Synthesis and Anti-cancer Activity of 3-substituted Benzoyl-4-substituted Phenyl-1H-pyrrole Derivatives

Author(s): Xiaoping Zhan, Weixi Qin, Shuai Wang, Kai Zhao, Yuxuan Xin, Yaolin Wang, Qi Qi, Zhenmin Mao*

Journal Name: Anti-Cancer Agents in Medicinal Chemistry
(Formerly Current Medicinal Chemistry - Anti-Cancer Agents)

Volume 17 , Issue 6 , 2017

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Graphical Abstract:


Background: Cancer is considered a major public health problem worldwide.

Objective: The aim of this paper is to design and synthesis of novel anticancer agents with potent anticancer activity and minimum side effects. Method: A series of pyrrole derivatives were synthesized, their anti-cancer activity against nine cancer cell lines and two non-cancer cell lines were evaluated by MTT assay, and their cell cycle progression were determined by flow cytometry analysis.

Results: The study of the structure-activity relationships revealed that the introduction of the electron-donation groups at the 4th position of the pyrrole ring increased the anti-cancer activity. Among the synthesized compounds, specially the compounds bearing 3,4-dimethoxy phenyl at the 4th position of the pyrrole ring showed potent anti-cancer activity, cpd 19 was the most potent against MGC 80-3, HCT-116 and CHO cell lines (IC50s = 1.0-1.7 μM), cpd 21 was the most potent against HepG2, DU145 and CT-26 cell lines (IC50s = 0.5-0.9 μM), and cpd 15 was the most potent against A549 (IC50 = 3.6 μM). Moreover, these potent compounds showed weak cytotoxicity against HUVEC and NIH/3T3. Thus, the cpds 15, 19 and 21 show potential anti-cancer for further investigation. Furthermore, the flow cytometry analysis revealed that cpd 21 arrested the CT-26 cells at S phase, and induced the cell apoptosis.

Conclusion: Thus, these compounds with the potent anticancer activity and low toxicity have potential for the development of new anticancer chemotherapy agents.

Keywords: Pyrrole derivatives, anticancer activity, synthesis, MTT assay, cytotoxicity, benzoyl-4-substituted.

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Article Details

Year: 2017
Page: [821 - 831]
Pages: 11
DOI: 10.2174/1871520616666160923092718
Price: $65

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