Monastrol模拟Biginelli二氢嘧啶衍生物的合成、对HepG2和HeLa细胞株的细胞毒性筛选及分子模拟研究

Uttara Soumyanarayanan, Varadaraj G Bhat, Sidhartha S Kar, Jesil A Mathew
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引用次数: 35

摘要

合成了monastrol的结构类似物Biginelli二氢嘧啶衍生物,monastrol是一种已知的人类激酶Eg5抑制剂。采用MTT法测定合成的化合物对人肝细胞癌和人上皮癌细胞增殖的IC50值。分子对接研究使化合物与monastrol的结构活性关系有了更清晰的认识。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

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Monastrol mimic Biginelli dihydropyrimidinone derivatives: synthesis, cytotoxicity screening against HepG2 and HeLa cell lines and molecular modeling study.

Biginelli dihydropyrimidinone derivatives as structural analogs of monastrol, a known human kinesin Eg5 inhibitor, were synthesized. IC50 values of the synthesized compounds against the proliferation of human hepatocellular carcinoma and human epithelial carcinoma cell lines were determined through MTT assay. Molecular docking study gave a clear insight into the structural activity relationship of the compounds in comparison with monastrol.

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