Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 27, Issue 2, Pages 191-195Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2016.11.076
Keywords
Indoles; Lactams; Anti-cancer; MTT
Categories
Funding
- NSF [RUI: 1362813]
- Hobart and William Smith Colleges
- Patchett Family
- Division Of Chemistry
- Direct For Mathematical & Physical Scien [1362183] Funding Source: National Science Foundation
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Analogs containing a central 3-pyrrolin-2-one core with different methoxyphenyl and/or indole substituents were prepared and tested for anti-proliferative activity in U-937 cells. The most efficacious analogs were non-rigid, (non-fused) contained methoxyaryl groups located at the 4-position, and contained either methoxyaryl or indole groups located at the 3-position. Both the number of methoxy groups contained in the substituents and the particular location of the indole rings with respect to the lactam carbonyl had significant affects on anti-proliferative activity. This work provides a framework to better understand structure-activity relationships for inducing anti-proliferative activity in diaryl heterocyclic scaffolds. (C) 2016 Elsevier Ltd. All rights reserved.
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