2. Academic Validation
  3. A rapid synthesis of lavendustin-mimetic small molecules by click fragment assembly

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

  • Bioorg Med Chem Lett. 2010 Jul 1;20(13):3930-5. doi: 10.1016/j.bmcl.2010.05.014.
Jieun Yoon 1,  Jae-Sang Ryu
Affiliations

Affiliation

  • 1 Center for Cell Signaling & Drug Discovery Research, Ewha Womans University, Seodaemun-Gu, Seoul, Republic of Korea.
PMID: 20570145 DOI: 10.1016/j.bmcl.2010.05.014
Abstract

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.

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