In this section, you can access to the latest technical information related to the FUTURE project topic.

Phosphamide-Containing Diphenylpyrimidine Analogues (PA-DPPYs) as Potent Focal Adhesion Kinase (FAK) Inhibitors with Enhanced Activity against Pancreatic Cancer Cell Lines

A family of phosphamide-containing diphenylpyrimidine analogues (PA-DPPYs) were synthesized as potent focal adhesion kinase (FAK) inhibitors. The PA-DPPY derivatives could significantly inhibit the FAK enzymatic activity within concentrations of lower than 10.69 nM. Among them, compounds 7a and 7e were two of the most active FAK inhibitors, possessing IC50 values of 4.25 nM and 4.65 nM, respectively. In particular, compound 7e also displayed strong activity against AsPC cell line, with an IC50 of 1.66 ?M, but show low activity against the normal HPDE6-C7 cells (IC50 > 20 ?M), indicating its low cell cytoxicity. Additionally, flow cytometry analysis showed that after treatment of 7e (8 ?M, 72 h), both AsPC and Panc cells were almost totally inhibited, with a cell viability rate of 16.8% and 18.1%, respectively. Overall, compound 7e may be served as a valuable FAK inhibitor for the treatment of pancreatic cancer.

» Author: He Liu, Bin Wu, Yang Ge, Jiaxin Xu, Shijie Song, Changyuan Wang, Jihong Yao, Kexin Liu, Yanxia Li, Xiuli Sun, Xiaodong Ma

» Reference: Bioorganic & Medicinal Chemistry

» More Information

« Go to Technological Watch



AIMPLAS Instituto Tecnológico del Plástico

C/ Gustave Eiffel, 4
(València Parc Tecnològic) - 46980
PATERNA (Valencia) - SPAIN

PHONE

(+34) 96 136 60 40

EMAIL

Project Management department - Sustainability and Industrial Recovery
life-future-project@aimplas.es