Therapeutic potential of the 2-alkyl and 2-alkylidene-19-nor-(20S)-modified analogs of 1alpha,25-dihydroxyvitamin D3

The Journal of Steroid Biochemistry and Molecular Biology
Hector F DeLuca

Abstract

Five analogs of 19-nor-1alpha,25-dihydroxyvitamin D(3) are described that show highly selective and potent activities. The 2-methylene-19-nor-(20S)-1alpha25-dihydroxyvitamin D(3) (2MD) and its 2alpha-methyl sister are selectively active on the osteoblast. 2MD is bone anabolic and causes bone formation in vivo and in vitro and is being developed as a therapy for bone loss diseases such as osteoporosis. 2-Methylene-19-nor (20S)-bishomo-1alpha-hydroxypregnacalciferol (2BMP) has no activity on calcium in vivo while totally suppressing circulating parathyroid hormone. Its homologs, i.e. 2-methylene-19-nor-1alpha-hydroxy-homopregnacalciferol (2MP) and 2-methylene-19-nor-1alpha-hydroxypregnacalciferol (2MPC) act similarly but are either less selective (2MP) or not as potent (2MPC). These abbreviated side chain analogs will be developed for diseases where a rise in serum calcium is not desired, as for example, cancer, renal osteodystrophy, psoriasis and autoimmune diseases.

References

Oct 11, 2002·Proceedings of the National Academy of Sciences of the United States of America·Nirupama K ShevdeHector F DeLuca
Jan 10, 2003·Journal of Cellular Biochemistry·Tatsuo SudaToshimasa Shinki
May 20, 2003·Kidney International. Supplement·Eduardo SlatopolskyAlex Brown

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Citations

Jul 20, 2005·The Journal of Steroid Biochemistry and Molecular Biology·Matthew D Griffin, Rajiv Kumar
Feb 3, 2006·Natural Product Reports·James R Hanson
Aug 2, 2005·The Journal of Steroid Biochemistry and Molecular Biology·Daniel M AlbertHector F DeLuca
Jun 22, 2013·ChemMedChem·Can-Fei ZhangZhao-Peng Liu

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