Abstract
The heterocyclic system is a promising core nucleus in many bioactive compounds. This work describes our effort to synthesize and characterize a set of new biphenyl, benzofuran and benzothiophene carboxamide derivatives. Our biological studies showed that compounds 10 and 17 have antifungal activity against C. galabrate more potent than fluconazole compounds 9, 10, and 17 exerted cytotoxic activities in immortalized embryonic mouse fibroblast cells (3T3) and a human cervical cancer cell line (HeLa); in particular, the cyclic amidine derivative 17 showed selective toxicity against HeLa. This study showed that the tested compounds have the potential to be useful as antitumor drugs after further optimization.
Keywords: Antifungal activity, cervical cancer cell, cytotoxicity, heterocyclic compounds, NMR, Synthesis.
Letters in Drug Design & Discovery
Title:Synthesis and Preliminary Biological Evaluation of New Heterocyclic Carboxamide Models
Volume: 12 Issue: 5
Author(s): Kamal Sweidan, Jorn Engelmann, Walid Abu Rayyan, Dima Sabbah, Musa Abu Zarga, Dima Sabbah, Tariq Al-Qirim, Yusuf Al-Hiari, Ghassan Abu Sheikha and Ghassan Shattat
Affiliation:
Keywords: Antifungal activity, cervical cancer cell, cytotoxicity, heterocyclic compounds, NMR, Synthesis.
Abstract: The heterocyclic system is a promising core nucleus in many bioactive compounds. This work describes our effort to synthesize and characterize a set of new biphenyl, benzofuran and benzothiophene carboxamide derivatives. Our biological studies showed that compounds 10 and 17 have antifungal activity against C. galabrate more potent than fluconazole compounds 9, 10, and 17 exerted cytotoxic activities in immortalized embryonic mouse fibroblast cells (3T3) and a human cervical cancer cell line (HeLa); in particular, the cyclic amidine derivative 17 showed selective toxicity against HeLa. This study showed that the tested compounds have the potential to be useful as antitumor drugs after further optimization.
Export Options
About this article
Cite this article as:
Sweidan Kamal, Engelmann Jorn, Abu Rayyan Walid, Sabbah Dima, Abu Zarga Musa, Sabbah Dima, Al-Qirim Tariq, Al-Hiari Yusuf, Abu Sheikha Ghassan and Shattat Ghassan, Synthesis and Preliminary Biological Evaluation of New Heterocyclic Carboxamide Models, Letters in Drug Design & Discovery 2015; 12 (5) . https://dx.doi.org/10.2174/1570180812666141201222527
DOI https://dx.doi.org/10.2174/1570180812666141201222527 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
- 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
-
The Initiation Mechanisms of Gene Expression in Ascitic Hepatoma Cells Under the Action of Dehydroepiandrosterone in a Complex with Apolipoprotein A-I
Current Chemical Biology MicroRNAs in Cancer: Small Molecules, Big Chances
Anti-Cancer Agents in Medicinal Chemistry Towards the Molecular Imaging of Prostate Cancer Biomarkers Using Protein-based MRI Contrast Agents
Current Protein & Peptide Science An update on Anti-inflammatory Compounds: A Review
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Status of Anti-Lung Cancer Drug Patents Applications in China from 2003 to 2012
Recent Patents on Anti-Cancer Drug Discovery Identification of Novel Key Targets and Candidate Drugs in Oral Squamous Cell Carcinoma
Current Bioinformatics Analysis of Codon Usage Patterns in the Human Papillomavirus Oncogenes
Current Bioinformatics Epi-Drugs and Epi-miRs: Moving Beyond Current Cancer Therapies
Current Cancer Drug Targets FDG-PET Scan in Sarcoidosis: Clinical and Imaging Indications
Current Medical Imaging Novel Chemotherapeutic Agents - The Contribution of Scorpionates
Current Medicinal Chemistry Influence of New Synthetic Xanthones on the Proliferation and Migration Potential of Cancer Cell Lines In Vitro
Anti-Cancer Agents in Medicinal Chemistry Mechanisms Used by Human Papillomaviruses to Escape the Host Immune Response
Current Cancer Drug Targets Alternative Splicing, DNA Damage and Modulating Drugs in Radiation Therapy for Cancer
Anti-Cancer Agents in Medicinal Chemistry MicroRNA and Bone Tumor: To Up Date
Current Signal Transduction Therapy Double-Edged Effects of Arsenic Compounds: Anticancer and Carcinogenic Effects
Current Drug Metabolism Carbonic Anhydrase Inhibitors and the Management of Cancer
Current Topics in Medicinal Chemistry Crocetin as an Active Secondary Metabolite of Saffron Stigma and Anticancer Effects
Current Cancer Therapy Reviews Pharmacological Interventions for the Prevention and Treatment of Kidney Injury Induced by Radiotherapy: Molecular Mechanisms and Clinical Perspectives
Current Molecular Pharmacology In vitro Study on the Effect of Nanoparticles and Transfersomes as Targeted Drug Carrier for Cancer
Nanoscience & Nanotechnology-Asia On the Role of Rab5 in Cell Migration
Current Molecular Medicine