Center for Cell Signaling & Drug Discovery Research, Ewha Womans University, Seodaemun-Gu, Seoul, Republic of Korea.
Bioorg Med Chem Lett. 2010 Jul 1;20(13):3930-5. doi: 10.1016/j.bmcl.2010.05.014. Epub 2010 May 12.
Lavendustin-mimetic small molecules modifying the linker -CH(2)-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 -CH(2)-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, 3-phenylpropyl ester 26b inhibited CCRF-CEM leukemia cell growth with GI(50) value of 0.9microM.
通过点击化学合成了用 1,2,3-三唑环修饰连接子-CH(2)-NH-的薰衣草素类似小分子。改变了薰衣草素的两个药效团片段以研究化学空间，并将助效基 -CH(2)-NH-改为 1,2,3-三唑以实现快速点击共轭。这些小分子针对 HCT116 结肠癌细胞和 CCRF-CEM 白血病细胞系进行了评估。在 28 种类似物中，3-苯基丙基酯 26b 对 CCRF-CEM 白血病细胞生长的 GI(50) 值为 0.9μM。
