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Synthesis and Cytotoxicity Evaluation of New 3‐substituted 4‐(4‐methyloxy phenyl)‐1 H ‐Pyrrole Derivatives
Author(s) -
Zhan Xiaoping,
Lan Lan,
Zhang Yuankui,
Chen Jian,
Zhao Kai,
Wang Shuai,
Xin Yuxuan,
Mao Zhenmin
Publication year - 2016
Publication title -
bulletin of the korean chemical society
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.237
H-Index - 59
ISSN - 1229-5949
DOI - 10.1002/bkcs.10653
Subject(s) - pyrrole , cytotoxicity , chemistry , selectivity , cell culture , stereochemistry , cancer cell , cancer cell lines , combinatorial chemistry , biochemistry , in vitro , cancer , organic chemistry , biology , genetics , catalysis
A new series of 3‐substituted 4‐(4‐methyloxy phenyl)‐1 H ‐pyrrole derivatives were synthesized and biologically evaluated for potential anticancer activity. Fifteen targeted compounds showed high selectivity toward normal cells and cancer cells: that is, all targeted compounds had no obvious cytotoxicity toward normal human cells ( HUVEC and NIH / 3T3 ), but some compounds exhibited broad‐spectrum proliferation inhibitory activity against the screened cancer cell lines. Among these pyrrole derivatives, compounds 3b and 3o showed potent anticancer activity against the MG ‐63 cell line, with IC 50 values of 14.9 and 12.7 μM , respectively. Other pyrrole derivatives also showed promising proliferation inhibitory activity, including compound 3d against A375 ( IC 50 = 18.6 μM ), compound 3f and 3j against MGC80 ‐3 ( IC 50 = 19.9 μM ), and compound 3o against MGC80 ‐3 ( IC 50 = 11.9 μM ). Because the developed pyrrole derivatives showed strong anticancer activity and high selectivity, this new series of pyrrole derivatives could be considered as promising lead compounds for further development of potent and safe anticancer agents.