Synthesis of STM2457, a selective small-molecule inhibitor of METTL3

被引：0

作者：

Zhu, Congwei ^{[1
,2
]}

Liu, Jianguang ^{[2
]}

Ni, Yong ^{[2
]}

Chen, Wei ^{[1
,2
]}

Rong, Weidong ^{[1
,2
]}

Zhang, Xiaohan ^{[2
]}

Guo, Chun ^{[1
]}

Kong, Xiangqian ^{[1
,2
,3
]}

Tang, Shibing ^{[1
,2
,3
]}

机构：

[1] Shenyang Pharmaceut Univ, Key Lab Struct Based Drugs Design & Discovery, Minist Educ, Shenyang 110016, Peoples R China

[2] Chinese Acad Sci, Guangzhou Inst Biomed & Hlth, Ctr Chem Biol & Drug Discovery, State Key Lab Resp Dis, Guangzhou 510530, Peoples R China

[3] China New Zealand Joint Lab Biomed & Hlth, Guangzhou 510530, Peoples R China

来源：

TETRAHEDRON LETTERS | 2024年 / 141卷

基金：

国家重点研发计划;

关键词：

STM2457; M 6 A methyltransferase METTL3; Chromatography -free synthesis;

D O I：

10.1016/j.tetlet.2024.155077

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

STM2457, a potent and selective inhibitor of m6A methyltransferase METTL3, is a first-in-class drug candidate for cancer therapy. Herein, we present a chromatography-free synthesis of STM2457 in nine steps and 32% overall yield. In comparison to the reported route, the current approach features inexpensive raw materials, gentle reagents and simple experimental manipulations. We expect the present work supports the production of STM2457 and facilitates its therapeutic applications.

引用

页数：6

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