Lipase-catalyzed preparation of chromomycin A₃ analogues and biological evaluation for anticancer activity

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• 作者：Javier Gonzá ; lez-Sabí ; n^a ; Luz Elena Nú ; ñ ; ez^a ; Nuria Mené ; ndez^a ; Alfredo F. Brañ ; a^b ; Carmen Mé ; ndez^b ; José ; A. Salas^b ; Vicente Gotor^c ; Francisco Morí ; s^a ; ^{fmv@entrechem.com}
• 关键词：Chromomycin A3 ; Aureolic acid ; Lipase ; Enzymatic catalysis ; Regioselective acylation
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：1 July, 2012
• 卷：22
• 期：13
• 页码：4310-4313
• 文件大小：444 K

摘要

Several acyl derivatives of the aureolic acid chromomycin A₃ were obtained via lipase-catalyzed acylation. Lipase B from Candida antarctica (CAL-B) was found to be the only active biocatalyst, directing the acylation regioselectively towards the terminal secondary hydroxyl group of the aglycone side chain. All new chromomycin A₃ derivatives showed antitumor activity at the micromolar or lower level concentration. Particularly, chromomycin A₃ 4鈥?vinyladipate showed 3-5 times higher activity against the four tumor cell lines assayed as compared to chromomycin A₃.