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

Title
A rapid synthesis of lavendustin-mimetic small molecules by click fragment assembly
Authors
Yoon J.Ryu J.-S.
Ewha Authors
류재상
SCOPUS Author ID
류재상scopus
Issue Date
2010
Journal Title
Bioorganic and Medicinal Chemistry Letters
ISSN
0960-894XJCR Link
Citation
vol. 20, no. 13, pp. 3930 - 3935
Indexed
SCI; SCIE; SCOPUS WOS scopus
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. © 2010 Elsevier Ltd. All rights reserved.
DOI
10.1016/j.bmcl.2010.05.014
Appears in Collections:
약학대학 > 약학과 > Journal papers
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