Abstract
Background: Due to the importance of 1,3,4-thiadiazoles and phthalimides in anticancer agents, a novel series of 1,3,4-thiadiazole-phthalimide system have been synthesized and evaluated in vitro against HT-29 and MCF-7 human cancer cell lines.
Methods: The target compounds were prepared through four-step reaction and their cytotoxicities were evaluated by MTT assay. Results: The results showed that 4-nitrobenzoyl moiety containing derivatives are the most potent ones. The morphological evaluation also indicated that these compounds are apoptotic inducers. Conclusion: 4-Nitro-N-(5-((3-(1,3-dioxoisoindolin-2-yl)propyl)thio)-1,3,4-thiadiazol-2-yl)benzamide (8m) exhibits the best inhibitory effect against HT-29 and MCF-7 cell lines with IC50 values of 23.83 and 27.21 μM, respectively.Keywords: Cancer, anticancer agents, 1, 3, 4-thiadiazole, phthalimide, anticancer agents, treatment.
Letters in Drug Design & Discovery
Title:Synthesis and Biological Evaluation of 1,3,4-Thiadiazole Linked Phthalimide Derivatives as Anticancer Agents
Volume: 14 Issue: 10
Author(s): Zahra Rezaei, Setareh Moghimi, Rezvan Javaheri, Mehdi Asadi, Mohammad Mahdavi, Shabnam Shabani, Najmeh Edraki, Omidreza Firuzi, Maliheh Safavi, Mohsen Amini, Ali Asadipour, Elnaz Zeinalzadeh, Loghman Firoozpour and Alireza Foroumadi*
Affiliation:
- Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran,Iran
Keywords: Cancer, anticancer agents, 1, 3, 4-thiadiazole, phthalimide, anticancer agents, treatment.
Abstract: Background: Due to the importance of 1,3,4-thiadiazoles and phthalimides in anticancer agents, a novel series of 1,3,4-thiadiazole-phthalimide system have been synthesized and evaluated in vitro against HT-29 and MCF-7 human cancer cell lines.
Methods: The target compounds were prepared through four-step reaction and their cytotoxicities were evaluated by MTT assay. Results: The results showed that 4-nitrobenzoyl moiety containing derivatives are the most potent ones. The morphological evaluation also indicated that these compounds are apoptotic inducers. Conclusion: 4-Nitro-N-(5-((3-(1,3-dioxoisoindolin-2-yl)propyl)thio)-1,3,4-thiadiazol-2-yl)benzamide (8m) exhibits the best inhibitory effect against HT-29 and MCF-7 cell lines with IC50 values of 23.83 and 27.21 μM, respectively.Export Options
About this article
Cite this article as:
Rezaei Zahra, Moghimi Setareh , Javaheri Rezvan, Asadi Mehdi, Mahdavi Mohammad, Shabani Shabnam, Edraki Najmeh, Firuzi Omidreza, Safavi Maliheh, Amini Mohsen, Asadipour Ali, Zeinalzadeh Elnaz , Firoozpour Loghman and Foroumadi Alireza*, Synthesis and Biological Evaluation of 1,3,4-Thiadiazole Linked Phthalimide Derivatives as Anticancer Agents, Letters in Drug Design & Discovery 2017; 14 (10) . https://dx.doi.org/10.2174/1570180814666170127164759
DOI https://dx.doi.org/10.2174/1570180814666170127164759 |
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
-
Molecular Determinants of Chronic Liver Disease as Studied by NMR-Metabolomics
Current Topics in Medicinal Chemistry Synthesis, Characterization, Anticancer and Antibacterial Activity of Some Novel Pyrano[2,3-d]pyrimidinone Carbonitrile Derivatives
Anti-Cancer Agents in Medicinal Chemistry Development of Peptide and Protein Based Radiopharmaceuticals
Current Pharmaceutical Design Synthesis of Some Novel 4-(Arylideneamino)-N'-((2-chloro-8-methylquinolin- 3-yl)methylene)-3-phenyl-2-thioxo-2,3-dihydrothiazole-5-carbohydrazides as Potential Antimicrobial Agents
Letters in Drug Design & Discovery Essential Attributes Identified in the Design of a Laboratory Information Management System for a High Throughput siRNA Screening Laboratory
Combinatorial Chemistry & High Throughput Screening The Challenges Involved in Modeling Toxicity Data In Silico: A Review
Current Pharmaceutical Design The Changing Role of Radiation in the Post-TME ERA of Rectal Cancer
Current Cancer Therapy Reviews Characterization of Phosphorylated Proteins Using Mass Spectrometry
Current Protein & Peptide Science Progress in Small Molecule Therapeutics for the Treatment of Retinoblastoma
Mini-Reviews in Medicinal Chemistry A Hybrid Discrete Imperialist Competition Algorithm for Gene Selection for Microarray Data
Current Proteomics Biodegradable Composite Scaffolds: A Strategy to Modulate Stem Cell Behaviour
Recent Patents on Drug Delivery & Formulation The Association of Chemotherapy and Radiotherapy in Squamous Cell Carcinoma of Anal Canal
Current Drug Therapy Separation Media in Affinity Chromatography of Proteins - A Critical Review
Current Proteomics HR-MAS NMR Spectroscopy: A Practical Guide for Natural Samples
Current Organic Chemistry MicroRNAs-based Therapy: A Novel and Promising Strategy for Cancer Treatment
MicroRNA 2, 7-Diarylidene-cycloheptanone, Hydrazonoyl Chlorides and Heterocyclic Amines as Precursors for Synthesis of Bioactive new Fused Cycloheptapyrimidine Derivatives
Current Organic Synthesis Vascular and Cardiac Oxidative Stress and Inflammation as Targets for Cardioprotection
Current Pharmaceutical Design Design of Lanthanide Complex Probes for Highly Sensitive Time-Resolved Fluorometric Detection Methods and Its Application to Biochemical, Environmental and Clinical Analyses
Current Analytical Chemistry Synthesis of Aminoalkoxy Substituted 4,5-Diphenylisoxazole Derivatives as Potential Anti-osteoporotic Agents
Medicinal Chemistry Targeting Anti-Cancer Active Compounds: Affinity-Based Chromatographic Assays
Current Pharmaceutical Design