Abstract
In search of novel cytotoxic agents based on acridone scaffold, twenty five derivatives of acridone-2- carboxamide were synthesized and evaluated against a panel of eleven cancer cell lines by using MTT assay. Amides, A5 and A8 (IC50 = 0.3 µM) exhibited good cytotoxicity against MCF7. Compound A22 (IC50 = 4.3 µM) was found to be selectively cytotoxic against cancer cell line MCF7 and KB403. Particularly, promising cytotoxic activities were shown by amides A6 (IC50 = 0.7 µM), A16 (IC50 = 6.3 µM), A8 (IC50 = 0.9 µM ), A21 (IC50 = 1.3 µM), A5 (IC50 = 2.9 µM), A8 (IC50 = 2.8 µM), A14 (IC50 = 0.8 µM), A9 (IC50 = 0.8 µM) and A8 (IC50 = 0.4 µM) against cell lines; PA1, WRL68, CaCO2, TK-10, K-562, PC-3, HOP-92, ECV-304 and UACC-257, respectively. The favorable cytotoxic profile and non-toxicity towards normal human cells displayed by the derivative revealed their potential for further anticancer drug developments.
Keywords: Acridone amides, anticancer, cytotoxicity, MTT assay, tricyclic compounds.
Anti-Cancer Agents in Medicinal Chemistry
Title:Synthesis of Novel Amides Based on Acridone Scaffold with Interesting Antineoplastic Activity
Volume: 15 Issue: 5
Author(s): Anand A. Mahajan, Rajesh A. Rane, Anish A. Amritkar, Shital S. Naphade, Pankaj B. Miniyar, Pavan Kumar Bangalore and Rajshekhar Karpoormath
Affiliation:
Keywords: Acridone amides, anticancer, cytotoxicity, MTT assay, tricyclic compounds.
Abstract: In search of novel cytotoxic agents based on acridone scaffold, twenty five derivatives of acridone-2- carboxamide were synthesized and evaluated against a panel of eleven cancer cell lines by using MTT assay. Amides, A5 and A8 (IC50 = 0.3 µM) exhibited good cytotoxicity against MCF7. Compound A22 (IC50 = 4.3 µM) was found to be selectively cytotoxic against cancer cell line MCF7 and KB403. Particularly, promising cytotoxic activities were shown by amides A6 (IC50 = 0.7 µM), A16 (IC50 = 6.3 µM), A8 (IC50 = 0.9 µM ), A21 (IC50 = 1.3 µM), A5 (IC50 = 2.9 µM), A8 (IC50 = 2.8 µM), A14 (IC50 = 0.8 µM), A9 (IC50 = 0.8 µM) and A8 (IC50 = 0.4 µM) against cell lines; PA1, WRL68, CaCO2, TK-10, K-562, PC-3, HOP-92, ECV-304 and UACC-257, respectively. The favorable cytotoxic profile and non-toxicity towards normal human cells displayed by the derivative revealed their potential for further anticancer drug developments.
Export Options
About this article
Cite this article as:
Mahajan A. Anand, Rane A. Rajesh, Amritkar A. Anish, Naphade S. Shital, Miniyar B. Pankaj, Bangalore Kumar Pavan and Karpoormath Rajshekhar, Synthesis of Novel Amides Based on Acridone Scaffold with Interesting Antineoplastic Activity, Anti-Cancer Agents in Medicinal Chemistry 2015; 15 (5) . https://dx.doi.org/10.2174/1871520614666141130130130
DOI https://dx.doi.org/10.2174/1871520614666141130130130 |
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
-
γ-Hydroxybutenolide Containing Marine Natural Products and Their Synthesis: A Review
Current Organic Chemistry Aberrant Splicing, Hyaluronan Synthases and Intracellular Hyaluronan as Drivers of Oncogenesis and Potential Drug Targets
Current Cancer Drug Targets Phytochemicals to Prevent Inflammation and Allergy
Recent Patents on Inflammation & Allergy Drug Discovery Females Live Longer than Males: Role of Oxidative Stress
Current Pharmaceutical Design Mediterranean Dietary Traditions for the Molecular Treatment of Human Cancer: Anti-Oncogenic Actions of the Main Olive Oils Monounsaturated Fatty Acid Oleic Acid (18:1n-9)
Current Pharmaceutical Biotechnology Colorectal Carcinogensis and Suppression of Tumor Development by Inhibition of Enzymes and Molecular Targets
Current Enzyme Inhibition Discovery of Potent Natural-Product-Derived SIRT2 Inhibitors Using Structure- Based Exploration of SIRT2 Pharmacophoric Space Coupled With QSAR Analyses
Anti-Cancer Agents in Medicinal Chemistry Leptin, Estrogens and Cancer
Mini-Reviews in Medicinal Chemistry Clinical Strategies for the Blockade of IL-18 in Inflammatory Bowel Diseases
Current Drug Targets Future Prospects for Targeted Alpha Therapy
Current Radiopharmaceuticals A Brief Survey on Computational Approaches to Reveal Drug and Disease Associations
Current Drug Discovery Technologies New Issues for Copper-64: from Precursor to Innovative Pet Tracers in Clinical Oncology
Current Radiopharmaceuticals Editorial (Thematic Issue: Advances with microRNAs in Tumorigenesis and Cancer Therapy)
Current Pharmaceutical Design Botulinum Toxin: Pharmacology and Clinical Developments: A Literature Review
Medicinal Chemistry The Therapeutic Impact of Manipulating Microbiota in Inflammatory Bowel Disease
Current Pharmaceutical Design Intestinal Barrier Dysfunction in Human Pathology and Aging
Current Pharmaceutical Design Editorial [Peptides and Proteins in Cancer Therapy]
Protein & Peptide Letters Role of Serum and Glucocorticoid-Inducible Kinase (SGK)-1 in Senescence: A Novel Molecular Target Against Age-Related Diseases
Current Medicinal Chemistry Anti-cancer and Other Bioactivities of Korean Angelica gigas Nakai (AGN) and Its Major Pyranocoumarin Compounds
Anti-Cancer Agents in Medicinal Chemistry Phosphotyrosine Phosphatases in Cancer Diagnostic and Treatment
Recent Patents on DNA & Gene Sequences