Design, synthesis, quantum chemical studies and biological activity evaluation of pyrazole-benzimidazole derivatives as potent Aurora A/B kinase inhibitors.

03:33 EST 29th November 2014 | BioPortfolio

Summary of "Design, synthesis, quantum chemical studies and biological activity evaluation of pyrazole-benzimidazole derivatives as potent Aurora A/B kinase inhibitors."

Novel pyrazole-benzimidazole derivatives have been designed and synthesized. The entire target compounds were determined against cancer cell lines U937, K562, A549, LoVo and HT29 and were screened for Aurora A/B kinase inhibitory activity in vitro. The compounds 7a, 7b, 7i, 7k and 7l demonstrated significant cancer cell lines and Aurora A/B kinase inhibitory activities. Molecular modeling studies suggested the derivatives have bound in the active site of Aurora A kinase through the formation of four hydrogen bonds. Quantum chemical studies were carried out on these compounds to understand the structural features essential for activity. The cellular activity of 7k was also tested by immunofluorescence.

Affiliation

School of Pharmacy, Xuzhou Medical College, Xuzhou 221004, China.

Journal Details

This article was published in the following journal.

Name: Bioorganic & medicinal chemistry letters
ISSN: 1464-3405
Pages: 3523-30

Links

PubMed Articles [43651 Associated PubMed Articles listed on BioPortfolio]

Rational Design, Synthesis and Biological Evaluation of Modular Fluorogenic Substrates with High Affinity and Selectivity for PTP1B.

Protein-tyrosine phosphatase 1B (PTP1B) is a key regulatory enzyme in several signal transduction pathways, and its upregulation has been associated with type-2 diabetes, obesity and cancer. Selective...

Synthesis and pharmacological evaluation of pyrazolopyrimidopyrimidine derivatives: anti-inflammatory agents with gastroprotective effect in rats.

We report the synthesis of new anti-inflammatory 1,7-dihydropyrazolo[3',4':4,5]pyrimido[1,6-a]pyrimidine 5 from aminocyanopyrazole. All compounds were characterized by physical, chemical and spectral ...

Review: three synthesis methods of CdX (X = Se, S or Te) quantum dots.

Quantum dots (QDs) are one of the first nanotechnologies to be integrated with the biological sciences that used for imaging or tracking macromolecules/cells in cell/tissue. Because of QDs are importa...

Design, Synthesis, Biological Screening and Molecular Docking Studies of Piperazine-Derived Constrained Inhibitors of DPP-IV for the Treatment of Type 2 Diabetes.

Novel piperazine-derived conformationally constrained compounds were designed, synthesized, and evaluated for in vitro Dipeptidyl peptidase-IV (DPP-IV) inhibitory activities. From a library of compoun...

N-Arylated-Lactam-Type Iminosugars as New Immunosuppressive Agents: Discovery, Optimization, and Biological Evaluation.

We have previously described the discovery of N-alkylated iminosugars that showed immunosuppressive activity both in vitro and in vivo. Herein, we report the synthesis and biological evaluation of...

Clinical Trials [4084 Associated Clinical Trials listed on BioPortfolio]

Intramedullary Fixation of Humerus Fractures Without Intramedullary Reaming

The purpose of the study is to evaluate the safety and efficacy of the composite Nail - the Quantum interlocking intramedullary nailing system in the reduction of humeral fractures.

Estimate of the Activity and the Forecast of the Lupus Disease of the Adult by a Transcriptomic Score (STUDY LU-PUCE)

Lupus erythematosus systemic is an auto-immune disease the evaluation of the activity of which remains very difficult because of an heterogeneousness of the clinical and biological symptom...

Magnetic Therapy in Migraine Prophylaxis

Background: The therapy with pulsed electromagnetic fields (PEFs) has been used as a therapeutic modality for at least 40 years. However, their effect in the migraine prophylaxis is unclea...

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...

Evaluation of Tranilast to Treat Pterygium Before Excision

Recurrent or secondary pterygium often has often a growing fibrovascular tissue more exuberant than the primary. Histological findings differ from the primary, since the typical changes in...

Medical and Biotech [MESH] Definitions

Studies determining the effectiveness or value of processes, personnel, and equipment, or the material on conducting such studies. For drugs and devices, CLINICAL TRIALS AS TOPIC; DRUG EVALUATION; and DRUG EVALUATION, PRECLINICAL are available.

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

Nanometer sized fragments (the dots) of semiconductor crystalline material which emit PHOTONS. The wavelength is based on the quantum confinement size of the dot. They are brighter and more persistent than organic chemical INDICATORS. They can be embedded in MICROBEADS for high throughput ANALYTICAL CHEMISTRY.

Studies designed to assess the efficacy of programs. They may include the evaluation of cost-effectiveness, the extent to which objectives are met, or impact.

Works consisting of studies determining the effectiveness or utility of processes, personnel, and equipment.

Search BioPortfolio:
Loading
Advertisement

Relevant Topic

Cancer
Latest News Clinical Trials Research Drugs Reports Corporate
Cancer is a condition where cells in a specific part of the body grow and reproduce uncontrollably. The cancerous cells can invade and destroy surrounding healthy tissue, including organs.  Cancer sometimes begins in one part of the body before spre...

Advertisement

Searches Linking to this Article