Synthesis and Anti-cancer Activity of 1,3,4-Thiadiazole and 1,3-Thiazole Derivatives Having 1,3,4-Oxadiazole Moiety

被引:83
作者
Dawood, Kamal M. [1 ]
Gomha, Sobhi M. [1 ]
机构
[1] Cairo Univ, Fac Sci, Dept Chem, Giza 12613, Egypt
关键词
ANTIMICROBIAL EVALUATION; BIOLOGICAL EVALUATION; TUBULIN POLYMERIZATION; ANTITUMOR-ACTIVITY; ANTICONVULSANT; CYTOTOXICITY; HETEROCYCLES; PRODUCTS; UTILITY;
D O I
10.1002/jhet.2250
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Reaction of 1,3,4-oxadiazolyl-phenylthiourea 3 with hydrazonoyl halides gave the corresponding 1,3,4-oxadiazolylimino-1,3,4-thiadiazoles. Also, treatment of 3 with ethyl chloroacetate and -haloketones afforded the corresponding thiazolidinone and thiazole derivatives, respectively. The structures of the synthesized products were confirmed by spectral data. Ten compounds were evaluated for their anti-cancer activity against the colon carcinoma cell line (HCT-116). The results revealed that 1,3,4-thiadiazole derivatives 13d and 19c (IC50=0.73 and 0.86 mu g/mL, respectively) have promising antitumor activity against colon carcinoma (HCT-116), and most of the tested compounds showed moderate anti-cancer activity.
引用
收藏
页码:1400 / 1405
页数:6
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