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ID: ALA1156000

Journal: Bioorg Med Chem Lett

Title: Synthesis of 2alpha-substituted-14-epi-previtamin D3 and its genomic activity.

Authors: Sawada D, Katayama T, Tsukuda Y, Saito N, Takano M, Saito H, Takagi K, Ochiai E, Ishizuka S, Takenouchi K, Kittaka A.

Abstract: We synthesized and isolated 2 alpha-substituted analogs of 14-epi-previtamin D3 after thermal isomerization at 80 degrees C for the first time. The VDR binding affinity and transactivation activity of osteocalcin promoter in HOS cells were evaluated, and the 2 alpha-methyl-substituted analog was found to have greater genomic activity than 14-epi-previtamin D3.

CiteXplore: 19692243

DOI: 10.1016/j.bmcl.2009.07.112