期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 17, 期 15, 页码 5627-5631出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2009.06.033
关键词
1 alpha,25-Dihydroxyvitamin D-3; Sulfone; Calcitriol; Trifluoromethyl; Antiproliferative
资金
- NCI NIH HHS [R01 CA093547, R01 CA093547-05] Funding Source: Medline
The replacement of a t-butyl group with a trifluoromethyl group has profound effects on the biological profile of 1 alpha,25-dihydroxyvitamin D-3 sulfone analogs. Investigation of whether the improved biological activities are due to steric and electronic factors of the trifluoromethyl group led to the design, synthesis and biological evaluation of two analogous alkyl sulfone molecules, methyl sulfone (AU-16-ene-25-SO2-CH3) and isopropyl sulfone (AU-16-ene-25-SO2-i-Pr). These alkyl sulfones are sterically comparable to, but electronically very different from a trifluoromethyl group. The syntheses, antiproliferative activities and calcemic activities of these new alkyl sulfones are presented herein. In comparing the in vitro antiproliferative profiles of the new alkyl sulfone 1 alpha,25-dihydroxyvitamin D-3 analogs with the trifluoromethylsulfone and an analogous t-butyl sulfone, the activities increase in the following order: CH3
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