-1 capsid inhibitor. It demonstrates an average EC50 of 50 pM (ranging from 20-160 pM) against 23 clinical isolates of HIV-1 from diverse subtypes, with tests performed in peripheral blood mononuclear cells (PBMCs). In vitro, Lenacapavir exhibits picomolar potency and shows no cross-resistance with existing antiretroviral compounds. Furthermore, Lenacapavir displays significant antiviral activity in individuals with HIV-1, regardless of prior treatment history, with no pre-existing resistance detected.

Tipranavir C-14 is an antiretroviral protease inhibitor primarily used for the treatment and prevention of human immunodeficiency virus (HIV) infection and acquired immunodeficiency syndrome (AIDS).

Pseudohypericin has photocytotoxic, and antiretroviral activities, it has potential therapeutic value in diseases such as AIDS.

Hck-IN-1 is a selective Nef-dependent Hck inhibitor (IC50s: 2.8 μM and >20 μM for Nef:Hck complex and Hck) with antiretroviral activity. Hck-IN-1 is a direct and wide HIV-1 Nef antagonist with an IC50 of 100-300 nM for wild-type HIV-1 replication.

Delavirdine is a non-nucleoside reverse transcriptase inhibitor (NNRTI). Delavirdine is part of Highly Active Antiretroviral Therapy (HAART), which can be used to treat human immunodeficiency virus (HIV) type 1.

Nevirapine-d3 is a deuterated compound of Nevirapine. Nevirapine has a CAS number of 129618-40-2. Nevirapine is a benzodiazepine non-nucleoside reverse transcriptase inhibitor. In combination with other antiretroviral drugs, nevirapine reduces HIV viral loads and increases CD4 counts, thereby retarding or preventing the damage to the immune system and reducing the risk of developing AIDS.

AZT triphosphate (3'-Azido-3'-deoxythymidine-5'-triphosphate) tetraammonium is an active triphosphate metabolite of Zidovudine (AZT). AZT triphosphate tetraammonium exhibits antiretroviral activity and inhibits replication of HIV . AZT triphosphate tetraammonium also inhibits the DNA polymerase of HBV . AZT triphosphate tetraammonium activates the mitochondria-mediated apoptosis pathway [1] [2] [3] .

AG 555 (Tyrphostin B46) is an EGFR tyrosine kinase inhibitor.

3β-Hydroxy-27-p-Z-coumaroyloxyurs-12-en-28-oic acid (compound 8) is a triterpene ester HIV-1 protease inhibitor with potential for use in antiretroviral combination therapy for AIDS.

AZT triphosphate TFA (3'-Azido-3'-deoxythymidine-5'-triphosphate TFA) is a active triphosphate metabolite of Zidovudine (AZT). AZT triphosphate TFA exhibits antiretroviral activity and inhibits replication of HIV. AZT triphosphate TFA also inhibits the DNA polymerase of HBV. AZT triphosphate TFA activates the mitochondria-mediated apoptosis pathway[1][2][3]. Treatment with 100 μM Zidovudine (AZT) for 48h disrupts the mitochondrial tubular network via accumulation of AZT triphosphate (AZT-TP) in H9c2 cells. AZT triphosphate accumulation causes downregulation of Opa1 and upregulation of Drp1. AZT triphosphate causes mitochondrial dysfunction, increases the production of cytotoxic reactive oxygen species (ROS), and impairs the balance of the mitochondrial quality control system in H9c2 cell model established from rat embryonic myoblasts[1]. [1]. Ryosuke Nomura, et al. Azidothymidine-triphosphate Impairs Mitochondrial Dynamics by Disrupting the Quality Control System. Redox Biol. 2017 Oct;13:407-417. [2]. Takeya Sato, et al. Engineered Human tmpk/AZT as a Novel Enzyme/Prodrug Axis for Suicide Gene Therapy. Mol Ther. 2007 May;15(5):962-70. [3]. K Y Hostetler, et al. Enhanced Oral Absorption and Antiviral Activity of 1-O-octadecyl-sn-glycero-3-phospho-acyclovir and Related Compounds in Hepatitis B Virus Infection, in Vitro. Biochem Pharmacol. 1997 Jun 15;53(12):1815-22.

2',3'-Dideoxyadenosine is an inhibitor of HIV replication, exhibiting antiretroviral activity and antiviral efficacy [1].