Online article for Non-subscribers

Pay per view

Heterocycles has a pay-per-view service for Non-subscribers.
You will be able to directly purchase the full text article through PayPal.
Your purchased Paper can be downloaded after the payment is completed.
An e-mail will be sent the URL to download the paper.
If you have any questions, please contact: purchase@heterocycles.com

Price: ¥ 4,400 (Yen only)
Period: This Article can be accessed for 7 days.

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

Abstract

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.