Ophiobolin C inhibits CCR5 binding to the envelop protein gp120 and CD4, which is responsible for mediating the entry of HIV-1 into cells[1]. Ophiobolin C is also cytotoxic to chronic lymphocytic leukemia cells[2].
Interiotherin A is a lignan with a dibenzocyclooctadiene skeleton isolated from Kadsura interior. Interiotherin A inhibits HIV replication to exhibit anti-HIV activity, it has a role as a metabolite and an anti-HIV agent[1].
HIV-1 inhibitor-20 is a potent HIV-1 inhibitor by non-classical isosteric replacement of amide to 1,2,4-oxadiazoles[1].
Elvitegravir is an HIV integrase inhibitor for HIV-1IIIB, HIV-2EHO and HIV-2ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM, respectively.
GLR-19 is an anti-HIV peptide. GLR-19 also has antiviral activity against HSV-2[1][2].
Fipravirimat is a potent HIV-1 inhibitor. Fipravirimat has the potential for HIV and AIDS research[1].
Inosine pranobex is a potent, broad-spectrum antiviral compound for HIV infection. Inosine pranobex is an immunopotentiator[1].
1-Deoxymannojirimycin hydrochloride is a selective class I α1,2-mannosidase inhibitor with an IC50 of 20 μM. 1-Deoxymannojirimycin hydrochloride is also a N-linked glycosylation inhibitor and inhibits HIV‐1 strains. 1-Deoxymannojirimycin hydrochloride has antiviral activity[1][2].
Tipranavir-d4 (PNU-140690-d4) is the deuterium labeled Tipranavir. Tipranavir (PNU-140690) inhibits the enzymatic activity and dimerization of HIV-1 protease, exerts potent activity against multi-protease inhibitor (PI)-resistant HIV-1 isolates with IC50s of 66-410 nM[1][2]. Tipranavir inhibits SARS-CoV-2 3CLpro activity[3].
Salicylanilide demonstrates a wide range of biological activities including antiviral potency which can inhibit HIV virus by targeting HIV-1 integrase or reverse transcriptase.
Azt-pmap, a nucleoside analogue, is an aryl phosphate derivative of AZT. Azt-pmap shows anti-HIV activity[1]. AZT is a nucleoside reverse transcriptase inhibitor (NRTI) for HIV infection[2].
Tenofovir hydrate is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B.
LDC4297 hydrochloride is a selective inhibitor of CDK7 with an IC50 value of 0.13 nM. LDC4297 hydrochloride inhibits human cytomegalovirus (HCMV) replication with an EC50 value of 24.5 nM. LDC4297 hydrochloride shows broad antiviral activities to Herpesviridae, Adenoviridae, Poxviridae, Retroviridae and Orthomyxoviridae with EC50 values of 0.02-1.21 μM. LDC4297 hydrochloride can be used for the research of infection[1].
Sparstolonin B acts as a selective TLR2 and TLR4 antagonist and selectively blocks TLR2- and TLR4-mediated inflammatory signaling. Sparstolonin B has anti-HIV and anticancer activities[1][2].
BMS-585248 is a potent, third-generation HIV-1 attachment inhibitor with a promising initial in vitro and in vivo pharmacokinetic profile[1].
Ro24-7429 is a potent and orally active HIV-1 transactivator protein Tat antagonist. Ro24-7429 is also a runt-related transcription factor 1 (RUNX1) inhibitor. Ro24-7429 has anti-HIV, antifibrotic and anti-inflammatory effects[1][2].
DENV-IN-7, a flavone analog, is a dengue virus (DENV) inhibitor with an EC50 value of 70 nM. DENV-IN-7 has low toxicity against normal cell and anti-dengue activity[1].
Tenofovir-C3-O-C12-trimethylsilylacetylene (ammonium) exhibits substantially longer t1/2 values than tenofovir in human liver microsomes, potent anti-HIV activity in vitro, and enhances pharmacokinetic properties in vivo.
Cosalane (NSC 658586) is a potent inhibitor of HIV replication. Cosalane has an intrinsic ability to block human and murine CCR7 function in vitro in response to both of its natural ligands, CCL19 and CCL21, with the IC50 of 0.207/2.66 μM in human for CCL19/CCL21 and 0.193/1.98 μM in murine, respectively[1][2].
HIV-1 inhibitor-10 is a nanomolar HIV-1 maturation inhibitor.
HIV-1 integrase inhibitor 4 is a HIV-1 integrase strand transfer (INST) inhibitor with an IC50 of 3.7 nM.
Isoapetalic acid (compound 4) is a potent anti-HIV agent[1].
Tifuvirtide (T-1249) is a peptide human immunodeficiency virus type-1 (HIV-1) fusion inhibitor. Tifuvirtide is a synthetically designed hybrid retroviral envelope polypeptide. Tifuvirtide has antiretroviral activity. Tifuvirtide can be used for the research of HIV infection[1].
Emtricitabine triphosphate ((-)-Emtricitabine triphosphate) is the phosphorylated anabolite of Emtricitabine (HY-17427). Emtricitabine is a nucleoside reverse transcriptase inhibitor. Emtricitabine is antiretroviral agent for HIV and HBV infection[1][2].
2-Hydroxycinnamic acid is isolated from the methanol extract of Cinnamomum cassia. 2-Hydroxycinnamic acid shows inhibitory effects on infection of HIV/SARS-CoV S pseudovirus with an IC50 of 0.3 mM[2]
Zinlirvimab is a humanized IgG1-λ2, HIV neutralising antibody targeting to HIV-1 gp120 envelope glycoprotein (IIIB gp120 V3 loop)[1][2].
Nelfinavir(AG-1341) is a potent and orally bioavailable human immunodeficiency virus HIV-1 protease inhibitor (Ki=2 nM) and is widely prescribed in combination with HIV reverse transcriptase inhibitors for the treatment of HIV infection. IC50 Valur: 2 nM (Ki for HIV-1 protease) [2]Target: HIV Proteasein vitro: In vitro exposure (72 hours) of HAECs to NEL (0.25-2 μg/mL) decreased both basal (2.5-fold) and insulin-induced NO production (4- to 5-fold). NEL suppressed insulin-induced phosphorylation of both Akt and eNOS at serine residues 473 and 1177, respectively. NEL decreased tyrosine phosphorylation of IR-β, IRS-1, and PI3K. Coexposure to troglitazone (TRO; 250 nM) ameliorated the suppressive effects of NEL on insulin signaling and NO production. Coexposure to TRO also increased eNOS expression in NEL-treated HAECs [1]. AG1343 is a potent enzyme inhibitor (Ki = 2 nM) and antiviral agent (HIV-1 ED50 = 14 nM). An X-ray cocrystal structure of the enzyme-AG1343 complex reveals how the novel thiophenyl ether and phenol-amide substituents of the inhibitor interact with the S1 and S2 subsites of HIV-1 protease, respectively [2].in vivo: In vivo studies indicate that AG1343 is well absorbed orally in a variety of species and possesses favorable pharmacokinetic properties in humans [2].
L-739594 is a HIV-1 protease inhibitor, with an IC50 of 1.8 nM[1].
Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV.
PKF050-638 is a potent and selective inhibitor of HIV-1 Rev (IC50=0.04 μM). PKF050-638 inhibits the CRM1-mediated Rev nuclear export by disrupting CRM1-NES interaction[1].