Abstract
Novel 2α-substituted 1α,25-dihydroxyvitamin D3 analogues were efficiently synthesized and their biological activities were evaluated. 2α-Methyl-1α25-dihydroxyvitamin D3 (2), whose unique biological activities were previously reported, was modified to 2α-alkyl (ethyl and propyl) and 2α-hydroxyalkyl (hydroxymethyl, hydroxyethyl, and hydroxypropyl) analogues 3-7 by elongation of the alkyl chain and/or introduction of a terminal hydroxyl group. 2α-Hydroxypropyl-1α,25-dihydroxyvitamin D3 (7) exhibited an exceptionally potent calcium-regulating effect and a unique activity profile. (C) 2000 Elsevier Science Ltd. All rights reserved.
| Original language | English |
|---|---|
| Pages (from-to) | 1129-1132 |
| Number of pages | 4 |
| Journal | Bioorganic and Medicinal Chemistry Letters |
| Volume | 10 |
| Issue number | 10 |
| DOIs | |
| Publication status | Published - 2000 May 15 |
| Externally published | Yes |
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ASJC Scopus subject areas
- Biochemistry
- Molecular Biology
- Organic Chemistry
- Drug Discovery
- Pharmaceutical Science
Cite this
Syntheses and biological evaluation of novel 2α-substituted 1α,25-dihydroxyvitamin D3 analogues. / Suhara, Yoshitomo; Nihei, Ken Ichi; Tanigawa, Hirokazu; Fujishima, Toshie; Konno, Katsuhiro; Nakagawa, Kimie; Okano, Toshio; Takayama, Hiroaki.
In: Bioorganic and Medicinal Chemistry Letters, Vol. 10, No. 10, 15.05.2000, p. 1129-1132.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Syntheses and biological evaluation of novel 2α-substituted 1α,25-dihydroxyvitamin D3 analogues
AU - Suhara, Yoshitomo
AU - Nihei, Ken Ichi
AU - Tanigawa, Hirokazu
AU - Fujishima, Toshie
AU - Konno, Katsuhiro
AU - Nakagawa, Kimie
AU - Okano, Toshio
AU - Takayama, Hiroaki
PY - 2000/5/15
Y1 - 2000/5/15
N2 - Novel 2α-substituted 1α,25-dihydroxyvitamin D3 analogues were efficiently synthesized and their biological activities were evaluated. 2α-Methyl-1α25-dihydroxyvitamin D3 (2), whose unique biological activities were previously reported, was modified to 2α-alkyl (ethyl and propyl) and 2α-hydroxyalkyl (hydroxymethyl, hydroxyethyl, and hydroxypropyl) analogues 3-7 by elongation of the alkyl chain and/or introduction of a terminal hydroxyl group. 2α-Hydroxypropyl-1α,25-dihydroxyvitamin D3 (7) exhibited an exceptionally potent calcium-regulating effect and a unique activity profile. (C) 2000 Elsevier Science Ltd. All rights reserved.
AB - Novel 2α-substituted 1α,25-dihydroxyvitamin D3 analogues were efficiently synthesized and their biological activities were evaluated. 2α-Methyl-1α25-dihydroxyvitamin D3 (2), whose unique biological activities were previously reported, was modified to 2α-alkyl (ethyl and propyl) and 2α-hydroxyalkyl (hydroxymethyl, hydroxyethyl, and hydroxypropyl) analogues 3-7 by elongation of the alkyl chain and/or introduction of a terminal hydroxyl group. 2α-Hydroxypropyl-1α,25-dihydroxyvitamin D3 (7) exhibited an exceptionally potent calcium-regulating effect and a unique activity profile. (C) 2000 Elsevier Science Ltd. All rights reserved.
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UR - http://www.scopus.com/inward/citedby.url?scp=0034658166&partnerID=8YFLogxK
U2 - 10.1016/S0960-894X(00)00189-X
DO - 10.1016/S0960-894X(00)00189-X
M3 - Article
VL - 10
SP - 1129
EP - 1132
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
SN - 0960-894X
IS - 10
ER -