Potent 19-norvitamin D analogs for prostate and liver cancer therapy

Atsushi Kittaka, Akihiro Yoshida, Kun Chun Chiang, Masashi Takano, Daisuke Sawada, Toshiyuki Sakaki, Tai C. Chen

Research output: Contribution to journalReview articlepeer-review

23 Citations (Scopus)


The active form of vitamin D3, 1α,25(OH)2D 3 or calcitriol, is known to inhibit the proliferation and invasiveness of many types of cancer cells, including prostate and liver cancer cells. These findings support the use of 1α,25(OH)2D 3 for prostate and liver cancer therapy. However, 1α,25(OH)2D3 can cause hypercalcemia, thus, analogs of 1α,25(OH)2D3 that are less calcemic but exhibit potent antiproliferative activity would be attractive as therapeutic agents. We have developed 2α-functional group substituted 19-norvitamin D3 analogs with and without 14-epimerization. Among them, 2α- and 2β-(3-hydroxypropyl)-1α,25-dihydroxy-19-norvitamin D3 (MART-10 and -11, respectively) and 14-epi-2α- and 14-epi-2β-(3- hydroxypropyl)-1α,25-dihydroxy-19-norvitamin D3 (14-epi-MART-10 and 14-epi-MART-11, respectively) were found to be the most promising. In this review, we discuss the synthesis of this unique class of vitamin D analogs, the molecular mechanism of anticancer actions of vitamin D, and the biological evaluation of these analogs for potential application to the prevention and treatment of prostate and liver cancer.

Original languageEnglish
Pages (from-to)2049-2065
Number of pages17
JournalFuture Medicinal Chemistry
Issue number16
Publication statusPublished - Oct 2012
Externally publishedYes

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology
  • Drug Discovery


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