Abstract
In this research work, a series of eighteen novel coumarinyl substituted thiazolidin-2,4-dione analogs (4a-4r) have been designed by molecular hybridization approach, synthesized and their structures were established on the basis of FTIR, 1H NMR, 13C NMR and elemental (CHN) analysis. These title compounds were screened for their cytotoxicity using MTT assay methodology against five different mammalian cancer cell lines viz. hormone dependant breast adenocarcinoma (MCF7), cervical carcinoma (HeLa), colorectal carcinoma (HT29), lung cancer (A549) and prostate adeno carcinoma (PC3). The cytotoxicity screening studies revealed that MCF-7, HeLa and A549 cancer cell lines were sensitive to all the tested compounds. Though the compounds showed varying degrees of cytotoxicity in the tested cell lines, most significant effect was observed for compounds 4i (1.06, 2.4 and 3.06 µM) and 4o (0.95, 3.2 and 2.38 μM) against MCF7, HeLa and A549 cell lines respectively. In conclusion, the anticancer results of these promising leads strongly encouraged us for additional lead optimization with the aim of developing more potential anticancer agents.
Keywords: Anticancer activity, Coumarin, Cytotoxicity, MTT assay, Thiazolidin-2, 4-dione.
Anti-Cancer Agents in Medicinal Chemistry
Title:Novel Series of Coumarinyl Substituted-thiazolidin-2,4-dione Analogs as Anticancer Agents: Design, Synthesis, Spectral Studies and Cytotoxicity Evaluation
Volume: 15 Issue: 8
Author(s): Mahesh B. Palkar, Sunil S. Jalalpure, Rajesh A. Rane, Harun M. Patel, Mahamadhanif S. Shaikh, Girish A. Hampannavar, Wesam S. Alwan, Girish S. Bolakatti and Rajshekhar Karpoormath
Affiliation:
Keywords: Anticancer activity, Coumarin, Cytotoxicity, MTT assay, Thiazolidin-2, 4-dione.
Abstract: In this research work, a series of eighteen novel coumarinyl substituted thiazolidin-2,4-dione analogs (4a-4r) have been designed by molecular hybridization approach, synthesized and their structures were established on the basis of FTIR, 1H NMR, 13C NMR and elemental (CHN) analysis. These title compounds were screened for their cytotoxicity using MTT assay methodology against five different mammalian cancer cell lines viz. hormone dependant breast adenocarcinoma (MCF7), cervical carcinoma (HeLa), colorectal carcinoma (HT29), lung cancer (A549) and prostate adeno carcinoma (PC3). The cytotoxicity screening studies revealed that MCF-7, HeLa and A549 cancer cell lines were sensitive to all the tested compounds. Though the compounds showed varying degrees of cytotoxicity in the tested cell lines, most significant effect was observed for compounds 4i (1.06, 2.4 and 3.06 µM) and 4o (0.95, 3.2 and 2.38 μM) against MCF7, HeLa and A549 cell lines respectively. In conclusion, the anticancer results of these promising leads strongly encouraged us for additional lead optimization with the aim of developing more potential anticancer agents.
Export Options
About this article
Cite this article as:
B. Palkar Mahesh, Jalalpure Sunil S., A. Rane Rajesh, M. Patel Harun, S. Shaikh Mahamadhanif, A. Hampannavar Girish, S. Alwan Wesam, S. Bolakatti Girish and Karpoormath Rajshekhar, Novel Series of Coumarinyl Substituted-thiazolidin-2,4-dione Analogs as Anticancer Agents: Design, Synthesis, Spectral Studies and Cytotoxicity Evaluation, Anti-Cancer Agents in Medicinal Chemistry 2015; 15 (8) . https://dx.doi.org/10.2174/1871520615666150424110339
DOI https://dx.doi.org/10.2174/1871520615666150424110339 |
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
-
Phosphodiesterase Type 5 Inhibitors: Unmet Needs
Current Pharmaceutical Design Inhibitors of the Chemokine Receptor CXCR4: Chemotherapy of AIDS, Metastatic Cancer, Leukemia and Rheumatoid Arthritis
Letters in Drug Design & Discovery Can the Use of HIV-1 Derived Gene Transfer Vectors for Clinical Application be Justified?
Current Gene Therapy Proteasome Inhibition as a New Therapeutic Principle in Hematological Malignancies
Current Drug Targets Polyphenols: Biological Activities, Molecular Targets, and the Effect of Methylation
Current Molecular Pharmacology Recent Developments in the Field of Tumor-Inhibiting Metal Complexes
Current Pharmaceutical Design Novel Anticancer Agents and Targets: Recent Advances and Future Perspectives
Mini-Reviews in Medicinal Chemistry Ferroptosis: A Novel Mechanism of Artemisinin and its Derivatives in Cancer Therapy
Current Medicinal Chemistry Gene Therapy for Severe Combined Immunodeficiency due to Adenosine Deaminase Deficiency
Current Gene Therapy Nutritional Antioxidants and Adaptive Cell Responses: An Update
Current Molecular Medicine FHIT and p53 Status and Response to Platinum-Based Treatment in Advanced Non-Small Cell Lung Cancer
Current Cancer Drug Targets Analysis of the Salivary Microbiome in the Periodontal Disease Patients with Hypertension and Non-hypertension
Current Bioinformatics Anti-cancer and Other Bioactivities of Korean Angelica gigas Nakai (AGN) and Its Major Pyranocoumarin Compounds
Anti-Cancer Agents in Medicinal Chemistry Systemic Treatment of Chest Tumors: Highlighting Some Differences Between Eastern and Western Countries
Current Cancer Therapy Reviews The Renin-angiotensin System as a Target of Novel Anticancer Therapy
Current Pharmaceutical Design The Uses of Dimedone for the Synthesis of Thiophene, Thiazole and Annulated Derivatives with Antitumor, Pim-1 Kinase Inhibitions, PAINS Evaluations and Molecular Docking
Anti-Cancer Agents in Medicinal Chemistry Recent Patents of Gene Mutation Relative to JAK/STAT Pathway and Their Implication in Myeloproliferative Diseases
Recent Patents on DNA & Gene Sequences Therapeutic Boosting of the Immune Response: Turning to CD14 for Help
Current Pharmaceutical Biotechnology Interplay between Epigenetics & Cancer Metabolism
Current Pharmaceutical Design Tumor Specific Novel Taxoid-Monoclonal Antibody Conjugates
Current Medicinal Chemistry