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
-
Should the Status of the Pathway Mediated by BRCA1 and BRCA2 be Evaluated Before Selecting Cancer Chemotherapy Drugs?
Current Pharmacogenomics Herb-drug Interactions Involving Drug Metabolizing Enzymes and Transporters
Current Drug Metabolism The Role of Vitamin D and Sunlight Incidence in Cancer
Anti-Cancer Agents in Medicinal Chemistry Advances in Regulating Tumorigenicity and Metastasis of Cancer Through TrkB Signaling
Current Cancer Drug Targets Use of Deoxyribozymes for Gene Knockdown
Medicinal Chemistry Reviews - Online (Discontinued) Vitamin, Mineral, and Drug Absorption Following Bariatric Surgery
Current Drug Metabolism Current Overview on the Usage of Poly(ADP-ribose)polymerase (PARP) Inhibitors in Treating Cancer
Clinical Cancer Drugs Relevance of Micrometastases and Targeting the Bone Marrow Niche with Zoledronic Acid in Breast Cancer
Current Cancer Therapy Reviews Traditional Chinese Medicine Remedy to Jury: The Pharmacological Basis for the Use of Shikonin as an Anticancer Therapy
Current Medicinal Chemistry Pyrimidinone Associated Triazole Carboxamides: Synthesis, Characterization, Cytotoxicity and DNA Binding Studies
Current Bioactive Compounds Editorial [Hot Topic: Anticancer Platinum Complexes - State of the Art and Future Prospects (Guest Editor: Markus Galanski)]
Anti-Cancer Agents in Medicinal Chemistry Targeted Therapy Towards Cancer-A Perspective
Anti-Cancer Agents in Medicinal Chemistry Thalidomide as an Immunotherapeutic Agent: The Effects on Neutrophil- Mediated Inflammation
Current Pharmaceutical Design Regulatory T-Cells: Immunomodulators in Health and Disease
Current Topics in Medicinal Chemistry Tissue Protective and Anti-Fibrotic Actions of Suramin: New Uses of an Old Drug
Current Clinical Pharmacology The NF-kB Pathway as a Potential Target for Autoimmune Disease Therapy
Current Pharmaceutical Design Synthesis and Cytotoxicities of 2-[4-hydroxy-(3,5-bis-aminomethyl)- benzylidene]-indan-1-ones
Letters in Drug Design & Discovery Network Pharmacology: Reigning in Drug Attrition?
Current Drug Discovery Technologies Comparative Proteomics Analysis of SKBR3 and MCF7 Breast Cancer Cell Lines Using Two Dimensional Electrophoresis: Ready to Build Postgenomics Capacity for OMICS R&D in Developing Countries?
Current Pharmacogenomics and Personalized Medicine Epigenetics in Clinical Management of Children and Adolescents with Brain Tumors
Current Cancer Drug Targets