Abstract
A series of novel 5-(substituted phenyl)-3-[(substituted phenylamino)methyl]-3H-[1,3,4]oxadiazole-2- thione derivatives were prepared and their in vitro cytotoxicity was evaluated against a panel of three cancer cell lines, namely, hepatocarcinoma HepG2, breast adenocarcinoma MCF-7, and leukemia HL-60 cells, using the widely accepted MTT assay. In general, the synthesized compounds displayed weak to moderate cytotoxic activity against the three tested cell lines. Compound 5a, which has trimethoxy substituents on both phenyl rings, exhibited the highest cytotoxic effect against all cell lines tested with IC50 values of 12.01, 7.52 and 9.7 μM against HepG2, MCF-7 and HL-60 cells, respectively. Mechanistic studies revealed that the test compounds showed a good inhibitory effect on cellular tubulin of hepatocellular carcinoma. Compound 5h was the most potent tubulin inhibitor in HepG2 cells, with 81.1 % inhibition of the original control tubulin. Moreover, the mechanism of tubulin polymerization inhibition was confirmed by immunofluorescence assay, flow cytometry, and docking study.
Keywords: Anticancer, immunofluorescence, 1, 3, 4-oxadiazole, tubulin.
Anti-Cancer Agents in Medicinal Chemistry
Title:1,3,4-oxadiazole-2-thione Derivatives; Novel Approach for Anticancer and Tubulin Polymerization Inhibitory Activities
Volume: 16 Issue: 2
Author(s): Mohamed Abdel-Aziz, Kamel A. Metwally, Amira M. Gamal-Eldeen and Omar M. Aly
Affiliation:
Keywords: Anticancer, immunofluorescence, 1, 3, 4-oxadiazole, tubulin.
Abstract: A series of novel 5-(substituted phenyl)-3-[(substituted phenylamino)methyl]-3H-[1,3,4]oxadiazole-2- thione derivatives were prepared and their in vitro cytotoxicity was evaluated against a panel of three cancer cell lines, namely, hepatocarcinoma HepG2, breast adenocarcinoma MCF-7, and leukemia HL-60 cells, using the widely accepted MTT assay. In general, the synthesized compounds displayed weak to moderate cytotoxic activity against the three tested cell lines. Compound 5a, which has trimethoxy substituents on both phenyl rings, exhibited the highest cytotoxic effect against all cell lines tested with IC50 values of 12.01, 7.52 and 9.7 μM against HepG2, MCF-7 and HL-60 cells, respectively. Mechanistic studies revealed that the test compounds showed a good inhibitory effect on cellular tubulin of hepatocellular carcinoma. Compound 5h was the most potent tubulin inhibitor in HepG2 cells, with 81.1 % inhibition of the original control tubulin. Moreover, the mechanism of tubulin polymerization inhibition was confirmed by immunofluorescence assay, flow cytometry, and docking study.
Export Options
About this article
Cite this article as:
Abdel-Aziz Mohamed, A. Metwally Kamel, Gamal-Eldeen M. Amira and Aly M. Omar, 1,3,4-oxadiazole-2-thione Derivatives; Novel Approach for Anticancer and Tubulin Polymerization Inhibitory Activities, Anti-Cancer Agents in Medicinal Chemistry 2016; 16 (2) . https://dx.doi.org/10.2174/1871520615666150907093855
DOI https://dx.doi.org/10.2174/1871520615666150907093855 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
Call for Papers in Thematic Issues
Induction of cell death in cancer cells by modulating telomerase activity using small molecule drugs
Telomeres are distinctive but short stretches present at the corners of chromosomes and aid in stabilizing chromosomal makeup. Resynthesis of telomeres supported by the activity of reverse transcriptase ribonucleoprotein complex telomerase. There is no any telomerase activity in human somatic cells, but the stem cells and germ cells undergone telomerase ...read more
Role of natural compounds as anti anti-cancer agents
Cancer is considered the leading cause of worldwide mortality, accounting for nearly 10 million deaths in 2022. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy remains an important approach in treatment o f several types of cancers, even though ...read more
Signaling and enzymatic modulators in cancer treatment
Cancer accounts for nearly 10 million deaths in 2022 and is considered the leading cause of worldwide mortality. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy, radiotherapy and surgery are the most important approach for the treatment of several ...read more
- 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
-
Survey of Functional Activities of Alpha-fetoprotein Derived Growth Inhibitory Peptides: Review and Prospects
Current Protein & Peptide Science Cause and Consequences of Genetic and Epigenetic Alterations in Human Cancer
Current Genomics Molecular Targets for Nutritional Preemption of Cancer
Current Cancer Drug Targets Future of Spermatogonial Stem Cell Culture: Application of Nanofiber Scaffolds
Current Stem Cell Research & Therapy Recent Clinical Aspects of Hyperprolactinemia Induced by Antipsychotics
Reviews on Recent Clinical Trials Aptamer-Mediated Cancer Gene Therapy
Current Gene Therapy Unraveling Progesterone-Induced Molecular Mechanisms in Physiological and Pathological Conditions
Current Clinical Pharmacology RNA Interference in Cancer: Targeting the Anti-Apoptotic Protein c-FLIP for Drug Discovery
Mini-Reviews in Medicinal Chemistry Risk Factors for Node Affectation and Recurrence in Endometrial Cancer
Current Women`s Health Reviews Subject Index To Volume 9
Combinatorial Chemistry & High Throughput Screening Epigenetics: Relations to Disease and Laboratory Findings
Current Medicinal Chemistry An Overview of Phytotherapeutic Approaches for the Treatment of Benign Prostatic Hyperplasia
Mini-Reviews in Medicinal Chemistry Current Perspectives on Novel Drug Delivery Systems and Approaches for Management of Cervical Cancer: A Comprehensive Review
Current Drug Targets microRNA Decay: Refining microRNA Regulatory Activity
MicroRNA Promises of Lipid-based Drug Delivery Systems in the Management of Breast Cancer
Current Pharmaceutical Design Cytotoxicity and Anti-proliferative Properties of Heterocyclic Compounds Derived from Progesterone
Anti-Cancer Agents in Medicinal Chemistry Pharmacological Inhibitors of Fatty Acid Synthase (FASN)-Catalyzed Endogenous Fatty Acid Biogenesis: A New Family of Anti-Cancer Agents?
Current Pharmaceutical Biotechnology Gene Therapy Targeting Nuclear Factor-κB: Towards Clinical Application in Inflammatory Diseases and Cancer
Current Gene Therapy Surgical Strategies for Fertility Preservation in Women with Cancer
Current Women`s Health Reviews Clinical Development of Microbicides for the Prevention of HIV Infection
Current Pharmaceutical Design