Synthesis, cytotoxicity and protein kinase C inhibition of arylpyrrolylmaleimides.
A series of novel arylpyrrolylmaleimides was synthesized and evaluated for their in-vitro cytotoxicity against various human cancer cell lines and their protein-kinase C inhibitory activity. Some of the compounds showed high or moderate cytotoxic activity against the tested cell lines. Compound 6b is the most promising compound against the tested cancer cell lines; 6d and 6e showed moderate protein-kinase C inhibition. Structure-activity relationships are discussed based on the experimental data obtained.
Xu
Gui-Qing
GQ
ZJU-ENS Joint Laboratory of Medicinal Chemistry, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, China.
Zhang
Chong
C
Zhang
Lei
L
Zhou
Xing-Lu
XL
Yang
Bo
B
He
Qiao-Jun
QJ
Hu
Yong-Zhou
YZ
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D006801:Humans; D008301:Maleimides / Q000138:chemical synthesis* / Q000494:pharmacology; D011493:Protein Kinase C / Q000037:antagonists & inhibitors*; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology
D000970:Antineoplastic Agents; D008301:Maleimides; D047428:Protein Kinase Inhibitors; D011493:Protein Kinase C