Antitumor properties of diastereomeric and geometric analogs of vitamin D3

Anticancer Drugs. 2007 Apr;18(4):447-57. doi: 10.1097/CAD.0b013e3280143166.


Analogs of 1,25-dihydroxyvitamin D3 with a reversed configuration at C-1 or C-24 and E or Z geometry of the double bond at C-22 in the side chain or at C-5 in the triene system were examined for their antiproliferative activity in vitro against a spectrum of various human cancer cell lines. The analogs coded PRI-2201 (calcipotriol), PRI-2202 and PRI-2205, such as calcitriol and tacalcitol (used as a referential agents), revealed antiproliferative activity against human HL-60, HL-60/MX2, MCF-7, T47D, SCC-25 and mouse WEHI-3 cancer cell lines. The toxicity studies in vivo showed that PRI-2202 and PRI-2205 are less toxic than referential agents. Even at total doses of 2.5-5.0 mg/kg distributed during 5 successive days, no changes in body weight were observed. Calcitriol and tacalcitol showed toxicity in the same protocol at 100 times lower doses. Calcipotriol was lethal to all mice after administration of a total dose of 5.0 mg/kg. The analog PRI-2205 appeared to be more active in mouse Levis lung cancer tumor growth inhibition than calcitriol, calcipotriol or PRI-2202. This analog did not reveal calcemic activity at doses which inhibit tumor growth in vivo nor at higher doses.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology*
  • Antineoplastic Agents / toxicity
  • Breast Neoplasms / drug therapy
  • Breast Neoplasms / pathology
  • CD11b Antigen / metabolism
  • Calcitriol / analogs & derivatives
  • Calcitriol / pharmacology
  • Calcium / blood
  • Carcinoma, Lewis Lung / drug therapy
  • Carcinoma, Lewis Lung / pathology
  • Cell Cycle / drug effects
  • Cell Differentiation / drug effects
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Cholecalciferol / analogs & derivatives*
  • Cholecalciferol / pharmacology*
  • Cholecalciferol / toxicity
  • Coloring Agents
  • Female
  • Fibroblasts / metabolism
  • HL-60 Cells
  • Humans
  • Lipopolysaccharide Receptors / metabolism
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Mice, Inbred DBA
  • Pancreatic Neoplasms / drug therapy
  • Pancreatic Neoplasms / pathology
  • Prostatic Neoplasms / drug therapy
  • Prostatic Neoplasms / pathology
  • Rhodamines
  • Stereoisomerism
  • Tetrazolium Salts
  • Thiazoles


  • Antineoplastic Agents
  • CD11b Antigen
  • Coloring Agents
  • Lipopolysaccharide Receptors
  • Rhodamines
  • Tetrazolium Salts
  • Thiazoles
  • calcipotriene
  • Cholecalciferol
  • lissamine rhodamine B
  • thiazolyl blue
  • Calcitriol
  • Calcium