5 取代噻唑基脲衍生物的合成和抗白血病活性。

IF 2.5 4区医学 Q3 CHEMISTRY, MEDICINAL Bioorganic & Medicinal Chemistry Letters Pub Date : 2024-11-11 DOI:10.1016/j.bmcl.2024.130018

Cheng Peng, Li Sheng, Gao-Ya Xu, Xiao-Lei Qi, Yu-Bo Zhou, Jia-Li, Yong-Mei Cui

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引用次数: 0

摘要

研究人员合成了一系列新型 5 取代噻唑基脲衍生物，并评估了它们作为抗白血病药物对两种人类白血病细胞系（THP-1 和 MV-4-11）的疗效。结果表明，所研究化合物的活性对芳香取代基的位置和性质相当敏感。在这些化合物中，化合物 12k 的活性最高，对 THP-1 细胞的 IC50 值为 29 ± 0.3 nM，对 MV-4-11 细胞的 IC50 值为 98 ± 10 nM。

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The synthesis and antileukemic activity of 5-substituted thiazolyl urea derivatives.

A series of novel 5-substituted thiazolyl urea derivatives were synthesized and evaluated for their efficacy as antileukemic agents against two human leukemic cell lines (THP-1 and MV-4-11). Results showed that the activities of the investigated compounds were quite sensitive to the positions and properties of the aromatic substituents. Among these compounds, compound 12k showed the highest activity with IC₅₀ values of 29 ± 0.3 nM for THP-1 cells and 98 ± 10 nM for MV-4-11 cells.

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来源期刊

Bioorganic & Medicinal Chemistry Letters 医学-医药化学

CiteScore

5.70

自引率

3.70%

发文量

463

审稿时长

27 days

期刊介绍： Bioorganic & Medicinal Chemistry Letters presents preliminary experimental or theoretical research results of outstanding significance and timeliness on all aspects of science at the interface of chemistry and biology and on major advances in drug design and development. The journal publishes articles in the form of communications reporting experimental or theoretical results of special interest, and strives to provide maximum dissemination to a large, international audience.