Synthesis and evaluation of new coumarin–pyridine hybrids with promising anti-osteoporotic activities
| Autor: | K. Bhaskara Rao, Ram K. Modukuri, Dharmendra Choudhary, Ritu Trivedi, Vikram Khedgikar, Manoj Kumar, Koneni V. Sashidhara |
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| Rok vydání: | 2013 |
| Předmět: |
Male
Pyridines ALIZARIN RED Mineralization (biology) Mice Structure-Activity Relationship chemistry.chemical_compound Coumarins Osteogenesis Drug Discovery medicine Animals MTT assay Gene Pharmacology Osteoblasts Bone Density Conservation Agents Dose-Response Relationship Drug Molecular Structure Chemistry Organic Chemistry Cell Differentiation Osteoblast General Medicine Coumarin Staining medicine.anatomical_structure Biochemistry Osteoporosis Alkaline phosphatase Female |
| Zdroj: | European Journal of Medicinal Chemistry. 70:802-810 |
| ISSN: | 0223-5234 |
| DOI: | 10.1016/j.ejmech.2013.10.060 |
| Popis: | Anti-osteoporotic effects of the newly synthesized coumarin–pyridine hybrids were evaluated in primary cultures of rat calvarial osteoblasts in vitro. Compounds 6a , i , j and k were potent in stimulating osteoblast differentiation and mineralization as assessed by the alkaline phosphatase production and alizarin red-S staining assay, respectively. These compounds were also found to be nontoxic in osteoblast cells as compared to the control group in an MTT assay. Furthermore, the effect of these compounds on the transcript levels of osteogenic genes revealed that the compound 6j robustly enhanced mineralization of the osteogenic genes in calvarial osteoblasts. In this context, compound 6j was selected as a potential lead for further structural optimization in the development of new anti-osteoporotic agents. |
| Databáze: | OpenAIRE |
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