Abstract
A novel series of hybrids of indolin-2-one and quinazolin-4(3H)-one linked via an imine bond were synthesized and tested for their inhibitory activity against the proliferation of a panel of five human cancer cell lines. We found that compound 5c bearing 5-bromo substituent at the indolin-2-one ring exhibited weak cytotoxic activity with percentages of inhibition ranging from 27% to 49% at 20 μM, while its counterpart 7c having 4-methoxybenzyl group at the N1-position of indolin-2-one ring was more active with percentages of inhibition in range of 32-63%. These results indicate that the presence of a bromo substituent at the 5-position and a 4-methoxybenzyl group at the N1-position of indolin-2-one ring is important for the cytotoxic activity.
Keywords: Antitproliferative activity, Hybrid, Indolin-2-one, Quinazolin-4(3H)-one, Synthesis, gastrointestinal stromal tumor, Nolatrexed, 2-Methylquinazolin, nitroquinazolin, MTT Assay
Letters in Drug Design & Discovery
Title:Synthesis and Antiproliferative Evaluation of Hybrids of Indolin-2-one and Quinazoline-4(3H)-one Linked via Imine Bond
Volume: 10 Issue: 1
Author(s): Wei-Yao Wu, Sheng-Li Cao, Bei-Bei Mao, Ji Liao, Zhong-Feng Li, Hao-Bin Song and Xingzhi Xu
Affiliation:
Keywords: Antitproliferative activity, Hybrid, Indolin-2-one, Quinazolin-4(3H)-one, Synthesis, gastrointestinal stromal tumor, Nolatrexed, 2-Methylquinazolin, nitroquinazolin, MTT Assay
Abstract: A novel series of hybrids of indolin-2-one and quinazolin-4(3H)-one linked via an imine bond were synthesized and tested for their inhibitory activity against the proliferation of a panel of five human cancer cell lines. We found that compound 5c bearing 5-bromo substituent at the indolin-2-one ring exhibited weak cytotoxic activity with percentages of inhibition ranging from 27% to 49% at 20 μM, while its counterpart 7c having 4-methoxybenzyl group at the N1-position of indolin-2-one ring was more active with percentages of inhibition in range of 32-63%. These results indicate that the presence of a bromo substituent at the 5-position and a 4-methoxybenzyl group at the N1-position of indolin-2-one ring is important for the cytotoxic activity.
Export Options
About this article
Cite this article as:
Wu Wei-Yao, Cao Sheng-Li, Mao Bei-Bei, Liao Ji, Li Zhong-Feng, Song Hao-Bin and Xu Xingzhi, Synthesis and Antiproliferative Evaluation of Hybrids of Indolin-2-one and Quinazoline-4(3H)-one Linked via Imine Bond, Letters in Drug Design & Discovery 2013; 10 (1) . https://dx.doi.org/10.2174/1570180811309010061
DOI https://dx.doi.org/10.2174/1570180811309010061 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
![](/images/wayfinder.jpg)
- 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
-
Strategies for the Preparation of Bifunctional Gadolinium(III) Chelators
Current Organic Synthesis Genus Euonymus: Chemical and Pharmacological Perception
Mini-Reviews in Organic Chemistry The Putative Adverse Effects of Bisphenol A on Autoimmune Diseases
Endocrine, Metabolic & Immune Disorders - Drug Targets An Integrative Systems Analysis of High-grade Glioma Cell Lines: TLRs, Wnt, BRCA1, Netrins, STXBP1 and MDH1 Provide Putative Molecular Targets for Therapeutic Intervention
Current Pharmacogenomics and Personalized Medicine It is All About Proteases: From Drug Delivery to In Vivo Imaging and Photomedicine
Current Medicinal Chemistry The Use of Intravenous Aminobisphosphonates for the Treatment of Pagets Disease of Bone
Mini-Reviews in Medicinal Chemistry Strategies for Non-Invasive Molecular Imaging of Acute Allograft Rejection by Gamma Scintigraphy and Positron Emission Tomography
Current Radiopharmaceuticals Immune Checkpoint Inhibitor Therapy and Risk of Myocarditis: A Review of the Literature
Current Immunology Reviews (Discontinued) Interleukin-18: Biology and Role in the Immunotherapy of Cancer
Current Medicinal Chemistry Anti-angiogenic Drug Resistance: Roles and Targeting of Non-coding RNAs (microRNAs and long non-coding RNAs)
Current Molecular Pharmacology Interaction of Human Brain Acetylcholinesterase with Cyclophosphamide: A Molecular Modeling and Docking Study
CNS & Neurological Disorders - Drug Targets New Derivatives of GnRH as Potential Anticancer Therapeutic Agents
Current Medicinal Chemistry Recent Developments in Structural Proteomics: From Protein Identifications and Structure Determinations to Protein-Protein Interactions
Current Proteomics Recent Advances in Molecular Modeling and Medicinal Chemistry Aspects of Phospho-Glycoprotein&#
Current Drug Metabolism Advantages of Multidetector CT Cystoscopy in the Detection of Bladder Tumors
Current Medical Imaging Biology of Protooncogene c-kit Receptor and Spermatogenesis
Current Pharmacogenomics Novel Drugs Targeting Microtubules: the Role of Epothilones
Current Pharmaceutical Design Nanocarriers Conjugated with Cell Penetrating Peptides: New Trojan Horses by Modern Ulysses
Current Pharmaceutical Biotechnology In Vitro and In Vivo Sirolimus for Modulation of Allogeneic Hematopoietic Stem Cell Transplantation
Current Medicinal Chemistry - Immunology, Endocrine & Metabolic Agents Efficacy of Bacteria in Cancer Immunotherapy: Special Emphasis on the Potential of Mycobacterial Species
Clinical Cancer Drugs