Synthesis and in vitro bone cell activity of analogues of the cyclohexapeptide dianthin G?
Organic & Biomolecular Chemistry Pub Date: 2016-05-27 DOI: 10.1039/C6OB00983B
Abstract
The cyclohexapeptide natural product dianthin G promotes osteoblast (bone-forming cell) proliferation in vitro at nanomolar concentrations, and is therefore considered a promising candidate for the treatment of osteoporosis. An Nα-methyl amide bond scan of dianthin G was performed to probe the effect of modifying amide bonds on osteoblast proliferation. In addition, to provide greater structural diversity, a series of dicarba dianthin G analogues was synthesised using ring closing metathesis. Dianthin G and one novel dicarba analogue increased the number of human osteoblasts and importantly they did not increase osteoclast (bone-resorbing cell) differentiation in bone marrow cells.
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Journal Name:Organic & Biomolecular Chemistry
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CAS no.: 89640-58-4