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Synthesis of Some New Thiazole Derivatives and Their Cytotoxicity on Different Human Tumor Cell Lines

机译:不同人肿瘤细胞系中一些新的噻唑衍生物及其细胞毒性的合成

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摘要

Some novel 1-(inden-3-ylidene)-2-(thiazol-2-ylidene) hydrazine derivatives 3-9 were synthesized by the Hantzsch reaction of thiosemicarbazone derivatives 2a-2c with halo ketones and halo esters. Thiosemicarbazone derivatives reacted with hydrozonyl chlorides to give diazenyl-4-methylthiazole derivatives 11a-11d. Structures of the products were elucidated from IR, H-1, and C-13 NMR, and Mass spectra elucidate. The synthesized compounds were screened for their cytotoxicity against three human tumor cell lines. Twenty compounds showed high (= 60 %) antiproliferative activity over breast cancer (MCF-7). Compounds 2b, 3c, 4a, 4b, 6b, 6c, 7b, 8a, and 11b possessed higher cytotoxic activity over breast tumor cell line than Doxorubicin.
机译:通过HANESEDABAZONE衍生物2A-2C与卤素酮和卤素酯,合成了一些新的1-(INDEN-3- ylidene)-2-(噻唑-2- ylidene)肼衍生物3-9。 Thiosimearbazone衍生物与氢氯化物反应,得到二亚苯基-4-甲基噻唑衍生物11a-11d。 从IR,H-1和C-13 NMR释放产物的结构,并阐明质谱。 将合成的化合物筛选它们对三种人肿瘤细胞系的细胞毒性。 二十种化合物在乳腺癌(MCF-7)上显示出高(& = 60%)抗增殖活性(MCF-7)。 化合物2b,3c,4a,4b,6b,6c,7b,8a和11b在乳腺肿瘤细胞系上具有比多柔比星的细胞毒性更高。

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