Synthesis and biological activities of 22-hydroxy and 22-methoxy derivatives of 1α,25-dihydroxyvitamin D3: Importance of side chain conformation for biological activities
✍ Scribed by Tadashi Eguchi; Mitsuzi Yoshida; Nobuo Ikekawa
- Publisher
- Elsevier Science
- Year
- 1989
- Tongue
- English
- Weight
- 900 KB
- Volume
- 17
- Category
- Article
- ISSN
- 0045-2068
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## Abstract An improved synthetic route to 1α,25‐dihydroxyvitamin D~3~ des‐side chain analogues **2 a** and **2 b** with substituents at C18 is reported, along with their biological activity. These analogues display significant antiproliferative effects toward MCF‐7 breast cancer cells and prodiffe
We found a concise route to the Trost A-ring precursor enyne for synthesizing 2a-alkylated 1a,25-dihydroxyvitamin D 3 (1) from d-glucose. The enynes were coupled with the 20-epi-CD ring part to study the effect of the double modification of 2asubstitution and 20-epimerization upon biological activit