Research and development of novel p-21 activated kinase 4 inhibitors

doi:10.19803/j.1672-8629.20240194

Abstract

Abstract: Objective To investigate the applications of p-21 activated kinase 4 (PAK4) inhibitors in tumor therapy in order to provide reference for the development of novel PAK4 inhibitors. Methods Small molecule PAK4 inhibitors were elaborated in terms of structural scaffold, eutectic structure, activity and pharmacokinetics. Results Among various structures of PAK4 inhibitors, the benzofuran inhibitor KPT-9274 exhibited significant inhibitory effects and had anti-tumor effects on various cancers. It was currently the only PAK4 inhibitor in clinical trials and could facilitate future design of PAK4 inhibitors. Conclusion Optimization of the structure of benzofuran compounds is expected to lead to better PAK4 inhibitors for tumor treatment.

Key words: p-21 activates kinase 4(PAK4), inhibitors, benzofuran, KPT-9274, targeted drugs, tumor

CLC Number:

R979.1

YAO Hailiang, DENG Meiyan, LI Xinyang, MENG Fanhao. Research and development of novel p-21 activated kinase 4 inhibitors[J]. Chinese Journal of Pharmacovigilance, 2024, 21(7): 822-828.

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https://zgywjj.magtechjournal.com/EN/Y2024/V21/I7/822

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