1447696-83-4Relevant academic research and scientific papers
Efficient construction of novel D-ring modified steroidal dienamides and their cytotoxic activities
Yu, Bin,Shi, Xiao-Jing,Ren, Jing-Li,Sun, Xiao-Nan,Qi, Ping-Ping,Fang, Yuan,Ye, Xian-Wei,Wang, Meng-Meng,Wang, Jun-Wei,Zhang, En,Yu, De-Quan,Liu, Hong-Min
, p. 171 - 179 (2013)
Two series of steroidal dienamides 4a-q and 5a-f were designed, synthesized and evaluated for cytotoxic activities against five human cancer cell lines (MGC-803, EC109, PC-3, SMMC-7721 and MCF-7). The protocol developed efficiently achieved the construction of carbon ecarbon double bond and selective conversion of nitrile group into carboxamide in one-pot procedure. Besides, compounds 4a-q and 5a-f showed moderate to excellent cytotoxic activities with the IC 50 values ranging from 0.1 to 40 μM and most of them were more potent than 5-fluorouracil. Particularly, four compounds 4d, 4-, 4q and 5a showed excellent selectivity against MGC-803 with the IC50 values less than 1 mM. Flow cytometry analysis demonstrated that compound 4c caused the cellular early apoptosis and cell cycle arrest in G2/M phase in a concentration-independent manner.
