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Anti-AIDS agents 72. Bioisosteres (7-carbon-DCKs) of the potent anti-HIV lead DCK. 2007
Yang Wang, and
Shao-Xu Huang, and
Peng Xia, and
Yi Xia, and
Zheng-Yu Yang, and
Nicole Kilgore, and
Susan L Morris-Natschke, and
Kuo-Hsiung Lee
Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai 200032, China.
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.
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