A series of amide derivatives of stilbene was synthesized and investigated for osteogenic activity. Out of sixteen, seven compounds viz19c, 19g, 19i, 24b, 25a, 25c and 26a showed significant osteoblast differentiation within 1 pM-1 µM concentrations. Amongst all, 26a was identified as most active molecule which presented effective mineralization of osteoblasts and expression of mRNA of osteogenic marker gene such as BMP-2, ALP, and Runx-2 at 1 pM. In estrogen-deficient balb/c mice, 26a showed significant osteogenic activity at 5 mg-kg-1 body weight dose. The protein expression study for estrogen receptors α and β (ER-α & ER-β) using mouse calvarial osteoblasts (MCOs) and molecular docking analyses showed preferential expression of ER-β by 26a indicating the possibility of ER-β mediated osteogenic activity of 26a.

中文翻译：

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sti的酰胺衍生物诱导的成骨细胞分化：可能的成骨剂。

合成了一系列的1,2-二苯乙烯酰胺衍生物，并研究了其成骨活性。在十六种化合物中，七种化合物viz19c，19g，19i，24b，25a，25c和26a在1 pM-1 µM浓度范围内显示出明显的成骨细胞分化。其中，26a被认为是最活跃的分子，在成骨细胞中有效矿化并以1 pM表达成骨标记基因（如BMP-2，ALP和Runx-2）的mRNA。在雌激素缺乏的balb / c小鼠中，26a在5 mg-kg-1体重剂量下显示出显着的成骨活性。使用小鼠颅骨成骨细胞（MCO）对雌激素受体α和β（ER-α和ER-β）的蛋白质表达研究以及分子对接分析显示，26a优先表达ER-β，表明ER-β介导的成骨活性的可能性26a。