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 language | English |
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Pages (from-to) | 3930-3935 |
Number of pages | 6 |
Journal | Bioorganic and Medicinal Chemistry Letters |
Volume | 20 |
Issue number | 13 |
DOIs | |
State | Published - 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