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Synthesis and anticancer activity of some new series of 1, 4-dihydropyridine derivatives

机译:一些新的1,4,二氢吡啶衍生物系列的合成及其抗癌活性

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摘要

A series of 1,4-dihydropyridine derivatives 1a-c have been prepared from 4-substituted aromatic aldehyde, ethyl acetoacetate and ammonium hydroxide following Hantzsch method. The compounds 1a-c have been reacted with semicarbazidc to give the compounds 2a-c. The compounds 1a-c have been reacted with thiosemicarbazide to give the compounds 3a-c. The structures of synthesized compounds are confirmed by IR, ~1H and ~(13)C NMR, mass spectrometry and elemental analyses. The newly synthesized compounds have been screened for preliminary anti-cancer activity against HepG2 (Liver), Hela (Cervical) and MCF-7 (Breast) cancer cells. The compound 2a is highly active against HepG2, MCF-7 and 3a is highly active against Hela (Cervical) and these have been selected for advanced preclinical development.
机译:按照Hantzsch方法,由4-取代的芳族醛,乙酰乙酸乙酯和氢氧化铵制备了一系列的1,4-二氢吡啶衍生物1a-c。使化合物1a-c与氨基脲反应,得到化合物2a-c。使化合物1a-c与硫代氨基脲反应,得到化合物3a-c。合成的化合物的结构通过IR,〜1H和〜(13)C NMR,质谱和元素分析确定。已经筛选了新合成的化合物针对HepG2(肝),Hela(宫颈)和MCF-7(乳腺癌)癌细胞的初步抗癌活性。化合物2a对HepG2具有高活性,MCF-7和3a对Hela(宫颈)具有高活性,因此已选择这些化合物用于高级临床前开发。

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