Anti-AIDS Agents. 33. Synthesis and Anti-HIV Activity of Mono-methyl Substituted 3',4'-di-O-(-)-camphanoyl-(+)-cis-khellactone (DCK) Analogues

Overview

Journal Bioorg Med Chem Lett

Specialty Biochemistry

Date 1999 Jan 5

PMID 9873504

Citations 10

Authors

L Xie

Y Takeuchi

L M Cosentino

K H Lee

Affiliations

Soon will be listed here.

Abstract

Four isomeric methyl substituted DCK analogues (2-5) were asymmetrically synthesized from different starting materials. 3-Methyl, 4-methyl, and 5-methyl-3',4'-di-O-(-)-camphanoyl-(+)-cis-khellactone (2-4) all were extremely potent against HIV-1 replication in H9 lymphocyte cells with EC50 and therapeutic index values of < 4.23 x 10(-7) microM and > 3.72 x 10(8), respectively, which are much better than those of DCK and AZT in this assay.

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