Bioorganic and Medicinal Chemistry Letters p. 955 - 959 (2001)
Update date:2022-08-02
Topics:
Qiao, Lixin
Zhao, Lian-Yun
Rong, Suo-Bao
Wu, Xiong-Wu
Wang, Shaomeng
Fujii, Teruhiko
Kazanietz, Marcelo G
Rauser, Laura
Savage, Jason
Roth, Bryan L
Flippen-Anderson, Judith
Kozikowski, Alan P
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 2 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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