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
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抗艾滋病药物 72. 有效抗 HIV 先导 DCK 的生物电子等排体（7-碳-DCK）
DOI：
10.1016/j.bmcl.2007.05.026
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发表时间：
2007-08-01
影响因子：
2.7
通讯作者：
Lee, Kuo-Hsiung
中科院分区：
文献类型：
--
作者：
Wang, Yang;Huang, Shao-Xu;Lee, Kuo-Hsiung
合成了三个9，10-二- O-（-）-胆酰基-7，8，9，10-四氢-苯并[h]色烯-2-酮（7-碳-DCK）类似物（3a-C），并评价了它们在H9淋巴细胞中对HIV-1复制的抑制作用。抗HIV先导化合物DCK的三个新碳生物电子等排体均显示出抗HIV活性。化合物3a具有0.068 pM的EC 50值，其在相同测定中与DCK相当。初步结果表明，7-碳-DCK类似物作为潜在的HIV-1抑制剂值得关注，以进一步开发为临床试验候选物。(c)2007爱思唯尔有限公司保留所有权利。
Three 9, 10-di- O-(-)-camphanoyl-7,8,9, 10-tetrahyd to -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 pM, 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. (c) 2007 Elsevier Ltd. All rights reserved.