Abstract
A series of hybrids of 3-hydroxy-indolin-2-one and 2,3-dihydroquinolin-4(1H) -one were synthesized and their anti-proliferative activities against two human cancer cell lines were initially evaluated. Compound 7g was selected for further study and demonstrated moderate anti-proliferative activities against four human cancer cell lines. Meanwhile, 7g had inhibitory effects on the growth of SGC-7901 cells in dosage-and time-dependent manners and the cancer cells appeared morphological changes. Moreover, 7g was more effective in the inhibition of xenografted tumor in vivo growth and mice treated with 7g showed more weight gain than 5-FU-treated mice over the treatment period, suggesting a lower toxic effect than 5-FU. After treatment with 7g, the tumor showed typical morphological changes as evaluated by H&E staining.
Keywords: 3-Hydroxy-indolin-2-one, 2, 3-Dihydroquinolin-4(1H)-one, anticancer, hybrid, isatin, synthesis.
Letters in Drug Design & Discovery
Title:Synthesis, in Vitro and in Vivo Anticancer Activity of Hybrids of 3- Hydroxy-indolin-2-one and 2,3-Dihydroquinolin-4(1H)-one
Volume: 12 Issue: 2
Author(s): Lei Zhang, Jing Wang, Wen-Yun Li, Juan Xia, Jing Gao and Qi-Zheng Yao
Affiliation:
Keywords: 3-Hydroxy-indolin-2-one, 2, 3-Dihydroquinolin-4(1H)-one, anticancer, hybrid, isatin, synthesis.
Abstract: A series of hybrids of 3-hydroxy-indolin-2-one and 2,3-dihydroquinolin-4(1H) -one were synthesized and their anti-proliferative activities against two human cancer cell lines were initially evaluated. Compound 7g was selected for further study and demonstrated moderate anti-proliferative activities against four human cancer cell lines. Meanwhile, 7g had inhibitory effects on the growth of SGC-7901 cells in dosage-and time-dependent manners and the cancer cells appeared morphological changes. Moreover, 7g was more effective in the inhibition of xenografted tumor in vivo growth and mice treated with 7g showed more weight gain than 5-FU-treated mice over the treatment period, suggesting a lower toxic effect than 5-FU. After treatment with 7g, the tumor showed typical morphological changes as evaluated by H&E staining.
Export Options
About this article
Cite this article as:
Zhang Lei, Wang Jing, Li Wen-Yun, Xia Juan, Gao Jing and Yao Qi-Zheng, Synthesis, in Vitro and in Vivo Anticancer Activity of Hybrids of 3- Hydroxy-indolin-2-one and 2,3-Dihydroquinolin-4(1H)-one, Letters in Drug Design & Discovery 2015; 12 (2) . https://dx.doi.org/10.2174/1570180811666140909010017
DOI https://dx.doi.org/10.2174/1570180811666140909010017 |
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
-
Intracellular Restriction Factors In Mammalian Cells - An Ancient Defense System Finds A Modern Foe
Current HIV Research The Future of Collateral Artery Research
Current Cardiology Reviews Telomeres, Telomerase and Malignant Transformation
Current Molecular Medicine Gold Nanoparticles - Synthesis and Applications in Cancer Management
Recent Patents on Materials Science Brain Perfusion SPECT with Brodmann Areas Analysis in Differentiating Frontotemporal Dementia Subtypes
Current Alzheimer Research Genetic and Modifying Factors that Determine the Risk of Brain Tumors
Central Nervous System Agents in Medicinal Chemistry Inorganic Phosphate as a Signaling Molecule: A Potential Strategy in Osteosarcoma Treatment
Current Pharmaceutical Design The PIK3CA Gene as a Mutated Target for Cancer Therapy
Current Cancer Drug Targets DNA-Binding Properties of Poly(ADP-Ribose) Polymerase: A Target for Anti-Cancer Therapy
Current Drug Targets Chemical Modifications and Biological Activities of Polysaccharides
Current Drug Targets Editorial (Thematic Issue: Chemoresistance in Gynecologic Cancers)
Current Cancer Therapy Reviews Pathophysiology and Biomarkers for Breast Cancer: Management Using Herbal Medicines
Current Nutrition & Food Science From Bacteria to Antineoplastic: Epothilones A Successful History
Anti-Cancer Agents in Medicinal Chemistry Vulvar Leiomyomatosis: A Diagnostic Challenge Case Report
Current Women`s Health Reviews The Use of Adenoviral Vectors for Genetic Manipulation and Analysis of Primitive Hematopoietic Cells
Current Gene Therapy Inactivated- or Killed-Virus HIV/AIDS Vaccines
Current Drug Targets - Infectious Disorders The Molecular Pathology of Eye Tumors: A 2019 Update Main Interests for Routine Clinical Practice
Current Molecular Medicine Biotransformation of Endocrine Disrupting Compounds by Selected Phase I and Phase II Enzymes – Formation of Estrogenic and Chemically Reactive Metabolites by Cytochromes P450 and Sulfotransferases
Current Medicinal Chemistry CNS Drug Delivery Systems: Novel Approaches
Recent Patents on Drug Delivery & Formulation Viruses and Oral Cancer: Crossreactivity as a Potential Link
Anti-Cancer Agents in Medicinal Chemistry