化学
前列腺癌
立体化学
体外
体内
癌症研究
细胞生长
生长抑制
生物活性
效力
LNCaP公司
癌细胞
细胞培养
化学合成
DU145型
结构-活动关系
药理学
IC50型
组合化学
癌症
生物化学
作者
Lixin Qiao,Lian Yun Zhao,Rong Suobao,Xiong Wu Wu,Shaomeng Wang,Teruhiko Fujii,Marcelo G. Kazanietz,Laura Rauser,Jason E. Savage,Bryan L. Roth,Judith L. Flippen-Anderson,Alan P. Kozikowski
标识
DOI:10.1016/s0960-894x(01)00097-x
摘要
Abstract In view of its role in tumor promotion and signal transduction, protein kinase C (PKC) has proven to be an exciting target for cancer therapy. With the aid of molecular modeling, we rationally designed and stereoselectively synthesized a new class of rigidified pyrrolidone-based PKC activators. Pyrrolidone 15 was found to exhibit reasonable affinity for PKCδ, with lower affinity for the other isozymes tested. Pyrrolidone Figure 1 , Scheme 1 causes the dose-dependent induction of apoptosis in LNCaP prostate cancer cells. This apoptotic effect could be markedly potentiated by the use of LNCaP cells overexpressing the PKCα or δ isozymes.
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