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Issue 12, 2016
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Design and synthesis of 3-arylbenzopyran based non-steroidal vitamin-D3 mimics as osteogenic agents

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Abstract

3-Arylbenzopyran based non-steroidal osteogenic agents have been explored as structural templates of estrogen and vitamin-D3. The target molecules 18a–c, 19a–c, 26a–c, 27a–c and intermediates 17a–c and 25a–c were studied for their osteogenic activity in an osteoblast differentiation assay in vitro using mouse calvarial osteoblast cells. Compounds 25c, 26b, 27b and 27c effectively increased ALP activity at 1 pM concentration compared to the untreated cells. The active compounds were devoid of inherent toxicity at 1 pM concentration in osteoblast cells. The most active compound, 27b, was studied for mineralization of osteoblast cells and expression of marker genes, viz. BMP-2, RUNX-2 & Osx, involved in osteogenesis. Molecular docking analysis performed for 27b showed its possible interactions with estrogen receptor-α and -β (ER-α and ER-β) as well as the vitamin-D receptor (VDR).

Graphical abstract: Design and synthesis of 3-arylbenzopyran based non-steroidal vitamin-D3 mimics as osteogenic agents

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Publication details

The article was received on 16 Aug 2016, accepted on 28 Sep 2016 and first published on 29 Sep 2016


Article type: Research Article
DOI: 10.1039/C6MD00469E
Citation: Med. Chem. Commun., 2016,7, 2381-2394
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    Design and synthesis of 3-arylbenzopyran based non-steroidal vitamin-D3 mimics as osteogenic agents

    Mohd. I. Ahmad, D. S. Raghuvanshi, S. Singh, A. A. John, R. Prakash, K. S. Nainawat, D. Singh, S. Tripathi, A. Sharma and A. Gupta, Med. Chem. Commun., 2016, 7, 2381
    DOI: 10.1039/C6MD00469E

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