Abstract
Seven novel 3-(1-(2-(2,7a-dihydrobenzo[d]thiazol-2-ylthio)acetyl)-5-substituted-phenyl-4,5-dihydro-1Hpyrazol- 3-yl)-2H-chromen-2-one derivatives were synthesized and characterized by 1H NMR and 13 C NMR. All of the compounds have been screened for their anticancer activity. The bioassay tests show that compound 4g exhibited potentially high activity against human gastric cancer cell SGC-7901 with IC50 value of 6.99±1.10 μg/mL. Docking simulation was performed to position compound 4g into the telomerase (3DU6) active site to determine the probable binding model.
Keywords: Coumarins, Dihydropyrazole, Molecular Docking, Anticancer activity, Telomerase, chromosomal integrity, 3DU6, gastric SGC-7901, dihydropyrazole heterocycle, Claisen-Schmidt, mother liquor, column chromatography, Cytotoxic Assay, Colorless crystals
Letters in Drug Design & Discovery
Title: Novel 3-(1-(2-(2,7a-dihydrobenzo[d]thiazol-2-ylthio)acetyl)-5-substitutedphenyl-4,5-dihydro-1H-pyrazol-3-yl)-Coumarins: Synthesis and Anticancer Activity
Volume: 9 Issue: 2
Author(s): Xian-Hai Lv, Xiu-Li Zhang, Xin-Hua Liu and Lei Shi
Affiliation:
Keywords: Coumarins, Dihydropyrazole, Molecular Docking, Anticancer activity, Telomerase, chromosomal integrity, 3DU6, gastric SGC-7901, dihydropyrazole heterocycle, Claisen-Schmidt, mother liquor, column chromatography, Cytotoxic Assay, Colorless crystals
Abstract: Seven novel 3-(1-(2-(2,7a-dihydrobenzo[d]thiazol-2-ylthio)acetyl)-5-substituted-phenyl-4,5-dihydro-1Hpyrazol- 3-yl)-2H-chromen-2-one derivatives were synthesized and characterized by 1H NMR and 13 C NMR. All of the compounds have been screened for their anticancer activity. The bioassay tests show that compound 4g exhibited potentially high activity against human gastric cancer cell SGC-7901 with IC50 value of 6.99±1.10 μg/mL. Docking simulation was performed to position compound 4g into the telomerase (3DU6) active site to determine the probable binding model.
Export Options
About this article
Cite this article as:
Lv Xian-Hai, Zhang Xiu-Li, Liu Xin-Hua and Shi Lei, Novel 3-(1-(2-(2,7a-dihydrobenzo[d]thiazol-2-ylthio)acetyl)-5-substitutedphenyl-4,5-dihydro-1H-pyrazol-3-yl)-Coumarins: Synthesis and Anticancer Activity, Letters in Drug Design & Discovery 2012; 9 (2) . https://dx.doi.org/10.2174/157018012799079743
DOI https://dx.doi.org/10.2174/157018012799079743 |
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
-
Carbohydrate based Potential Chemotherapeutic Agents: Recent Developments and their Scope in Future Drug Discovery
Mini-Reviews in Medicinal Chemistry Immunomodulation in Inflammatory Neuropathies: Rationale and Safety
Current Drug Safety Genetic Mechanisms and Aberrant Gene Expression during the Development of Gastric Intestinal Metaplasia and Adenocarcinoma
Current Genomics Naturally Occurring Hydroxytyrosol: Synthesis and Anticancer Potential
Current Medicinal Chemistry Global Gastrointestinal Safety Profile of Etoricoxib and Lumiracoxib
Current Pharmaceutical Design Recent Patents on Thiazole Derivatives Endowed with Antitumor Activity
Recent Patents on Anti-Cancer Drug Discovery COVID-19 Invades Several Important Organs other than the Lungs: Organs Crosstalk
Coronaviruses Clinical Signs, Prevention and Treatment of Viral Infections in Infants
Infectious Disorders - Drug Targets PET Imaging to Monitor Cancer Therapy
Current Pharmaceutical Biotechnology Targeting Vesicle Trafficking: An Important Approach to Cancer Chemotherapy
Recent Patents on Anti-Cancer Drug Discovery Editorial [Hot Topic: Benefits, Problems and Alternatives to COX-2 Inhibition (Guest Editor: Angel Lanas)]
Current Topics in Medicinal Chemistry MicroRNAs Regulate the Epithelial to Mesenchymal Transition (EMT) in Cancer Progression
MicroRNA Synthesis and Cytotoxicity Assessment of Novel 7-O- and 14-O-Derivatives of Glaucocalyxin A
Anti-Cancer Agents in Medicinal Chemistry Role of Moving Average Analysis for Development of Multi-Target (Q)SAR Models
Mini-Reviews in Medicinal Chemistry Monoclonal Antibodies in Cancer Therapy
Current Medicinal Chemistry - Anti-Cancer Agents Epigenetic Mechanism Involved in the HBV/HCV-Related Hepatocellular Carcinoma Tumorigenesis
Current Pharmaceutical Design Structural Patterning Used for Polyfunctional Devices in Diagnostics and for the Delivery of Therapeutics
Recent Patents on Materials Science The Impact of Asymmetric Dimethylarginine (ADAMA), the Endogenous Nitric Oxide (NO) Synthase Inhibitor, to the Pathogenesis of Gastric Mucosal Damage
Current Pharmaceutical Design Synthesis and Evaluation of Glycyrrhetic Acid-aromatic Hybrids as Anti-inflammatory Agents
Medicinal Chemistry The Finely Regulating Well-defined Functional Polymeric Nanocarriers for Anti-tumor Immunotherapy
Mini-Reviews in Medicinal Chemistry