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

The small molecule STM2457, a selective inhibitor of m6A methyltransferase METTL3, holds considerable potential for cancer therapy. In this paper, a chromatography-free synthesis of STM2457 featuring inexpensive raw materials and easy synthetic manipulations is presented. [Display omitted] STM2457,...

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Bibliographic Details
Published in:Tetrahedron letters 2024-05, Vol.141, p.155077, Article 155077
Main Authors: Zhu, Congwei, Liu, Jianguang, Ni, Yong, Chen, Wei, Rong, Weidong, Zhang, Xiaohan, Guo, Chun, Kong, Xiangqian, Tang, Shibing
Format: Article
Language:English
Subjects:
Chromatography-free synthesis
M6A methyltransferase METTL3
STM2457
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Summary:The small molecule STM2457, a selective inhibitor of m6A methyltransferase METTL3, holds considerable potential for cancer therapy. In this paper, a chromatography-free synthesis of STM2457 featuring inexpensive raw materials and easy synthetic manipulations is presented. [Display omitted] 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.
ISSN:0040-4039
1873-3581
DOI:10.1016/j.tetlet.2024.155077