Synthesis and Evaluation of Cytotoxic Activity of Some Pyrroles and Fused Pyrroles

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.

Cite this article as:

Fatahala S. Samar, Mohamed S. Mosaad, Youns Mahmoud and Abd-El Hameed H. Rania*, Synthesis and Evaluation of Cytotoxic Activity of Some Pyrroles and Fused Pyrroles, Anti-Cancer Agents in Medicinal Chemistry 2017; 17 (7) . https://dx.doi.org/10.2174/1871520617666170102152928

DOI https://dx.doi.org/10.2174/1871520617666170102152928	Print ISSN 1871-5206
Publisher Name Bentham Science Publisher	Online ISSN 1875-5992