Advertisement

Topics

Design, synthesis and biological evaluation of 3,4-diaryl-1,2,5-oxadiazole-2/5-oxides as highly potent inhibitors of tubulin polymerization.

08:00 EDT 14th May 2019 | BioPortfolio

Summary of "Design, synthesis and biological evaluation of 3,4-diaryl-1,2,5-oxadiazole-2/5-oxides as highly potent inhibitors of tubulin polymerization."

Structure-activity relationships for rigid analogues of combretastatin A-4 (CA-4) were investigated, leading to the discovery of a series of 3,4-diaryl-1,2,5-oxadiazole-N-oxides. Among them, 7n' and 7n'' showed remarkable antiproliferative activities against three cancer cell lines in nanomolar concentrations. Interestingly, 7n' inhibited tubulin polymerization much more efficiently than CA-4. Cellular mechanism investigation elucidated 7n' disrupted the cellular microtubule structure, arrested cell cycle at G/M phase and induces apoptosis. Molecular modeling study revealed 1,2,5-oxadiazole-N-oxide ring could increase a hydrogen bond interaction with the binding site. These results provide impetus and further guidance for the development of new CA-4 analogues.

Affiliation

Journal Details

This article was published in the following journal.

Name: European journal of medicinal chemistry
ISSN: 1768-3254
Pages: 287-296

Links

DeepDyve research library

PubMed Articles [23814 Associated PubMed Articles listed on BioPortfolio]

Design, synthesis and biological evaluation of 2-(phenoxymethyl)-5-phenyl-1,3,4-oxadiazole derivatives as anti-breast cancer agents.

Structural based molecular docking approach revealed the findings of 2-(phenoxymethyl) -5-phenyl-1,3,4-oxadiazole derivatives. The compounds (7a-o) were synthesized and characterized well by using con...

Synthesis, antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety.

Tuberculosis is the infectious disease caused by mycobacterium tuberculosis (Mtb), responsible for the utmost number of deaths annually across the world. Herein, twenty-one new substituted 1,2,4-oxadi...

1,2,4-Oxadiazole-5-ones as analogues of tamoxifen: synthesis and biological evaluation.

A series of 2,3,4-triaryl-substituted 1,2,4-oxadiazole-5-ones have been prepared as fixed-ring analogues of tamoxifen (TAM), a drug inhibitor of Estradiol Receptor (ER) used in breast cancer therapy, ...

Design, synthesis, in vivo, and in silico evaluation of new coumarin-1,2,4-oxadiazole hybrids as anticonvulsant agents.

A novel series of coumarin-1,2,4-oxadiazole hybrids were designed, synthesized, and evaluated as anticonvulsant agents. The title compounds were easily synthesized from reaction of appropriate coumari...

Correction to "Short Total Synthesis of Δ-Prostaglandin J and Related Prostaglandins. Design, Synthesis, and Biological Evaluation of Macrocyclic Δ-Prostaglandin J Analogues".

Clinical Trials [6455 Associated Clinical Trials listed on BioPortfolio]

Redox Determinants in Severe Asthma

Hypotheses: 1) Airway pH regulation is abnormal in severe asthma; 2) In severe asthma, there is formation of cytotoxic nitrogen oxides and loss of beneficial nitrogen oxides in the airways

Magnetic Resonance Imaging (MRI) for Aortic Dissection to Visualise Inflammation

The study is a single-centre, prospective, observational cross-sectional imaging study aimed to determine if macrophage-mediated inflammation can be visualised in the aorta of patients wit...

Comparison of Time-restricted Feeding and Continuous Feeding in Critically Ill Patients

In the nutrition guideline (A.S.P.E.N guideline), there was no recommendation about the feeding type in enteral feeding of critically ill patients. Continuous feeding is the most popular f...

A Study Evaluating the Effects of Lipid Lowering Treatment on Steroid Synthesis

Cholesterol is the precursor of glucocorticoids, mineralocorticoids and sex steroids. Both adrenal and non-adrenal (ovarian + testicular) all steroid hormones are primarily synthesized usi...

Effects of Oral Supplementation of Arginine, Zinc and Vitamin C on Collagen Synthesis in Inguinal Hernia Patients

Collagen synthesis is depressed systemically in the immediate postoperative period. Arginine, zinc and vitamin C impact collagen synthesis. The aim of this study is to investigate the eff...

Medical and Biotech [MESH] Definitions

A field of biological research combining engineering in the formulation, design, and building (synthesis) of novel biological structures, functions, and systems.

Binary compounds of oxygen containing the anion O(2-). The anion combines with metals to form alkaline oxides and non-metals to form acidic oxides.

An approach, process, or methodology which emphasizes credible evidence and the best available scientific knowledge, judiciously integrated to achieve the best possible outcomes in structural design. For example, the design of a new OUTPATIENT CLINIC might incorporate a review of published research on outpatient clinic design, decisions on similar past projects, along with interviews with staff and consumers.

Oxides of a ring compound having atoms other than carbon in its ring.

Inorganic oxides of sulfur.

Advertisement
Quick Search
Advertisement
Advertisement

 


DeepDyve research library

Relevant Topics

Biological Therapy
Biological therapy involves the use of living organisms, substances derived from living organisms, or laboratory-produced versions of such substances to treat disease. Some biological therapies for cancer use vaccines or bacteria to stimulate the body&rs...

Cancer Disease
Cancer is not just one disease but many diseases. There are more than 100 different types of cancer. Most cancers are named for the organ or type of cell in which they start - for example, cancer that begins in the colon is called colon cancer; cancer th...


Searches Linking to this Article