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.Keywords: Pyrrole, tetrahydroindoles, pyrrolopyrimidine, pyrrolopyridines, cytotoxicity, apoptosis, wound healing and cancer.
Anti-Cancer Agents in Medicinal Chemistry
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.Export Options
About this article
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 |
Call for Papers in Thematic Issues
Induction of cell death in cancer cells by modulating telomerase activity using small molecule drugs
Telomeres are distinctive but short stretches present at the corners of chromosomes and aid in stabilizing chromosomal makeup. Resynthesis of telomeres supported by the activity of reverse transcriptase ribonucleoprotein complex telomerase. There is no any telomerase activity in human somatic cells, but the stem cells and germ cells undergone telomerase ...read more
Role of natural compounds as anti anti-cancer agents
Cancer is considered the leading cause of worldwide mortality, accounting for nearly 10 million deaths in 2022. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy remains an important approach in treatment o f several types of cancers, even though ...read more
Signaling and enzymatic modulators in cancer treatment
Cancer accounts for nearly 10 million deaths in 2022 and is considered the leading cause of worldwide mortality. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy, radiotherapy and surgery are the most important approach for the treatment of several ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Reprograming Carcinoma Associated Fibroblasts by microRNAs
Current Molecular Medicine Modulation of Nitric Oxide Pathway by Multiligands/RAGE Axis: A Crossing Point on the Road to Microvascular Complication in Diabetes
Current Enzyme Inhibition Chemical Senses in Cancer Patients
Current Pharmaceutical Design Cellular and Biochemical Alterations Caused by Artificial Depletion of Glutathione
Current Enzyme Inhibition Antiangiogenic Drugs and Tyrosine Kinases
Anti-Cancer Agents in Medicinal Chemistry Thirty Years of Polyamine-Related Approaches to Cancer Therapy. Retrospect and Prospect. Part 1. Selective Enzyme Inhibitors
Current Drug Targets Concentrations of Cd, Cu, Pb and Zn in Blood Serum of Cancer Patients and Comparison with Healthy Person by Atomic Absorption Spectrometry
Current Analytical Chemistry The High Mobility Group A1 (HMGA1) Transcriptome in Cancer and Development
Current Molecular Medicine What does the Hospital Anxiety and Depression Scale (HADS) Really Measure in Liaison Psychiatry Settings?
Current Psychiatry Reviews Digital Mammograms with Image Enhancement Techniques for Breast Cancer Detection: A Systematic Review
Current Medical Imaging Protein Tyrosine Signaling and its Potential Therapeutic Implications in Carcinogenesis
Current Pharmaceutical Design New Approaches in Glioblastoma Multiforme: The Potential Role of Immune- check Point Inhibitors
Current Cancer Drug Targets Insulin-Like Growth Factor 1 Receptor Targeted Therapeutics: Novel Compounds and Novel Treatment Strategies for Cancer Medicine
Recent Patents on Anti-Cancer Drug Discovery Microarray Data Analysis to Find Diagnostic Approach and Identify Families of Disease-Altered Genes Based on Rank-Reverse of Gene Expression
Current Bioinformatics Strategies to Increase the Oral Bioavailability of Nucleoside Analogs
Current Medicinal Chemistry Relevance of Protein Isoforms in Proteomic Studies
Current Proteomics Doxorubicin-Loaded Micelle Targeting MUC1: A Potential Therapeutic for MUC1 Triple Negative Breast Cancer Treatment
Current Drug Delivery Novel dibenzo[b,d]furan–1H-1,2,4-triazole derivatives: Synthesis and antitumor activity
Anti-Cancer Agents in Medicinal Chemistry Preclinical and Clinical Studies of Chidamide (CS055/HBI-8000), An Orally Available Subtype-selective HDAC Inhibitor for Cancer Therapy
Anti-Cancer Agents in Medicinal Chemistry Janus Molecule I: Dichotomous Effects of COMT in Neuropathic vs Nociceptive Pain Modalities
CNS & Neurological Disorders - Drug Targets