Gemini Analogs of Vitamin D

被引:5
|
作者
Pazos, Gonzalo [1 ]
Rivadulla, Marcos L. [1 ]
Perez-Garcia, Xenxo [1 ]
Gandara, Zoila [1 ,2 ]
Perez, Manuel [1 ,3 ]
机构
[1] Univ Vigo, Fac Quim, Dept Quim Organ, Vigo 36202, Spain
[2] Palacky Univ, Fac Sci, Dept Chem Biol & Genet, Ctr Reg Hana Biotechnol & Agr Res, CZ-78371 Olomouc, Czech Republic
[3] Univ Toronto, Dept Chem, Toronto, ON M5S 3H6, Canada
关键词
Chemical synthesis; Gemini analogs; Steroid; Vitamin D; LIGAND-BINDING DOMAIN; DIFFERENT SIDE-CHAINS; NUCLEAR RECEPTOR; CALCITRIOL DERIVATIVES; MAMMARY TUMORIGENESIS; EXPRESSION; D-3;
D O I
10.2174/1568026615666141208100411
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The Gemini analogs are the last significant contribution to the family of vitamin D derivatives in medicine, for the treatment of cancer. The first Gemini analog was characterized by two symmetric side chains at C-20. Following numerous modifications, the most active analog bears a C-23-triple bond, C-26, 27-hexafluoro substituents on one side chain and a terminal trideuteromethylhydroxy group on the other side chain. This progression was possible due to improvements in the synthetic methods for the preparation of these derivatives, which allowed for increasing molecular complexity and complete diastereoselective control at C-20 and the substituted sidechains.
引用
收藏
页码:2388 / 2397
页数:10
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