Abstract

Reactions of 5-(1,3-benzothiazol-2-yl)furan-2-carbaldehyde with 2-acetylfuran, 2-acetylthiophene, and some compounds containing an active methylene group gave a number of new 3-[5-(1,3-benzothiazol-2-yl)furan-2-yl]-1-(furan- or thiophen-2-yl)prop-2-en-1-one, 3-[5-(1,3-benzothiazol-2-yl)furan-2-yl]acrylonitrile, 3-[5-(1,3-benzothiazol-2-yl)furan-2-yl]-2-cyanoacrylamide, and 5-{[5-(1,3-benzothiazol-2-yl)furan-2-yl]methylidene}-2-sulfanylidene-1,3-thiazolidin-4-one derivatives. 5-{[5-(1,3-Benzothiazol-2-yl)furan-2-yl]methylidene}-2-(morpholin-4-yl)-1,3-thiazol-4-one and diethyl 4-[5-(1,3-benzothiazol-2-yl)furan-2-yl]-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate were synthesized by multicomponent reactions involving the title compound. Antitumor screening of the synthesized 5-(1,3-benzothiazol-2-yl)furan-2-carbaldehyde derivatives revealed a lead compound, 3-[5-(1,3-benzothiazol-2-yl)furan-2-yl]-2-(4-phenyl-1,3-thiazol-2-yl)prop-2-enenitrile, which proved to be superior to 5-fluorouracil, cisplatin, and curcumin taken as reference drugs.

中文翻译：

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设计抗肿瘤药中的5-（1,3-苯并噻唑-2-基）呋喃-2-甲醛

摘要

5-（1,3-苯并噻唑-2-基）呋喃-2-甲醛与2-乙酰基呋喃，2-乙酰基噻吩和一些含有活性亚甲基的化合物的反应产生了许多新的3- [5-（1， 3-苯并噻唑-2-基呋喃-2-基] -1-（呋喃或噻吩-2-基）丙-2-烯-1-酮，3- [5-（1,3-苯并噻唑-2 -基）呋喃-2-基]丙烯腈，3- [5-（1,3-苯并噻唑-2-基）呋喃-2-基] -2-氰基丙烯酰胺和5-{[5-（1,3-苯并噻唑-2-基）呋喃-2-基]亚甲基} -2-亚磺酰基-1，3-噻唑烷酮-4-一衍生物。5-{[5-（1,3-苯并噻唑-2-基）呋喃-2-基]亚甲基} -2-（吗啉-4-基）-1,3-噻唑-4-酮和二乙基4- [通过涉及标题化合物的多组分反应合成了5-（1,3-苯并噻唑-2-基）呋喃-2-基] -2,6-二甲基-1,4-二氢吡啶-3,5-二羧酸酯。合成的5-（1，