AI Article Synopsis
- - Researchers developed a series of 3-aroyl-1-arylpyrrole (ARAP) compounds as potential anticancer agents, focusing on how different side groups affect their activity.
- - The key components required for effective anticancer activity include a 1-phenyl ring and a 3-(3,4,5-trimethoxyphenyl)carbonyl group, which are essential for inhibiting tubulin polymerization and cancer cell growth.
- - Among the tested compounds, ARAP 22 demonstrated significant anti-cancer effects, including strong inhibition of certain cancer cell lines and suppression of the Hedgehog signaling pathway, indicating its potential as a novel cancer treatment.
Article Abstract
We synthesized 3-aroyl-1-arylpyrrole (ARAP) derivatives as potential anticancer agents having different substituents at the pendant 1-phenyl ring. Both the 1-phenyl ring and 3-(3,4,5-trimethoxyphenyl)carbonyl moieties were mandatory to achieve potent inhibition of tubulin polymerization, binding of colchicine to tubulin, and cancer cell growth. ARAP 22 showed strong inhibition of the P-glycoprotein-overexpressing NCI-ADR-RES and Messa/Dx5MDR cell lines. Compounds 22 and 27 suppressed in vitro the Hedgehog signaling pathway, strongly reducing luciferase activity in SAG treated NIH3T3 Shh-Light II cells, and inhibited the growth of medulloblastoma D283 cells at nanomolar concentrations. ARAPs 22 and 27 represent a new potent class of tubulin polymerization and cancer cell growth inhibitors with the potential to inhibit the Hedgehog signaling pathway.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4154712 | PMC |
| http://dx.doi.org/10.1021/jm500561a | DOI Listing |
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