Abstract

A new library of 6-(pyridin-4-yl)imidazo[2,1-b][1,3]thiazole derivatives (11a–11j) containing an isoxazole ring linked to C³ through a p-phenylene spacer was designed, synthesized, and tested for their in vitro anticancer activity against four human cancer cell lines, including PC3 and DU-145 (prostate cancer), A549 (lung cancer), and MCF-7 (breast cancer) by using MTT assay with etoposide as positive control. Among them, five compounds displayed more potent anticancer activity, and those bearing 3,4,5-trimethoxyphenyl and pyridin-4-yl substituents on C³ of the isoxazole ring showed most promising activity.

中文翻译：

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含异恶唑环6-(吡啶-4-基)咪唑并[2,1-b][1,3]噻唑衍生物的合成及抗癌评价

摘要

设计了一个新的 6-(吡啶-4-基)咪唑并[2,1- b ][1,3]噻唑衍生物库 ( 11a–11j )，其中包含通过对亚苯基间隔基与 C ³连接的异恶唑环，合成并以依托泊苷为阳性的 MTT 法测试了其对四种人类癌细胞系的体外抗癌活性，包括 PC3 和 DU-145（前列腺癌）、A549（肺癌）和 MCF-7（乳腺癌）控制。其中，5种化合物表现出更强的抗癌活性，其中异恶唑环C ³上带有3,4,5-三甲氧基苯基和吡啶-4-基取代基的化合物表现出最有希望的活性。