Document Detail

Synthesis and Biological Evaluation of 3-Substituted-4-(4-methylthio phenyl)-1H-Pyrrole Derivatives as Potential Anticancer Agents.
MedLine Citation:
PMID:  24372525     Owner:  NLM     Status:  Publisher    
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.
Lan Lan; Weixi Qin; Xiaoping Zhan; Zenglu Liu; Zhenmin Mao
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2013-12-24
Journal Detail:
Title:  Anti-cancer agents in medicinal chemistry     Volume:  -     ISSN:  1875-5992     ISO Abbreviation:  Anticancer Agents Med Chem     Publication Date:  2013 Dec 
Date Detail:
Created Date:  2013-12-30     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  101265649     Medline TA:  Anticancer Agents Med Chem     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
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