title: Synthesis and biological evaluation of 3-substituted-4-(4-methylthio phenyl)-1H-pyrrole derivatives as potential anticancer agents.
abstract: A novel series of 3-substituted-4-(4-methylthio phenyl)-1H-pyrrole derivatives were synthesized via Van Leusen pyrrole synthesis. The in vitro anticancer activity against a panel of 16 cancer cell lines and 2 normal cell lines was investigated by MTT assay. It was found that some of the pyrrole compounds showed similar antiproliferative activity against cancer cells compared with Paclitaxel, but little impact on normal cell lines, which indicated that the novel pyrrole derivatives could be used as potential anticancer candidates for possessing both selectivity and good therapeutic efficacy. Structure-activity relationship analysis found that 3-phenylacetyl-4- (4-methylthio phenyl)-1H-pyrrole derivatives displayed the most strong anticancer activity, among which [4-(4-methylthio phenyl)-1H-pyrrol- 3-yl] (4-methoxy phenyl) methanone (3j) was employed to investigate the effect of these pyrrole analogues on cell cycle by propidium iodide (PI) staining on cell flow cytometry. Cell necrotic effect of 10.0 µM 3j against MGC80-3 cells were also observed under fluorescence microscope and transmission electron microscope by ultrathin sections observation.
authors.forename: Lan
authors.initials: L
authors.lastname: Lan
authors.forename: Weixi
authors.initials: W
authors.lastname: Qin
authors.forename: Xiaoping
authors.initials: X
authors.lastname: Zhan
authors.forename: Zenglu
authors.initials: Z
authors.lastname: Liu
authors.affiliation: School of Pharmacy, Shanghai Jiaotong University, 800 Dongchuan Road, Shanghai 200240, China. zmmao@sjtu.edu.cn.
authors.forename: Zhenmin
authors.initials: Z
authors.lastname: Mao
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D009336:Necrosis; D011758:Pyrroles / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D011758:Pyrroles