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 |
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
-
Leptin Plasma Levels in the General Population: Influence of Age, Gender, Body Weight and Medical History
Protein & Peptide Letters Mapping the High Throughput SEREX Technology Screening for Novel Tumor Antigens
Combinatorial Chemistry & High Throughput Screening Targeting Histone Onco- Modifications Using Plant-Derived Products
Current Drug Targets An Emerging Molecular Target in Melanoma: Cellular Carbonyl Stress and the Inhibition of Mitochondrial Survival Pathways by Carbonyl Scavenger Agents
Current Cancer Therapy Reviews Synthesis of Aryl-Substituted Naphthalenoids as Potent Topoisomerase Inhibitors
Medicinal Chemistry Cyclopeptides from Marine Organisms
Mini-Reviews in Organic Chemistry Hedgehog Signaling and Urological Cancers
Current Drug Targets Antiproliferative and Antioxidant Potential of Leaf and Leaf Derived Callus Extracts of Aerva lanata (L.) Juss. Ex Schult. Against Human Breast Cancer (MCF-7) Cell Lines
The Natural Products Journal Protein Geranylgeranyltransferase Type 1 as a Target in Cancer
Current Cancer Drug Targets Rhein Derivatives, A Promising Pivot?
Mini-Reviews in Medicinal Chemistry Remote Ischemic Conditioning Improves Cognitive Function During Cerebral Vascular Injury Through the Induction of Autophagy
Current Neurovascular Research The Antitumor Effects of Icaritin Against Breast Cancer is Related to Estrogen Receptors
Current Molecular Medicine A Systematic Evaluation of Solubility Enhancing Excipients to Enable the Generation of Permeability Data for Poorly Soluble Compounds in Caco-2 Model
Drug Metabolism Letters Prodigiosins as Anti Cancer Agents: Living Upto Their Name
Current Pharmaceutical Design Bee Venom: Its Potential Use in Alternative Medicine
Anti-Infective Agents Current Clinical Applications of In Vivo Magnetic Resonance Spectroscopy and Spectroscopic Imaging
Current Medical Imaging Anti-Cancer Effects of a New Docosahexaenoic Acid Monoacylglyceride in Lung Adenocarcinoma
Recent Patents on Anti-Cancer Drug Discovery Integrins as Novel Drug Targets for Overcoming Innate Drug Resistance
Current Cancer Drug Targets The Cell-Type Specificity and Endosomal Escape of Cell-Penetrating Peptides
Current Pharmaceutical Design Nanostructured Cubosomes as a Platform for Oral Drug Delivery
Current Pharmaceutical Biotechnology