1,2,3-三唑尼洛替尼类似物：合成与细胞毒性活性

IF 2.1 3区化学 Q2 CHEMISTRY, ORGANIC Tetrahedron Pub Date : 2024-09-26 DOI:10.1016/j.tet.2024.134284

Leticia Almazán-Sánchez , María Teresa Ramírez-Apan , David Morales-Morales , Marco A. García-Eleno , Erick Cuevas-Yañez

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引用次数: 0

摘要

以 CuAAC 反应为关键步骤，通过发散合成方法将尼洛替尼分子中的咪唑环替换为 1,2,3 三唑分子，制备出一系列新型尼洛替尼类似物。合成的化合物对一系列肿瘤细胞系（包括 U251、PC-3、K562、HCT-15、MCF-7 和 SKLU）进行了细胞毒活性测试。结果表明，一些化合物对肿瘤细胞生长的抑制率高达 85.6%。

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1,2,3-Triazole nilotinib analogues: Synthesis and Cytotoxic activity

Using the CuAAC reaction as a key step, a novel series of Nilotinib analogues was prepared by replacing the imidazole ring in the Nilotinib molecule with 1,2,3-triazole moiety via a divergent synthetic approach. The synthesized compounds were tested for cytotoxic activity against a series of tumor cell lines which included U251, PC-3, K562, HCT-15, MCF-7 and SKLU. Inhibition growth up to 85.6 % was observed for some compounds.

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来源期刊

Tetrahedron 化学-有机化学

CiteScore

3.90

自引率

4.80%

发文量

439

审稿时长

34 days

期刊介绍： Tetrahedron publishes full accounts of research having outstanding significance in the broad field of organic chemistry and its related disciplines, such as organic materials and bio-organic chemistry. Regular papers in Tetrahedron are expected to represent detailed accounts of an original study having substantially greater scope and details than that found in a communication, as published in Tetrahedron Letters. Tetrahedron also publishes thematic collections of papers as special issues and ''Reports'', commissioned in-depth reviews providing a comprehensive overview of a research area.

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