Design, synthesis and biological evaluation of novel triazoloquinazolinone and imidazoquinazolinone derivatives as allosteric inhibitors of SHP2 phosphatase

Wenjun Ye, Ye Liu, Qian Ren, Tianhui Liao, Yumei Chen, Dongmei Chen, Sisi Wang, Lihong Yao, Yihe Jia, Chunshen Zhao & Zhixu Zhou
A series of novel triazoloquinolinone and imidazoquinazolinone derivatives were designed and synthesised, and their biological activities against SHP2 protein and melanoma A357 cell line were evaluated in vitro. The results show that some target compounds have moderate to excellent inhibitory activity on SHP2 protein and melanoma A357 cell line. Structure-activity relationships (SARs) showed that both imidazoquinazolinone and triazoloquinazolinone derivatives have good SHP2 protein kinase and melanoma cell line A357 inhibitory activity. The results of molecular...
1 citation reported since publication in 2022.
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