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

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

  • Bioorg Med Chem Lett. 2007 Aug 1;17(15):4316-9. doi: 10.1016/j.bmcl.2007.05.026.
Yang Wang 1,  Shao-Xu Huang,  Peng Xia,  Yi Xia,  Zheng-Yu Yang,  Nicole Kilgore,  Susan L Morris-Natschke,  Kuo-Hsiung Lee
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai 200032, China.
PMID: 17533128 DOI: 10.1016/j.bmcl.2007.05.026
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.

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