Abstract
Background: Different 3-aroylpropionic acids and dihydropyrimidine hydrazine derivatives were condensed together to yield a series of dihydropyrimidine and pyridazinone hybrids (5a-u).
Objective: This was done in order to develop therapeutic agents for the treatment of breast cancer with improved Cycloxygenase-2 (COX-2) selectivity. In-vitro anticancer evaluation for these compounds was done against human breast cancer cell lines (MCF-7, MDA-MB-231) and normal human keratinocytes (HaCaT).
Conclusion: Amongst all the developed analogs, compound 5l emerged as the most potent agent against both these cell lines with IC50 values of 3.43 and 2.56 µM respectively. The synthesized compounds were also evaluated for COX-2 selectivity. To observe the binding pattern of the compounds with COX-2, a docking study was performed using PDB ID: 1CX2.
Keywords: Anticancer agent, breast cancer, COX-2 inhibitors, cyanopyrimidne, hybrid, pyridazinone.
Mini-Reviews in Medicinal Chemistry
Title:Synthesis of Hybrids of Dihydropyrimidine and Pyridazinone as potential Anti-Breast Cancer Agents
Volume: 18 Issue: 4
Author(s): Wasim Akhtar, Garima Verma, Mohemmed Faraz Khan, Mohammad Shaquiquzzaman, Arpana Rana, Tarique Anwer, Mymoona Akhter and M. Mumtaz Alam*
Affiliation:
- Drug Design and Medicinal Chemistry Lab, Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard, New Delhi 110062,India
Keywords: Anticancer agent, breast cancer, COX-2 inhibitors, cyanopyrimidne, hybrid, pyridazinone.
Abstract: Background: Different 3-aroylpropionic acids and dihydropyrimidine hydrazine derivatives were condensed together to yield a series of dihydropyrimidine and pyridazinone hybrids (5a-u).
Objective: This was done in order to develop therapeutic agents for the treatment of breast cancer with improved Cycloxygenase-2 (COX-2) selectivity. In-vitro anticancer evaluation for these compounds was done against human breast cancer cell lines (MCF-7, MDA-MB-231) and normal human keratinocytes (HaCaT).
Conclusion: Amongst all the developed analogs, compound 5l emerged as the most potent agent against both these cell lines with IC50 values of 3.43 and 2.56 µM respectively. The synthesized compounds were also evaluated for COX-2 selectivity. To observe the binding pattern of the compounds with COX-2, a docking study was performed using PDB ID: 1CX2.
Export Options
About this article
Cite this article as:
Akhtar Wasim, Verma Garima, Khan Faraz Mohemmed, Shaquiquzzaman Mohammad, Rana Arpana, Anwer Tarique, Akhter Mymoona and Alam Mumtaz M.*, Synthesis of Hybrids of Dihydropyrimidine and Pyridazinone as potential Anti-Breast Cancer Agents, Mini-Reviews in Medicinal Chemistry 2018; 18 (4) . https://dx.doi.org/10.2174/1389557517666170220153456
DOI https://dx.doi.org/10.2174/1389557517666170220153456 |
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
Mitochondria as a Therapeutic Target in Metabolic Disorders
Mitochondria are the primary site of adenosine triphosphate (ATP) production in mammalian cells. Moreover, these organelles are an important source of reactive oxygen and nitrogen species in virtually any nucleated cell type. The modulation of a myriad of cellular signaling pathways depends on the mitochondrial physiology. Mitochondrial dysfunction is observed ...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
- 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
-
Cucurbitacin IIb from Ibervillea sonorae Induces Apoptosis and Cell Cycle Arrest via STAT3 Inhibition
Anti-Cancer Agents in Medicinal Chemistry Biodistribution and Pharmacokinetics of I-131 Labelled 4- Iodophenylacetic Acid
Current Radiopharmaceuticals Thirty Years of Polyamine-Related Approaches to Cancer Therapy. Retrospect and Prospect. Part 1. Selective Enzyme Inhibitors
Current Drug Targets Human Multidrug Transporter ABCG2, a Target for Sensitizing Drug Resistance in Cancer Chemotherapy
Current Medicinal Chemistry The Typical Metabolic Modifiers Conferring Improvement in Cancer Resistance
Current Medicinal Chemistry From Ocean to Bedside: the Therapeutic Potential of Molluscan Hemocyanins
Current Medicinal Chemistry TRICOM Vector Based Cancer Vaccines
Current Pharmaceutical Design Exploring Cancer Therapeutics with Natural Products from African Medicinal Plants, Part I: Xanthones, Quinones, Steroids, Coumarins, Phenolics and other Classes of Compounds
Anti-Cancer Agents in Medicinal Chemistry Antiviral Immunotherapy for Mosquito-Borne Flaviviruses: A Review of Current Status
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Induced Fit Docking and Automated QSAR Studies Reveal the ER-α Inhibitory Activity of <i>Cannabis sativa</i> in Breast Cancer
Recent Patents on Anti-Cancer Drug Discovery Meet Our Executive Editor
Current Traditional Medicine Molecular Cytogenetics of Autism
Current Genomics Integrins and Cancer: Gene Expression, Epigenetics and Metastasis
Current Genomics Venoms and Poisonings during the Centuries: A Narrative Review
Endocrine, Metabolic & Immune Disorders - Drug Targets Mass Spectrometry Data Analysis in the Proteomics Era
Current Bioinformatics Sulforaphane Protects Small Intestinal Mucosa From Aspirin/NSAID-Induced Injury by Enhancing Host Defense Systems Against Oxidative Stress and by Inhibiting Mucosal Invasion of Anaerobic Enterobacteria
Current Pharmaceutical Design Calcium Metabolism & Hypercalcemia in Adults
Current Medicinal Chemistry FDG-PET/CT Predicts Outcome in Oropharingeal Carcinoma Patients Undergoing Intensity Modulated Radiation Therapy with Dose Escalation to FDG-avid Tumour Volumes
Current Radiopharmaceuticals Ghrelin and Motilin in the Gastrointestinal System
Current Pharmaceutical Design Heparan Sulphate as a Regulator of Leukocyte Recruitment in Inflammation
Current Protein & Peptide Science