Design, synthesis and biological activity study of thiazolehydrazone-based small molecule inhibitors of IGF2BP2
10.16438/j.0513-4870.2024-0564
- VernacularTitle:噻唑腙类IGF2BP2小分子抑制剂的设计、合成及生物活性研究
- Author:
Shi-di ZHANG
1
;
Sai MA
1
;
Ying-zhe WANG
1
;
Yuan-qian CAI
1
;
Yan ZHANG
1
;
Qi-dong YOU
1
;
Xiao-ke GUO
1
Author Information
1. Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing; School of Pharmacy, China Pharmaceutical University, Nanjing
- Publication Type:Research Article
- Keywords:
thiazole hydrazone derivative;
insulin-like growth factor 2 mRNA binding protein 2;
italic>N6-methyladenosine;
small-molecule inhibitor;
esign and synthesis
- From:
Acta Pharmaceutica Sinica
2024;59(11):3006-3016
- CountryChina
- Language:Chinese
-
Abstract:
Insulin-like growth factor 2 mRNA binding protein 2 (IGF2BP2) is a recognition protein for N6-methyladenosine (m6A), mediating the stability of downstream mRNA, and is a promising anti-tumor target. Based on the lead compound 1g from previous screening, this study designed and synthesized 52 IGF2BP2 small molecule inhibitors using thiazole hydrazone as the parent nucleus. Among them, 9g, 10g, 37g, 47g and 52g showed good inhibitory activities. This work represents an initial exploration in the development of small molecule inhibitors targeting IGF2BP2, using thiazolehydrazone as the core structure. It lays a foundation for subsequent related research.
