Title:Synthesis and Evaluation of Cytotoxic Activity of Some Pyrroles and Fused Pyrroles
Volume: 17
Issue: 7
Author(s): Samar S. Fatahala, Mosaad S. Mohamed, Mahmoud Youns and Rania H. Abd-El Hameed*
Affiliation:
- Pharmaceutical organic chemistry department, Faculty of Pharmacy, Helwan University, Ain- Helwan, Helwan, Cairo,Egypt
Keywords:
Pyrrole, tetrahydroindoles, pyrrolopyrimidine, pyrrolopyridines, cytotoxicity, apoptosis, wound healing and cancer.
Abstract: Aims: 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.
Method: 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.
Result: 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.
