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.
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http://dx.doi.org/10.1016/j.ejmech.2013.10.060 | DOI Listing |
Front Chem
June 2022
The Institute of Pharmaceutical Sciences (TIPS), Tehran University of Medical Sciences, Tehran, Iran.
Anal Chem
June 2022
Hefei National Laboratory for Physical Science at Microscale, iChem, University of Science and Technology of China, Hefei230051, P. R. China.
Various suborganelles are delimited by lipid bilayers, in which high spatial and temporal morphological changes are essential to many physiological and pathological processes of cells. However, almost all the amphiphilic fluorescent molecules reported until now are not available for in situ precise tracking of membrane dynamics in cell apoptosis. Here, the MO (coumarin pyridine derivatives) was devised by engineering lipophilic coumarin and cationic pyridine salt, which not only lastingly anchored onto the plasma membrane in dark due to appropriate amphipathicity and electrostatic interactions but also in situ reflected the membrane damage and heterogeneity with secretion of extracellular vesicles (EVs) under reactive oxygen species regulation and was investigated by two-photon fluorescence lifetime imaging microscopy.
View Article and Find Full Text PDFSpectrochim Acta A Mol Biomol Spectrosc
February 2022
Department of Organic and Biomolecular Chemistry, Ural Federal University, Mira 19, Ekaterinburg 620002, Russian Federation; Institute of Organic Synthesis, Ural Branch of the Russian Academy of Sciences, Kovalevskoy 22, Ekaterinburg 620219, Russian Federation.
A series of coumarin-pyridine-based push-pull fluorophores were prepared starting from 1,2,4-triazines by using direct C-H functionalization (S-reaction)-Diels-Alder-retro Diels-Alder domino reaction sequence. This efficient synthetic strategy allowed to obtain a series of 19 coumarin-pyridine fluorophores. Their photophysical properties were studied.
View Article and Find Full Text PDFEur J Med Chem
September 2014
Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, (CSIR-CDRI), BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, P.O. Box 173, Lucknow 226031, India. Electronic address:
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.
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