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■ Simple Synthesis of New 3-Substituted 4-(3-Chloro-4-fluorophenyl)-1H-pyrrole Derivatives and Their Anticancer Activity in Vitro

Lan Lan, Xiaoping Zhan, Weixi Qin, Zenglu Liu, and Zhenmin Mao*

*School of Pharmacy, Shanghai Jiaotong University , No.800 Dongchuan Road, Minhang District, Shanghai 200240, China

Abstract

The preparation of the new 3-substituted 4-(3-chloro-4-fluorophenyl)-1H-pyrrole derivatives was based on the Van Leusen pyrrole synthesis. In this article, eighteen compounds were readily synthesized in satisfactory to good yields and their cell proliferation inhibiting activities against 2 normal cell lines and 16 cancer cell lines were evaluated. It was particularly important that the new pyrroles displayed barely cytotoxicity against the tested normal cell, which meant these pyrrole analogues might show excellent selectivity towards cancer cell and normal cell. Cell cycle analysis by flow cytometry (FCM) showed that the G0/G1 phase decreased a lot and S phase arrested, in between a minor and transient G2/M block was observed. Cell death induced by 3-cyano-4-(3-chloro-4-fluorophenyl)-1H-pyrrole (2r) was also verified by multiple methods.