首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis and biological evaluation of conformationally flexible as well as restricted dimers of monastrol and related dihydropyrimidones.
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Synthesis and biological evaluation of conformationally flexible as well as restricted dimers of monastrol and related dihydropyrimidones.

机译:合成和生物学评估构型柔性以及单体和相关二氢嘧啶酮的受限二聚体。

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摘要

A series of conformationally flexible and restricted dimers of monastrol as well as related dihydropyrimidones have been synthesized by employing one-pot Biginelli multicomponent reaction. These dimers have been evaluated for cytotoxic potency against selected human cancer cell lines and some of the compounds have exhibited more cytotoxic potency than the parent monastrol. Further, the DNA binding ability by thermal denaturation studies and antimicrobial activities of these compounds are also discussed.
机译:通过采用一锅Biginelli多组分反应合成了一系列Monastrol构象灵活和受限制的二聚体以及相关的二氢嘧啶酮。已经评估了这些二聚体对选定的人类癌细胞系的细胞毒性潜能,并且某些化合物比亲代monastrol具有更高的细胞毒性潜能。此外,还讨论了通过热变性研究得到的DNA结合能力以及这些化合物的抗菌活性。

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