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

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.

SUBMITTER: Wang Y

PROVIDER: S-EPMC2697499 | biostudies-literature | 2007 Aug

REPOSITORIES: biostudies-literature

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

Wang Yang Y Huang Shao-Xu SX Xia Peng P Xia Yi Y Yang Zheng-Yu ZY Kilgore Nicole N Morris-Natschke Susan L SL Lee Kuo-Hsiung KH

Bioorganic & medicinal chemistry letters 20070516 15

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 deve ...[more]

PMID: 17533128

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