Abstract
Azetidin-2-one, a β -lactam four-membered heterocyclic ring is widely identified for its diverse medicinal properties. Ezetimibe a cholesterol absorption inhibitor and Aztreonam a potent cephalosporinase inhibitor proved the medicinal value of azetidin-2-ones. On the other hand marine bromopyrrole alkaloids are well known for their diverse biological significance. Hence twenty novel conjugates of azetidin-2-ones integrated with 4,5-dibromopyrrole motif were synthesized and screened for antineoplastic activity using MTT assay. Synthesized hybrids displayed good antineoplastic profile particularly towards breast cancer cell line MCF7, where hybrid 5e displayed maximum cytotoxicity (IC50 = 0.5 µM). The selective cytotoxicity displayed by these conjugates towards tested cancer cells with non-toxicity against normal human VERO cells indicated their potential for further antineoplastic drug development.
Keywords: Antineoplastic, azetidinone, bromopyrrole alkaloid, natural product.
Anti-Cancer Agents in Medicinal Chemistry
Title:Design and Synthesis of Novel Antineoplastic Agents Inspired from Marine Bromopyrrole Alkaloids
Volume: 15 Issue: 5
Author(s): Rajesh A. Rane, Pavan Kumar Bangalore, Shital S. Naphade, Harun M. Patel, Mahesh B. Palkar and Rajshekhar Karpoormath
Affiliation:
Keywords: Antineoplastic, azetidinone, bromopyrrole alkaloid, natural product.
Abstract: Azetidin-2-one, a β -lactam four-membered heterocyclic ring is widely identified for its diverse medicinal properties. Ezetimibe a cholesterol absorption inhibitor and Aztreonam a potent cephalosporinase inhibitor proved the medicinal value of azetidin-2-ones. On the other hand marine bromopyrrole alkaloids are well known for their diverse biological significance. Hence twenty novel conjugates of azetidin-2-ones integrated with 4,5-dibromopyrrole motif were synthesized and screened for antineoplastic activity using MTT assay. Synthesized hybrids displayed good antineoplastic profile particularly towards breast cancer cell line MCF7, where hybrid 5e displayed maximum cytotoxicity (IC50 = 0.5 µM). The selective cytotoxicity displayed by these conjugates towards tested cancer cells with non-toxicity against normal human VERO cells indicated their potential for further antineoplastic drug development.
Export Options
About this article
Cite this article as:
Rane A. Rajesh, Bangalore Kumar Pavan, Naphade S. Shital, Patel M. Harun, Palkar B. Mahesh and Karpoormath Rajshekhar, Design and Synthesis of Novel Antineoplastic Agents Inspired from Marine Bromopyrrole Alkaloids, Anti-Cancer Agents in Medicinal Chemistry 2015; 15 (5) . https://dx.doi.org/10.2174/1871520614666141203124745
DOI https://dx.doi.org/10.2174/1871520614666141203124745 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
- 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
-
Na<sup>+</sup>/K<sup>+</sup> ATPase Inhibitors in Cancer
Current Drug Targets Biomedical Potentialities of Taraxacum officinale-based Nanoparticles Biosynthesized Using Methanolic Leaf Extract
Current Pharmaceutical Biotechnology Regulation of Apoptosis and Cell Survival by Resveratrol
Mini-Reviews in Organic Chemistry Paclitaxel (Taxol) and Taxoid Derivates for Lung Cancer Treatment: Potential for Aerosol Delivery
Current Cancer Drug Targets Increasing Testosterone Levels and Effects on Cognitive Functions in Elderly Men and Women: A Review
Current Drug Targets - CNS & Neurological Disorders Cardiac Dys-Synchronization and Arrhythmia in Hyperhomocysteinemia
Current Neurovascular Research Phosphoinositide-3-kinases as the Novel Therapeutic Targets for the Inflammatory Diseases: Current and Future Perspectives
Current Drug Targets Advances in Systemic Therapy for Gastroenteropancreatic Neuroendocrine Malignancies
Current Clinical Pharmacology Inhibiting the Enzymes of the Endothelin and Renin-Angiotensin Systems in Cancer
Current Enzyme Inhibition HSF1, A Versatile Factor in Tumorogenesis
Current Molecular Medicine Targeting ATP7A to Increase the Sensitivity of Neuroblastoma Cells to Retinoid Therapy
Current Cancer Drug Targets Recent Advances in Predicting Functional Impact of Single Amino Acid Polymorphisms: A Review of Useful Features, Computational Methods and Available Tools
Current Bioinformatics Fluorinated Molecules as Drugs and Imaging Agents in the CNS
Current Topics in Medicinal Chemistry TEM8 Targeted Cancer Therapy
Anti-Cancer Agents in Medicinal Chemistry The Urokinase Receptor in the Central Nervous System
CNS & Neurological Disorders - Drug Targets Preparation, Characterization and <i>In Vitro</i> Biological Evaluation of Novel Curcumin Derivatives as Cytotoxic and Apoptosis-Inducing Agents
Anti-Cancer Agents in Medicinal Chemistry Four Major Factors Regulate Phosphatidylinositol 3-kinase Signaling Pathway in Cancers Induced by Infection of Human Papillomaviruses
Current Medicinal Chemistry The Potential Use of Peptides in Cancer Treatment
Current Protein & Peptide Science Nitroimidazole Radiopharmaceuticals in Hypoxia: Part II Cytotoxicity and Radiosensitization Applications
Current Radiopharmaceuticals Small Interfering RNA for Effective Cancer Therapies
Mini-Reviews in Medicinal Chemistry