|Description||Among CDKs, CDK9 is a validated pathological target in HIV infection, inflammation and cardiac hypertrophy; however selective CDK9 inhibitors are still not available. We present a selective inhibitor family of CDK9 based on the 4-phenylamino-6- phenylpyrimidine nucleus. We show a convenient synthetic method to prepare a useful intermediate and its derivatisation resulting in novel compounds. The CDK9 inhibitory activity of the derivatives was measured in specific kinase assay and the CDK inhibitory profile of the best ones (IC50 > 100nM) was determined. The most selective compounds had high selectivity over CDK1, 2, 3, 5, 6, 7 and showed at least one order of magnitude higher inhibitory activity over CDK4 inhibition. The most selective molecules were examined in cytotoxicity assays and their ability to inhibit HIV-1 replication was determined in cellular assays.|
Raltegravir is a potent, selective, and orally bioavailable inhibitor of HIV integrase (IC50 = 15 nM). It is metabolized primarily by uridine diphosphate glucur...
Tenofovir(GS 1278, PMPA) is an antiretroviral drug known as nucleotide analogue reverse transcriptase inhibitors (NRTIs), which block reverse transcriptase, a c...
BMS-488043 is a small-molecule HIV fusion inhibitor.
Lopinavir is a potent HIV protease inhibitor with Ki of 1.3 pM.
Tenofovir hydrate reduces the viral cytopathic effect of HIV-1(IIIB), HIV-2(ROD) and HIV(EHO) with EC50 of 1.15 μg/mL, 1.12 μg/mL and 1.05 μg/mL in MT-4 cells. ...
PNU-104489, a sulfonamidoindol derivative, has been found to be a HIV-1 specific inhibitor and was proved to exhibit activity against BHA-P-resistant HIV-1MF ha...
A selective HIV protease inhibitor. Antiviral.
Fosamprenavir Calcium Salt
HIV protease inhibitor; water soluble prodrug of amprenavir.
BMS585248 is a highly potent and novel human immunodeficiency virus type 1 (HIV-1) attachment inhibitor with 4-fluoro-6-azaindole core heterocycles. It targets ...
BMS-663068 tris is an HIV-1 attachment inhibitor in development for the treatment of HIV-1 infection.
BMS-663749 is HIV-1 attachment inhibitor.
Censavudine is a nucleoside reverse transcriptase inhibitor. It is active against HIV resistant to both abacavir and tenofovir. It is a candidate for people wit...
Lamivudine is a potent nucleoside analog reverse transcriptase inhibitor, used for treatment of chronic HBV and HIV/AIDS.
Delavirdine is a non-nucleoside reverse transcriptase inhibitor (NNRTI). It is used as part of highly active antiretroviral therapy (HAART) for the treatment of...
NBD-557 is a N-phenyl-N'-(2,2,6,6-tetramethyl-piperidin-4-yl)-oxalamide analog, a novel class of human immunodeficiency virus type 1 (HIV-1) entry inhibitors th...
Tenofovir blocks reverse transcriptase and hepatitis B virus infections.
Gomisin G, carboxylic acid with additional oxygen functions, exhibited the most potent anti-HIV activity with EC50 and therapeutic index (TI) values of 0.006 mi...
Bevirimat, also known as MPC-4326 and PA-457, is an anti-HIV drug derived from a betulinic acid-like compound, first isolated from Syzygium claviflorum, a Chine...
Indinavir is a member of the novel hydroxyaminopentane amide class of HIV-1 protease inhibitors. Indinavir is used as an antiviral.
Ebselen, also known as SPI-1005, is an organoselenium compound with potential anti-oxidant, anti-inflammatory and cytoprotective activity. Upon oral administra...