Abstract
Background: Chemotherapy has become one of the methods that are being adopted to treat cancer. Coumarins, thiazoles and thiadiazoles are versatile synthetic scaffolds possessing wide spectrum of biological effects including potential anticancer activity.
Objective: In the efforts to develop suitable anticancer drugs, medicinal chemists have focused on coumarin derivatives. A series of novel thiazole-pyranochromene and thiadiazole-pyranochromene derivatives were synthesized via heterocyclization of varies hydrazonoyl halides with methyl pyrano[3,2- g]chromen-3-yl)ethylidene)hydrazine-1-carbodithioate and pyrano[3,2-g]chromen-3-yl)ethylidene)- hydrazine-1-carbothioamide, respectively.
Method: All the newly synthesized compounds have been characterized on the basis of elemental analysis and spectral data (IR, 1H and 13C NMR, Mass). Moreover, all the products were evaluated for their anticancer activity against HEPG2-1.
Results: The results revealed that six new compounds showed promising anticancer activity.
Conclusion: In the present paper, 3-acetyl-5-methoxy-8-methyl-2H,6H-pyrano[3,2-g]chromene-2,6- dione proved to be a useful precursor for synthesis of various 1,3-thiazoles and 1,2,4-thiadiazoles incorporating pyrano[3,2-g]chromene moiety as anticancer agents. The computational studies using MOE 2014.09 software are confirming the results in biological activity.
Keywords: Pyranochromene, hydrazonoyl halides, thiazoles, thiadiazoles, molecular docking studies, antitumor activity.
Mini-Reviews in Medicinal Chemistry
Title:Synthesis and Molecular Docking of Some Novel Thiazoles and Thiadiazoles Incorporating Pyranochromene Moiety as Potent Anticancer Agents
Volume: 18 Issue: 19
Author(s): Sobhi M. Gomha*, Abdou O. Abdelhamid, Omaima M. Kandil, Sahar M. Kandeel and Nadia A. Abdelrehem
Affiliation:
- Department of Chemistry, Faculty of Science, Cairo University, Giza 12613,Egypt
Keywords: Pyranochromene, hydrazonoyl halides, thiazoles, thiadiazoles, molecular docking studies, antitumor activity.
Abstract: Background: Chemotherapy has become one of the methods that are being adopted to treat cancer. Coumarins, thiazoles and thiadiazoles are versatile synthetic scaffolds possessing wide spectrum of biological effects including potential anticancer activity.
Objective: In the efforts to develop suitable anticancer drugs, medicinal chemists have focused on coumarin derivatives. A series of novel thiazole-pyranochromene and thiadiazole-pyranochromene derivatives were synthesized via heterocyclization of varies hydrazonoyl halides with methyl pyrano[3,2- g]chromen-3-yl)ethylidene)hydrazine-1-carbodithioate and pyrano[3,2-g]chromen-3-yl)ethylidene)- hydrazine-1-carbothioamide, respectively.
Method: All the newly synthesized compounds have been characterized on the basis of elemental analysis and spectral data (IR, 1H and 13C NMR, Mass). Moreover, all the products were evaluated for their anticancer activity against HEPG2-1.
Results: The results revealed that six new compounds showed promising anticancer activity.
Conclusion: In the present paper, 3-acetyl-5-methoxy-8-methyl-2H,6H-pyrano[3,2-g]chromene-2,6- dione proved to be a useful precursor for synthesis of various 1,3-thiazoles and 1,2,4-thiadiazoles incorporating pyrano[3,2-g]chromene moiety as anticancer agents. The computational studies using MOE 2014.09 software are confirming the results in biological activity.
