Abstract
The present anticancer research demands more potent anticancer agents with fewer side effects than the existing ones. A series of novel substituted thiazole and benzothiazole containing nitrogen mustards (5-8; 15-17; 22-23) were synthesized and the structures of the compounds were analyzed by IR, NMR and mass spectras. Their in-vitro cytotoxicity against human lung carcinoma (A549) was investigated by MTT Assay. The compounds 16, 8 showed promising activity against A549 human lung carcinoma cell lines with % CPI 52 (More than Cisplatin) and 45.9 respectively. The DNA binding properties of the compounds were also evaluated based on their affinity or intercalation with CT-DNA measured with absorption titration. The compounds 22 and 5 showed the highest binding affinity with binding constant (Ki) 48.34 and 41.8 respectively.
Keywords: Anticancer activity, Benzothiazoles, Cytotoxicity, DNA binding, Nitrogen mustards, Thiazoles, recrystallized, diethanolamine, triethylamine, TLC plates, over anhydrous magnesium sulphate, scaffolds, aryl hydrocarbon receptor (AhR), TNF-a, 1H NMR
Letters in Drug Design & Discovery
Title: Thiazole Containing Nitrogen Mustards: Synthesis, Structural Evaluation, Cytotoxicity and DNA Binding Studies
Volume: 8 Issue: 9
Author(s): Nulgulmnalli Manjunathiah Raghavendra, Surampudi Renuka, Sayan Dutta Gupta and Pingili Divya
Affiliation:
Keywords: Anticancer activity, Benzothiazoles, Cytotoxicity, DNA binding, Nitrogen mustards, Thiazoles, recrystallized, diethanolamine, triethylamine, TLC plates, over anhydrous magnesium sulphate, scaffolds, aryl hydrocarbon receptor (AhR), TNF-a, 1H NMR
Abstract: The present anticancer research demands more potent anticancer agents with fewer side effects than the existing ones. A series of novel substituted thiazole and benzothiazole containing nitrogen mustards (5-8; 15-17; 22-23) were synthesized and the structures of the compounds were analyzed by IR, NMR and mass spectras. Their in-vitro cytotoxicity against human lung carcinoma (A549) was investigated by MTT Assay. The compounds 16, 8 showed promising activity against A549 human lung carcinoma cell lines with % CPI 52 (More than Cisplatin) and 45.9 respectively. The DNA binding properties of the compounds were also evaluated based on their affinity or intercalation with CT-DNA measured with absorption titration. The compounds 22 and 5 showed the highest binding affinity with binding constant (Ki) 48.34 and 41.8 respectively.
Export Options
About this article
Cite this article as:
Manjunathiah Raghavendra Nulgulmnalli, Renuka Surampudi, Dutta Gupta Sayan and Divya Pingili, Thiazole Containing Nitrogen Mustards: Synthesis, Structural Evaluation, Cytotoxicity and DNA Binding Studies, Letters in Drug Design & Discovery 2011; 8 (9) . https://dx.doi.org/10.2174/157018011797200830
DOI https://dx.doi.org/10.2174/157018011797200830 |
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
-
BMPS and Liver: More Questions than Answers
Current Pharmaceutical Design Mechanisms of the Penetration of Blood-Borne Substances into the Brain
Current Neuropharmacology Thrombotic Microangiopathy and Occult Neoplasia
Cardiovascular & Hematological Disorders-Drug Targets Targeting Oncogenes and Tumor Suppressors genes to Mitigate Chemoresistance
Current Cancer Drug Targets Heat Shock Protein 90 – a Potential Target in the Treatment of Human Acute Myelogenous Leukemia
Current Cancer Drug Targets Targeting DNA Minor Groove by Hybrid Molecules as Anticancer Agents
Current Medicinal Chemistry Role of Imaging in Testicular Cancer
Current Medical Imaging Curcumin Pellets of Carboxymethylated Tamarind Seed Polysaccharide for the Treatment of Inflammatory Bowel Disease
Drug Delivery Letters The Application of Natural Products in Cancer Therapy by Targeting Apoptosis Pathways
Current Drug Metabolism The Role of Image Guided Radiotherapy in the Treatment of Soft Tissue Sarcoma
Current Cancer Therapy Reviews Recent Advances in Oral Pulsatile Drug Delivery
Recent Patents on Drug Delivery & Formulation Selective Estrogen Receptor Modulators. Current and Future Treatment Options for Osteoporosis
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery Diagnosis, Pathogenesis and Therapeutic Targets in Amyotrophic Lateral Sclerosis
CNS & Neurological Disorders - Drug Targets NBN Polymorphysms and Cancer Susceptibility: A Systematic Review
Current Genomics Design, Synthesis, and Biological Evaluation of Novel C5-Modified Pyrimidine Ribofuranonucleosides as Potential Antitumor or/and Antiviral Agents
Medicinal Chemistry Cardiac Toxicity of Antineoplastic Anthracyclines
Current Medicinal Chemistry - Anti-Cancer Agents Naturally-occurring Dimers of Flavonoids as Anticarcinogens
Anti-Cancer Agents in Medicinal Chemistry Roles of Secreted Phospholipases A<sub>2</sub> in the Mammalian Immune System
Protein & Peptide Letters An Overview of Bioactive Peptides for in vivo Imaging and Therapy in Human Diseases
Mini-Reviews in Medicinal Chemistry Carbonic Anhydrase Inhibitors and the Management of Cancer
Current Topics in Medicinal Chemistry