title: Synthesis and Evaluation of Cytotoxic Activity of Some Pyrroles and Fused Pyrroles.
abstract: OBJECTIVE
  Pyrrole derivatives represent a very interesting class as biologically active compounds. The objective of our study was to investigate the cytotoxic and apoptotic effects and antioxidant activity of the newly synthesized pyrrole derivatives.
  
  
  METHODS
  A series of novel pyrroles and fused pyrroles (tetrahydroindoles, pyrrolopyrimidines, pyrrolopyridines and pyrrolotriazines) were synthesized and characterized using IR, 1H NMR, 13C NMR, MS and elemental analysis techniques. The antiproliferative activity of our synthesized compounds and their modulatory effect apoptotic pathway were investigated. The effect on cellular proliferation and viability was monitored by resazurin assay. Apoptotic effect was evaluated by caspase glo 3/7 assay. Synthesized compounds are then tested for their anticancer activities against three different cell lines representing three different tumor types, namely; the HepG-2 (Human hepatocellular liver carcinoma cell line), the human MCF-7 cell line (breast cancer) and the pancreatic resistant Panc-1 cells.
  
  
  RESULTS
  Compounds Ia-e, IIe, and IXc, d showed a promising anti-cancer activity on all tested cell lines. Antioxidant and wound healing invasion assays were examined for promising anticancer candidate compounds.
authors.affiliation: Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Helwan University, Ain-Helwan, Helwan, Cairo. Egypt.
authors.forename: Samar S
authors.initials: SS
authors.lastname: Fatahala
authors.affiliation: Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Helwan University, Ain-Helwan, Helwan, Cairo. Egypt.
authors.forename: Mosaad S
authors.initials: MS
authors.lastname: Mohamed
authors.affiliation: Biochemistry and Molecular Biology Department, Faculty of Pharmacy, Helwan University, Ain-Helwan, Helwan,Cairo. Egypt.
authors.forename: Mahmoud
authors.initials: M
authors.lastname: Youns
authors.affiliation: Pharmaceutical organic chemistry department, Faculty of Pharmacy, Helwan University, Ain- Helwan, Helwan, Cairo. Egypt.
authors.forename: Rania H
authors.initials: RH
authors.lastname: Abd-El Hameed
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D000975:Antioxidants / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects*; D020169:Caspases / Q000378:metabolism; D045744:Cell Line, Tumor; D002465:Cell Movement / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy / Q000378:metabolism; D011758:Pyrroles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D015398:Signal Transduction / Q000187:drug effects
chemical_list: D000970:Antineoplastic Agents; D000975:Antioxidants; D011758:Pyrroles; D020169:Caspases
keywords: Pyrrole; apoptosis; cytotoxicity; pyrrolopyridines; pyrrolopyrimidine; tetrahydroindoles; wound healing and cancer