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

作者：Yoon Jieun; Ryu Jae Sang^*

来源：Bioorganic & Medicinal Chemistry Letters, 2010, 20(13): 3930-3935.

DOI：10.1016/j.bmcl.2010.05.014

• Lavendustin
• Click chemistry
• Library
• Triazole
• Anticancer

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 0.9 mu M.

• 出版日期2010-7-1