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Short Paper | Special issue | Vol 95, No. 1, 2017, pp.557-567
Published online, 18th October, 2016
DOI: 10.3987/COM-16-S(S)20
Synthesis of β-Dihydropyrrolyl and β-Pyrrolyl Acrylates and Their Antiproliferative Activity against HCT-116 and HL-60 Cells

Noriyuki Hatae,* Yoko Sakai, Kohei Yorozu, Chiaki Okada, Mitsuhiro Yoshimatsu, and Teruki Yoshimura*

*Faculty of Pharmaceutical Sciences, Health Sciences University of Hokkaido, Ishikari-Tobetsu, Hokkaido 061-0293, Japan


The α,β-unsaturated carbonyl derivatives have been reported as bioactive substances, in particular acting as antiproliferative and antifungal agents. In this study, β-dihydropyrrolyl and β-pyrrolyl acrylates were synthesized by copper-mediated 5-endo cyclization of isolable Blaise-type β-enamino esters and were assessed for antiproliferative activity against HCT-116 and HL-60 cells. Some β-dihydropyrroles and β-pyrroles showed such activities, which were found to be due to different mechanisms: the β-dihydropyrroles act as cytotoxic agents, whereas the β-pyrroles act as cell cycle inhibitors.