title: Synthesis and Anticancer Activity of 3-(Substituted Aroyl)-4-(3,4,5-trimethoxyphenyl)-1H-pyrrole Derivatives.
abstract: A series of 3-(substituted aroyl)-4-(3,4,5-trimethoxyphenyl)-1H-pyrrole derivatives were synthesized and determined for their anticancer activity against eleven cancer cell lines and two normal tissue cell lines using MTT assay. Among the synthesized compounds, compound 3f was the most potent compound against A375, CT-26, HeLa, MGC80-3, NCI-H460 and SGC-7901 cells (IC50= 8.2 - 31.7 μm); 3g, 3n and 3a were the most potent compounds against CHO (IC50= 8.2 μm), HCT-15 (IC50= 21 μm) and MCF-7 cells (IC50= 18.7 μm), respectively. Importantly, all the target compounds showed no cytotoxicity towards the normal tissue cell (IC50> 100 μm). Thus, these compounds with the potent anticancer activity and low toxicity have potential for the development of new anticancer chemotherapy agents.
authors.affiliation: School of Pharmacy, Shanghai Jiaotong University, 800 Dongchuan Road, Shanghai, 200240, P. R. China.
authors.forename: Xiao-Ping
authors.initials: XP
authors.lastname: Zhan
authors.affiliation: School of Pharmacy, Shanghai Jiaotong University, 800 Dongchuan Road, Shanghai, 200240, P. R. China.
authors.forename: Lan
authors.initials: L
authors.lastname: Lan
authors.affiliation: School of Pharmacy, Shanghai Jiaotong University, 800 Dongchuan Road, Shanghai, 200240, P. R. China.
authors.forename: Shuai
authors.initials: S
authors.lastname: Wang
authors.affiliation: School of Pharmacy, Shanghai Jiaotong University, 800 Dongchuan Road, Shanghai, 200240, P. R. China.
authors.forename: Kai
authors.initials: K
authors.lastname: Zhao
authors.affiliation: School of Pharmacy, Shanghai Jiaotong University, 800 Dongchuan Road, Shanghai, 200240, P. R. China.
authors.forename: Yu-Xuan
authors.initials: YX
authors.lastname: Xin
authors.affiliation: School of Pharmacy, Shanghai Jiaotong University, 800 Dongchuan Road, Shanghai, 200240, P. R. China.
authors.forename: Qi
authors.initials: Q
authors.lastname: Qi
authors.affiliation: School of Pharmacy, Shanghai Jiaotong University, 800 Dongchuan Road, Shanghai, 200240, P. R. China.
authors.forename: Yao-Lin
authors.initials: YL
authors.lastname: Wang
authors.affiliation: School of Pharmacy, Shanghai Jiaotong University, 800 Dongchuan Road, Shanghai, 200240, P. R. China.
authors.forename: Zhen-Min
authors.initials: ZM
authors.lastname: Mao
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D049109:Cell Proliferation / Q000187:drug effects*; D002478:Cells, Cultured; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D061307:Human Umbilical Vein Endothelial Cells; D006801:Humans; D015394:Molecular Structure; D009369:Neoplasms / Q000188:drug therapy* / Q000473:pathology; D011758:Pyrroles / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: C000614476:(4-bromophenyl)(4-(3,4,5-trimethoxyphenyl)-1H-pyrrol-3-yl)methanone; D000970:Antineoplastic Agents; D011758:Pyrroles
keywords: Anticancer activities; Cytotoxic activities; MTT Assay; Pyrrole derivatives; Synthesis