Chinese Journal of Organic Chemistry >
Synthesis and Antiproliferative Activity of Novel 1,3,4-Thiadiazole Derivatives
Received date: 2015-07-29
Revised date: 2015-09-13
Online published: 2015-10-23
Twenty eight novel 1,3,4-thiadiazole derivatives were synthesized using different phenylacetic acids as the starting material, followed by the reaction of cyclization, coupling, deprotection, and finally introduced different substituted benzenesulfonamides. The structures of all target compounds were identified by 1H NMR, 13C NMR and HRMS. The biological evaluation was performed on PC-3 (prostatic cancer cell), MDA-MB-231 (breast cancer cell) and K562 (chronic myelogenous leukemia cell) by 3-(4,5-dimethylthigal-2-yl)-2,5-(diphenyltetragalium) bromide (MTT) assay. The results suggested that some compounds exhibited good anti-proliferative activities against tumor cell lines. Especially, compounds 6a and 6b showed similar inhibitory activities against K562 cell compared with gossypol.
Key words： thiadiazole; anticancer activity; synthesis
Liu Tingting , Wan Yichao , Fang Hao . Synthesis and Antiproliferative Activity of Novel 1,3,4-Thiadiazole Derivatives[J]. Chinese Journal of Organic Chemistry, 2016 , 36(2) : 417 -424 . DOI: 10.6023/cjoc201507038
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