Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 57, Issue 15, Pages 6531-6552Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm500561a
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Funding
- PRIN [2010W7YRLZ_001, 2010W7YRLZ_001006, 2012CSYJSK002]
- AIRC [IG 14535, IG14723]
- Bando Futuro in Ricerca [RBFR10ZJQT]
- Progetti di Ricerca di Universita, Sapienza Universita di Roma [C26H135FL5]
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We synthesized 3-aroy1-1-arylpyrrole (ARAP) derivatives as potential anticancer agents having different substituents at the pendant 1-phenyl ring. Both the 1-phenyl ring and 343,4,5-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 11 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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