Modeling and Toxicity Profiling of a Set of Quinoline Derivatives as c-MET Inhibitors in the treatment of Human Tumors.

Objectives: 4-(2-fluorophenoxy) quinoline derivatives constitute one of the chemical classes of hepatocyte growth factor receptor (c-MET) inhibitors, a promising treatment against various human tumors. There are three aims of the present study: (1) To develop a robust and validated quantitative structure-activity relationship model to predict the c-Met kinase inhibition; (2) to examine the toxicity profiles of these compounds; (3) to design new quinoline derivatives and apply the developed model on these compounds to observe its pertinence.

Materials And Methods: A multiple linear regression method was used to develop the model with calculated descriptors.

Piperazine and piperidine-substituted 7-hydroxy coumarins for the development of anti-inflammatory agents.

Coumarins (2H-1-benzopyran-2-one), derivatives that can be isolated from several plants, have been reported for their anticoagulant, antimicrobial, anti-inflammatory, or anticancer activity. Some of these structures are currently approved for the treatment of cardiovascular diseases, as antibiotics or as an anticancer drug. Given the great potential of this structure and the limited number of studies that focus on molecules derived from carbon 8 of the benzopyranone heterocycle, we synthesized in this project 38 coumarin derivatives by substituting carbon 8 of the benzopyran ring with some aromatic and aliphatically substituted piperidines and piperazines.

Do We Build Similar Molecules for Comorbid Diseases? in Drug Design, an Analysis for Depression and Inflammation.

designates two poets coincidently writing a same verse in the Ottoman Divan literature. This study aims to analyze the structural similarity of molecules independently designed for inflammation and depression to determine if coincidentally we are building similar molecules for comorbid diseases. For this purpose, a molecule library was first constituted with structures that were developed as anti-inflammatory (AI) and antidepressant (AD) agents these last decades.

A Quantitative Curriculum Mapping of the Faculty of Pharmacy of Yeditepe University, Turkey: A Process to Assess the Consistency of a Curriculum with the Mission and Vision of an Institution and National Requirements.

The changing role of the pharmacist led to some improvements of pharmacy education worldwide these last years. Curricula have evolved and the content-based education has been converted into a competency-based education. The definition of a global practice-based competency framework by the International Pharmaceutical Federation (FIP) and the European Pharmacy Competencies Framework by the European the Quality Assurance in European Pharmacy Education and Training (PHAR-QA) project helps Universities to keep in with these changes.

Novel 8-Substituted Coumarins That Selectively Inhibit Human Carbonic Anhydrase IX and XII.

A novel series of 8-substituted coumarin-based compounds, characterized by the presence of alkylpiperazine and arylpiperazine chains, were synthesized and tested for their inhibitory activity against four human carbonic anhydrase (CA) isoforms. All compounds displayed nanomolar potency against the cancer-related CA IX and CA XII; moreover, they were shown to be devoid of any inhibitory activity toward the cytosolic CA I and CA II up to 10 µM concentration in the assay system. Therefore, the synthesized coumarin ligands demonstrated to be potent and selective CA IX/XII inhibitors, and were shown to be as potent as the reference inhibitor acetazolamide against CA XII, with single-digit nanomolar values.