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

Jieun Yoon, Jae Sang Ryu

Research output: Contribution to journalArticlepeer-review

29 Scopus citations

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 -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, 3-phenylpropyl ester 26b inhibited CCRF-CEM leukemia cell growth with GI50 value of 0.9 μM.

Original languageEnglish
Pages (from-to)3930-3935
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume20
Issue number13
DOIs
StatePublished - 2010

Bibliographical note

Funding Information:
This work was supported by the Korea Research Foundation Grant funded by the Korean Government (MOEHRD) ( KRF-2007-313-E00645 ). J.Y. was supported by the Brain Korea 21 project. Authors thank Hwayoung Yun and Dr. Seung-Mann Paek for mass spectroscopy.

Keywords

  • Anticancer
  • Click chemistry
  • Lavendustin
  • Library
  • Triazole

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