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Synthesis of STM2457, a selective small-molecule inhibitor of METTL3
Tetrahedron Letters ( IF 1.8 ) Pub Date : 2024-04-18 , DOI: 10.1016/j.tetlet.2024.155077
Congwei Zhu , Jianguang Liu , Yong Ni , Wei Chen , Weidong Rong , Xiaohan Zhang , Chun Guo , Xiangqian Kong , Shibing Tang

STM2457, a potent and selective inhibitor of mA 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.

中文翻译:

METTL3选择性小分子抑制剂STM2457的合成

STM2457 是一种有效的选择性 m6A 甲基转移酶 METTL3 抑制剂,是癌症治疗的一流候选药物。在此,我们提出了 STM2457 的无色谱合成,分九步,总产率为 32%。与报道的路线相比,目前的方法具有原料便宜、试剂温和和实验操作简单的特点。我们期望目前的工作支持 STM2457 的生产并促进其治疗应用。
更新日期:2024-04-18
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