Cancer chemoprevention using natural vitamin D and synthetic analogs

K. Z. Guyton, T. W. Kensler, G. H. Posner

Research output: Contribution to journalReview articlepeer-review

94 Scopus citations


Substantial epidemiologic data support a role for vitamin D in cancer prevention. However, dose-limiting hypercalcemic effects have proved a major obstacle to the development of natural vitamin D as a cancer chemopreventive. Structure-activity studies have sought to disassociate the toxicities and chemopreventive activities of vitamin D, and a number of synthetic deltanoids (vitamin D analogs) have shown considerable promise in this regard. Several such compounds have chemopreventive efficacy in preclinical studies, as does natural vitamin D. Data supporting further development of agents of this class include in vitro and in vivo evidence of antiproliferative, proapoptotic, prodifferentiating and antiangiogenic activities. Ongoing studies are aimed at further defining the molecular mechanisms through which vitamin D and synthetic deltanoids affect gene expression and cellular fate. Additional efforts are focused on establishing the chemopreventive index (efficacy vs toxicity) of each synthetic deltanoid.

Original languageEnglish (US)
Pages (from-to)421-442
Number of pages22
JournalAnnual Review of Pharmacology and Toxicology
StatePublished - 2001
Externally publishedYes


  • 1α,25-dihydroxyvitamin D analogs
  • Calcitriol analogs
  • Deltanoids
  • Hybrid deltanoids
  • Noncalcemic deltanoids

ASJC Scopus subject areas

  • Toxicology
  • Pharmacology


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