Synthesis and anti-integrase evaluation of novel calix[4]arene derivatives containing the triazolyl 1,3-diketo moiety
Synthesis and anti-integrase evaluation of novel calix[4]arene derivatives containing the triazolyl 1,3-diketo moiety
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含有三唑基1,3-二酮部分的新型杯[4]芳烃衍生物的合成和抗整合酶评价
DOI：
10.1016/j.cclet.2014.03.012
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发表时间：
2014-05-01
影响因子：
9.1
通讯作者：
He, Hong-Qiu
中科院分区：
文献类型：
--
作者：
Luo, Zai-Gang;Zhao, Yu;He, Hong-Qiu
合成了一系列新型的杯[4]芳烃衍生物，并对其进行了HIV整合酶抑制活性的筛选。这些化合物的化学结构通过H-1 NMR、C-13 NMR和ESI-MS进行了确认。初步的生物测定表明，杯[4]芳烃衍生物比对叔丁基杯[4]芳烃衍生物具有更高的活性。特别是化合物4g表现出最强的整合酶链转移抑制活性，其IC 50值为6.1 μ mol/L。(C)2014年，罗在刚和徐雪梅。Elsevier B. V.代表中国化学会出版。All rights reserved.
A series of novel calix[4]arene derivatives incorporating two triazolyl 1,3-diketo subunits in alternate positions at the lower rim were synthesized and screened for HIV integrase inhibition activity. The chemical structures of these compounds were confirmed by means of H-1 NMR, C-13 NMR, and ESI-MS. Preliminary bioassays indicated that calix[4]arene derivatives proved to be more active than p-tert-butylcalix[4]arene derivatives. In particular, compound 4g presented the most potent integrase strand transfer inhibitory activity with an IC50 value of 6.1 mu mol/L. (C) 2014 Zai-Gang Luo and Xue-Mei Xu. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.