The enone motif of (+)-grandifloracin is not essential for 鈥榓nti-austerity鈥?antiproliferative activity

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• 作者：Monika Ali Khan^a ; Pauline J. Wood^b ; Natasha M. Lamb-Guhren^a ; Lorenzo Caggiano^b ; Gabriele Kociok-Kö ; hn^c ; David Tosh^d ; Simon E. Lewis^a ; ^{S.E.Lewis@bath.ac.uk" class="auth_mail}
• 关键词：Antiproliferative ; Pancreatic cancer ; Analogue synthesis ; Natural products ; Organoiron chemistry
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：1 July 2014
• 年：2014
• 卷：24
• 期：13
• 页码：2815-2819
• 全文大小：1015 K

文摘

We report the synthesis and biological evaluation of three analogues of the natural product (+)-grandifloracin (+)-1. All three analogues exhibit enhanced antiproliferative activity against PANC-1 and HT-29 cells compared to the natural product. The retention of activity in an analogue lacking the enone functional group, 9, implies this structural element is not an essential part of the (+)-grandifloracin pharmacophore.