Bioorganic and Medicinal Chemistry p. 3989 - 3996 (2017)
Update date:2022-08-05
Topics:
Qu, Menghua
Liu, Zhihao
Zhao, Dan
Wang, Changyuan
Zhang, Jianbin
Tang, Zeyao
Liu, Kexin
Shu, Xiaohong
Yuan, Hong
Ma, Xiaodong
A class of sulfonamide-substituted diphenylpyrimidines (Sul-DPPYs) were synthesized to improve activity against the focal adhesion kinase (FAK). Most of these new Sul-DPPYs displayed moderate activity against the FAK enzyme with IC50 values of less than 100?nM; regardless, they could effectively inhibit several classes of refractory cancer cell lines with IC50 values of less than 10?μM, including the pancreatic cancer cell lines (AsPC-1, Panc-1 and BxPC-3), the NSCLC-resistant H1975 cell line, and the B lymphocyte cell line (Ramos cells). Results of flow cytometry indicated that inhibitor 7e promoted apoptosis of pancreatic cancer cells in a dose-dependent manner. In addition, it almost completely induced the apoptosis at a concentration of 10?μM. Compound 7e may be selected as a potent FAK inhibitor for the treatment of pancreatic cancer.
View MoreXinji City Taida Sinopec Co., Ltd.
Contact:0086-311-85341278
Address:No.6, Nanhua Road,Xinji City Road,Hebei Province,China
Longhui qunfeng Chemical Co., Ltd
Contact:86-731-82173407
Address:South-east Industrial Park, Longhui County, Hunan Province, China
NEW FORTUNE INDUSTRIAL CO.,LTD.
website:http://newfortune.lookchem.com/
Contact:+86-25-8645-9456
Address:C4-105 GREEN ISLAND FLOWER TOWN
Wuhan Jadechem International Trade Co.,Ltd.
website:http://www.jadechem-intl.com
Contact:+86-27-83527060
Address:Room 502,Building C11,Software new city No.8,Huacheng Avenue,East Lake High-tech development zone,Wuhan,Hubei,China
Zhejiang Chemicals Import & Export Corporation (ZHECHEM)
Contact:+86-571-87046953
Address:No. 37, Qingchun Road
Doi:10.1007/BF00904765
()Doi:10.1016/j.tetlet.2004.08.147
(2004)Doi:10.1246/bcsj.54.2099
(1981)Doi:10.1021/ja00365a023
(1982)Doi:10.1021/jo00336a049
(1981)Doi:10.1039/P29810001392
(1981)