Export Options
About this article
Cite this article as:
Gomha M. Sobhi *, Abdelhamid O. Abdou , Kandil M. Omaima , Kandeel M. Sahar and Abdelrehem A. Nadia , Synthesis and Molecular Docking of Some Novel Thiazoles and Thiadiazoles Incorporating Pyranochromene Moiety as Potent Anticancer Agents, Mini-Reviews in Medicinal Chemistry 2018; 18 (19) . https://dx.doi.org/10.2174/1389557518666180424113819
DOI https://dx.doi.org/10.2174/1389557518666180424113819 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
Call for Papers in Thematic Issues
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Computational Frontiers in Medicinal Chemistry
The thematic issue "Computational Frontiers in Medicinal Chemistry" provides a robust platform for delving into state-of-the-art computational methodologies and technologies that significantly propel advancements in medicinal chemistry. This edition seeks to amalgamate top-tier reviews spotlighting the latest trends and breakthroughs in the fusion of computational approaches, including artificial intelligence (AI) ...read more
Natural Products and Dietary Supplements in Alleviation of Metabolic, Cardiovascular, and Neurological Disorders
Metabolic disorders like diabetes, obesity, inflammation, oxidative stress, cancer etc, cardiovascular disorders like angina, myocardial infarction, congestive heart failure etc as well as neurological disorders like Alzheimer?s, Parkinson?s, Epilepsy, Depression, etc are the global burden. They covered the major segment of the diseases and disorders from which the human community ...read more
Natural Products in Drug Discovery
Natural products have always been one of the important ways of drug discovery due to their novel skeleton and diverse functional group characteristics. According to statistics, between 1981 and 2019, the FDA approved a total of 1,394 small molecule drugs for marketing, of which 930 marketed drugs originated from the ...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
-
The Pleiotropic Effects of PPARs on Vascular Cells and Angiogenesis: Implications for Tissue Engineering
Current Stem Cell Research & Therapy Tyrosinase Activated Melanoma Prodrugs
Anti-Cancer Agents in Medicinal Chemistry Design of New Oxazaphosphorine Anticancer Drugs
Current Pharmaceutical Design Base Excision Repair: Contribution to Tumorigenesis and Target in Anticancer Treatment Paradigms
Current Medicinal Chemistry Tailored Multi-Target Agents. Applications and Design Considerations
Current Pharmaceutical Design Ornithine Decarboxylase Inhibition: A Strategy to Combat Various Diseases
Mini-Reviews in Medicinal Chemistry Brachial Plexopathy as a Complication of Radiotherapy: A Systematic Review
Current Cancer Therapy Reviews Variability in Reward Responsivity and Obesity: Evidence from Brain Imaging Studies
Current Drug Abuse Reviews Based on Nucleotides Analysis of Tumor Cell Lines to Construct and Validate a Prediction Model of Mechanisms of Chemotherapeutics
Anti-Cancer Agents in Medicinal Chemistry Flavonoids and Related Compounds in Non-Alcoholic Fatty Liver Disease Therapy
Current Medicinal Chemistry Hormonal Therapy for Prostate Cancer: Toward Further Unraveling of Androgen Receptor Function
Anti-Cancer Agents in Medicinal Chemistry Patent Selections
Recent Patents on CNS Drug Discovery (Discontinued) Eriocalyxin B-Induced Apoptosis in Pancreatic Adenocarcinoma Cells Through Thiol-Containing Antioxidant Systems and Downstream Signalling Pathways
Current Molecular Medicine Skin Cancers in Elderly Patients
Anti-Cancer Agents in Medicinal Chemistry DNA Methyltransferase-1 Inhibitors as Epigenetic Therapy for Cancer
Current Cancer Drug Targets Garlic-Derived Allyl Sulfides in Cancer Therapy
Anti-Cancer Agents in Medicinal Chemistry Mitochondria as a Target for Exercise-Induced Cardioprotection
Current Drug Targets Synthesis and Biological Evaluation of a Novel Apogossypolone Derivative
Letters in Drug Design & Discovery Blocking IL-6/GP130 Signaling Inhibits Cell Viability/Proliferation, Glycolysis, and Colony Forming Activity in Human Pancreatic Cancer Cells
Current Cancer Drug Targets Role of Prolyl Isomerase Pin1 in Pathogenesis of Diseases and Remedy for the Diseases from Natural Products
Current Drug Targets