Potent Farnesyltransferase Inhibitors with 1,4-Diazepane Scaffolds as Novel Destabilizing Microtubule Agents in Hormone-Resistant Prostate Cancer
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- 作者：Nicolas Wlodarczyk ; Delphine Le Broc-Ryckewaert ; Pauline Gilleron ; Ame虂lie Lemoine ; Amaury Farce ; Philippe Chavatte ; Joe虉lle Dubois ; Nicole Pommery ; Jean-Pierre He虂nichart ; Christophe Furman ; Re虂gis Millet
- 刊名：Journal of Medicinal Chemistry
- 出版年：2011
- 出版时间：March 10, 2011
- 年：2011
- 卷：54
- 期：5
- 页码：1178-1190
- 全文大小：1002K
- 年卷期：v.54,no.5(March 10, 2011)
- ISSN：1520-4804
文摘
A new class of potent farnesyltransferase inhibitors based on a 1,4-diazepane scaffold was synthesized with protein farnesyltransferase inhibition potencies in the low nanomolar range. The compounds block the growth on two hormone-resistant tumor prostatic cell lines (DU145 and PC3). The advanced cellular evaluation of the more potent farnesyltransferase inhibitors was explored and revealed a disorganization of tubulin in PC3 cells.