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.
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