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

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• 作者：Yang Wang ; Shao-Xu Huang ; Peng Xia ; Yi Xia ; Zheng-Yu Yang ; Nicole Kilgore ; Susan L. Morris-Natschke ; Kuo-Hsiung Lee
• 关键词：Anti-HIV activity ; DCK ; Bioisostere
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2007
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：1 August 2007
• 卷：17
• 期：15
• 页码：4316-4319
• 文件大小：225 K

摘要

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 EC₅₀ value of 0.068 μM, 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.