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通过点击化学方便地合成具有潜在抗癌活性的新型吉帕伐林类似物。

Convenient synthesis of novel geiparvarin analogs with potential anti-cancer activity via click chemistry.

机构信息

Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, No 325, Guohe Road, Shanghai 200433, China.

出版信息

Eur J Med Chem. 2012 Jul;53:356-63. doi: 10.1016/j.ejmech.2012.04.026. Epub 2012 Apr 26.

Abstract

Based on the advantages of natural products in new anti-cancer drug development, we synthesized a series of novel benzopyran-4-one derivatives and evaluated their in vitro anti-cancer activities. The bioassays showed that the majority of the resultant compounds exerted anti-tumor effect against six human cancer cell lines to various extents, which supported the rationale of the design. Compound 5s exhibited highest potency of all the synthesized compounds.

摘要

基于天然产物在新型抗癌药物开发中的优势,我们合成了一系列新型苯并吡喃-4-酮衍生物,并评估了它们的体外抗癌活性。生物测定结果表明,大多数所得化合物对六种人癌细胞系均表现出不同程度的抗肿瘤作用,这支持了设计的合理性。化合物 5s 表现出所有合成化合物中最高的活性。

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