Bioorganic & medicinal chemistry letters

A rapid synthesis of lavendustin-mimetic small molecules by click fragment assembly

J Yoon, JS Ryu

文献索引：Yoon, Jieun; Ryu, Jae-Sang Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 13 p. 3930 - 3935

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被引用次数: 19

摘要

Lavendustin-mimetic small molecules modifying the linker–CH2–NH–with an 1, 2, 3-triazole ring have been synthesized via a click chemistry. Two pharmacophoric fragments of lavendustin were varied to investigate chemical space and the auxophoric–CH2–NH–was altered to an 1, 2, 3-triazole for rapid click conjugation. The small molecules were evaluated against HCT116 colon cancer and CCRF-CEM leukemia cell lines. Among 28 analogues, ...