Highly antiproliferative, low-calcemic, side-chain amide and hydroxamate analogs of the hormone 1alpha,25-dihydroxyvitamin D3

Four new side-chain amide (2 and 3) and hydroxamate (4 and 5) analogs of the hormone calcitriol (1) have been prepared. Even though lacking the 25-OH group characteristic of natural calcitriol (1), analogs 2-4 are as antiproliferative in vitro as calcitriol (1) but are 20-40 times less calciuric in...

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Published inBioorganic & medicinal chemistry Vol. 14; no. 18; pp. 6341 - 6348
Main Authors Sinishtaj, Sandra, Jeon, Heung Bae, Dolan, Patrick, Kensler, Thomas W, Posner, Gary H
Format Journal Article
LanguageEnglish
Published England 15.09.2006
Subjects
Amides - chemistry
Animals
Calcitriol - analogs & derivatives
Calcitriol - chemical synthesis
Calcitriol - pharmacology
Calcium - chemistry
Cell Proliferation - drug effects
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Hydroxamic Acids - chemistry
In Vitro Techniques
Keratinocytes - drug effects
Molecular Conformation
Stereoisomerism
Structure-Activity Relationship
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Summary:Four new side-chain amide (2 and 3) and hydroxamate (4 and 5) analogs of the hormone calcitriol (1) have been prepared. Even though lacking the 25-OH group characteristic of natural calcitriol (1), analogs 2-4 are as antiproliferative in vitro as calcitriol (1) but are 20-40 times less calciuric in vivo than calcitriol (1).
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
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ISSN:0968-0896
1464-3391