Table of Contents
ISRN Urology
Volume 2011 (2011), Article ID 301490, 9 pages
Review Article

Novel Vitamin D Analogs for Prostate Cancer Therapy

1Boston University School of Medicine, Room M-1022, 715 Albany Street, Boston, MA 02118, USA
2Faculty of Pharmaceutical Sciences, Teikyo University, Midori-ku, Sagamihara, Kanagawa 252-5195, Japan

Received 15 May 2011; Accepted 3 June 2011

Academic Editors: A. M. El-Assmy, T. Nelius, K. Pummer, and F. Staerman

Copyright © 2011 Tai C. Chen and Atsushi Kittaka. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.


Prostate cells contain specific receptors for 1 ๐›ผ ,25-dihydroxyvitamin D [1 ๐›ผ ,25(OH)2D] or calcitriol, the active form of vitamin D. 1 ๐›ผ ,25(OH)2D is known to inhibit the proliferation and invasiveness of prostate cancer cells. These findings support the use of 1 ๐›ผ ,25(OH)2D for prostate cancer therapy. However, 1 ๐›ผ ,25(OH)2D can cause hypercalcemia, analogs of 1 ๐›ผ ,25(OH)2D that are less calcemic but exhibit potent antiproliferative activity would be attractive as therapeutic agents. To accomplish these goals, different strategies, based on metabolism, molecular mechanism of actions, and structural modeling, have been taken to modify the structure of vitamin D molecule with the aims to improve the efficacy and decrease the toxicity of vitamin D to treat different diseases. During the past four decades, over 3,000 analogs have been synthesized. In this paper, we discuss the development and the biological analysis of a unique class of vitamin D analogs with a substitution at the carbon 2 of 19-nor-1 ๐›ผ ,25(OH)2D3 molecule for potential application to the prevention and treatment of prostate cancer as well as other cancers.