Literature

Abstract

Three 9,10-di-O-(-)-camphanoyl-7,8,9,10-tetrahydro-benzo[h]chromen-2-one (7-carbon-DCK) analogs (3a-c) were synthesized and evaluated for inhibition of HIV-1 replication in H9 lymphocytes. All three new carbon bioisosteres of the anti-HIV lead DCK showed anti-HIV activity. Compound 3a had an EC(50) value of 0.068 microM, which was comparable to that of DCK in the same assay. The preliminary results indicated that 7-carbon-DCK analogs merit attention as potential HIV-1 inhibitors for further development into clinical trials candidates.

DOI： 10.1016/j.bmcl.2007.05.026

Anti-AIDS agents 72. Bioisosteres (7-carbon-DCKs) of the potent anti-HIV lead DCK

Bioorganic & Medicinal Chemistry Letters 2007.0

Anti-aids agents 33.1 Synthesis and anti-HIV activity of mono-methyl substituted 3′,4′-di-O-(−)-camphanoyl-(+)-cis-khellactone (DCK) analogues

Bioorganic & Medicinal Chemistry Letters 1998.0

Anti-AIDS agents. Part 58: Synthesis and anti-HIV activity of 1-thia-di-O-(−)-camphanoyl-(+)-cis-khellactone (1-thia-DCK) analogues

Bioorganic & Medicinal Chemistry Letters 2004.0

Anti-AIDS Agents. 42. Synthesis and Anti-HIV Activity of Disubstituted (3‘R,4‘R)-3‘,4‘-Di-O-(S)-camphanoyl-(+)-cis-khellactone Analogues

Journal of Medicinal Chemistry 2001.0

Anti-AIDS Agents. 52. Synthesis and Anti-HIV Activity of Hydroxymethyl (3‘R,4‘R)-3‘,4‘-Di-O-(S)-camphanoyl-(+)-cis-khellactone Derivatives

Journal of Medicinal Chemistry 2004.0

Anti-AIDS agents 84. Synthesis and anti-human immunodeficiency virus (HIV) activity of 2′-monomethyl-4-methyl- and 1′-thia-4-methyl-(3′R,4′R)-3′,4′-di-O-(S)-camphanoyl-(+)-cis-khellactone (DCK) analogs☆