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
N1 - Funding Information:
This work was supported in part by a Grant-in-Aid from the Ministry of Education, Science and Culture of Japan.
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.
UR - http://www.scopus.com/inward/record.url?scp=0034658166&partnerID=8YFLogxK
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
C2 - 10843234
AN - SCOPUS:0034658166
VL - 10
SP - 1129
EP - 1132
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
SN - 0960-894X
IS - 10
ER -