Abstract
A series of 2-(3,4,5-trimethoxybenzoyl)-indol-3-yl acetic acid derivatives 2a-g and 3a-j were synthesized and the effects of all the compounds on human leukemia K562 cell growth were investigated. The results showed that the presence of one or more electron-donating methoxy groups at 7- or 5- and 7- positions of N-methyl indole ring, corresponding to compounds 3d and 3f, increased antiproliferative activity against K562 cells and induced the cell apoptosis. The results demonstrated that the methylation of the nitrogen atom of indole nucleus plays an important role for the antiproliferative activities. Replacing the 3,4,5-trimethoxybenzoyl functionality with a 3,4-dimethoxybenzoyl, 4- methoxybenzoy or benzoyl group (compounds 3h-j, respectively) yielded inactive compounds.
Keywords: 2-Aroylindole 3-acetic acid, Apoptosis, Anticancer agents
Letters in Drug Design & Discovery
Title: Synthesis and Biological Evaluation of a Series of 2-(3,4,5-Trimethoxybenzoyl)-Indol-3-yl Acetic Acid Derivatives as Potential Agents against Human Leukemia K562 Cells
Volume: 5 Issue: 3
Author(s): Romeo Romagnoli, Pier Giovanni Baraldi, Olga Cruz-Lopez, Maria Dora Carrion, Carlota Lopez Cara, Jan Balzarini, Enrica Fabbri and Robero Gambari
Affiliation:
Keywords: 2-Aroylindole 3-acetic acid, Apoptosis, Anticancer agents
Abstract: A series of 2-(3,4,5-trimethoxybenzoyl)-indol-3-yl acetic acid derivatives 2a-g and 3a-j were synthesized and the effects of all the compounds on human leukemia K562 cell growth were investigated. The results showed that the presence of one or more electron-donating methoxy groups at 7- or 5- and 7- positions of N-methyl indole ring, corresponding to compounds 3d and 3f, increased antiproliferative activity against K562 cells and induced the cell apoptosis. The results demonstrated that the methylation of the nitrogen atom of indole nucleus plays an important role for the antiproliferative activities. Replacing the 3,4,5-trimethoxybenzoyl functionality with a 3,4-dimethoxybenzoyl, 4- methoxybenzoy or benzoyl group (compounds 3h-j, respectively) yielded inactive compounds.
Export Options
About this article
Cite this article as:
Romagnoli Romeo, Baraldi Giovanni Pier, Cruz-Lopez Olga, Carrion Dora Maria, Cara Lopez Carlota, Balzarini Jan, Fabbri Enrica and Gambari Robero, Synthesis and Biological Evaluation of a Series of 2-(3,4,5-Trimethoxybenzoyl)-Indol-3-yl Acetic Acid Derivatives as Potential Agents against Human Leukemia K562 Cells, Letters in Drug Design & Discovery 2008; 5 (3) . https://dx.doi.org/10.2174/157018008784083983
DOI https://dx.doi.org/10.2174/157018008784083983 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
- 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
-
Development of a High Throughput Drug Screening Assay for the Detection of Changes in Tau Levels - Proof of Concept with HSP90 inhibitors
Current Alzheimer Research Chemopreventive Properties of Indole-3-Carbinol, Diindolylmethane and Other Constituents of Cardamom Against Carcinogenesis
Recent Patents on Food, Nutrition & Agriculture Microwave-Assisted Domino Cyclization Reactions
Current Microwave Chemistry Developments of Polo-like Kinase 1 (Plk1) Inhibitors as Anti-Cancer Agents
Mini-Reviews in Medicinal Chemistry Skp2 Inhibitors: Novel Anticancer Strategies
Current Medicinal Chemistry Influence of Dietary Substances on Intestinal Drug Metabolism and Transport
Current Drug Metabolism A Review on Exploring Better Safety Prospects in Managing Cancer using Liposomal Combinations of Food Bioactive Compounds and Anticancer Drugs: Combisomes
Current Drug Delivery Structure, Roles and Inhibitors of a Mitotic Protein Kinase Haspin
Current Medicinal Chemistry Mannosylated Solid Lipid Nanocarriers of Chrysin to Target Gastric Cancer: Optimization and Cell Line Study
Current Drug Delivery Evidence for Epigenetic Alterations in Turner Syndrome Opens up Feasibility of New Pharmaceutical Interventions
Current Pharmaceutical Design Current Trends in Cancer Biomarker Discovery Using Urinary Metabolomics: Achievements and New Challenges
Current Medicinal Chemistry Detection of Squamous Cell Carcinoma Antigen with Micro- and Nanogap Interdigitated Electrodes and Gold Nanoparticles
Micro and Nanosystems Microbicides for Prevention of Transmission of Sexually Transmitted Diseases
Current Pharmaceutical Design Novel Agents Targeting Bioactive Sphingolipids for the Treatment of Cancer
Current Medicinal Chemistry Luteolin, a Flavonoid with Potential for Cancer Prevention and Therapy
Current Cancer Drug Targets Flavonoids as Anticancer Agents: Structure-Activity Relationship Study
Current Medicinal Chemistry - Anti-Cancer Agents Emerging Multi-cancer Regulatory Role of ESRP1: Orchestration of Alternative Splicing to Control EMT
Current Cancer Drug Targets Editorial
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery The Novel RARβ Isoform (β 5) is a Potential Target of Retinoids in Breast Cancer
Current Cancer Drug Targets Biological Activity of Carotenoids: Its Implications in Cancer Risk and Prevention
Current Pharmaceutical Biotechnology