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

Design, synthesis and activity evaluation of isopropylsulfonyl-substituted 2,4- diarylaminopyrimidine derivatives as FAK inhibitors for the potential treatment of pancreatic cancer

A series of isopropylsulfonyl-substituted 2,4-diarylaminopyrimidine derivatives were designed and synthesized as FAK inhibitors to evaluate their biological activity against pancreatic cancer. One of the most promising compound, 9h, effectively interfered with FAK-mediated phosphorylation and suppressed the proliferation of human pancreatic cancer AsPC-1?cells with half maximal inhibitory concentration (IC50) values of 0.1165?nM and 0.1596??M, respectively. In addition, 9h also exhibited relatively low toxicity against immortalized normal human liver L-02?cells, indicating its low hepatotoxicity at an equivalent dosage. Furthermore, the elucidation of the mechanism of action revealed that compound 9h effectively inhibited cell migration and inhibited the proliferation of AsPC-1 by blocking the cell cycle at the G2/M phase. Moreover, 9h also demonstrated efficacy in inhibiting tumor growth in a murine AsPC-1?cell xenograft model at the dosage of 10?mg/kg without losing noticeable body weight. All these findings provide important clues for the identification of potent FAK inhibitors.

» Author: Xu Zheng, Xing Li, Liangliang Tian, Bin Wu, Jiawen Yu, Changyuan Wang, Xiuli Sun, Xiaodong Ma, Lixue Chen, Yanxia Li

» Publication Date: 05/11/2022

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