| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1374022 | Bioorganic & Medicinal Chemistry Letters | 2010 | 6 Pages |
Lavendustin-mimetic small molecules modifying the linker –CH2–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.
Graphical abstractA lavendustin-mimetic small-molecule library has been synthesized via a click chemistry. 3-Phenylpropyl ester 26b inhibited CCRF-CEM leukemia cell growth with GI50 value of 0.9 μM.Figure optionsDownload full-size imageDownload as PowerPoint slide
