TY - JOUR
T1 - The difference between 14-epi-previtamin D 3 and 14-epi-19-norprevitamin D 3
T2 - Their synthesis and binding affinity for human VDR
AU - Sawada, Daisuke
AU - Katayama, Tomoyuki
AU - Tsukuda, Yuya
AU - Saito, Nozomi
AU - Saito, Hiroshi
AU - Kakuda, Shinji
AU - Takimoto-Kamimura, Midori
AU - Takenouchi, Kazuya
AU - Kittaka, Atsushi
PY - 2012/1/1
Y1 - 2012/1/1
N2 - The synthesis of 14-epi-1α,25(OH) 2previtamin D 3, 14-epi-19-nor-1α,25(OH) 2previtamin D 3, and their 2-substituted analogs is described. The vitamin D receptor (VDR) binding affinity was further evaluated and 2α-methyl substituted 14-epi-1α,25(OH) 2previtamin D 3 had 17-fold more potent affinity than 14-epi-1α25(OH) 2previtamin D 3. In the comparison of these compounds, the effects of thermal equilibrium, with or without 19-carbon at the A-ring, and their CD-ring structures are discussed.
AB - The synthesis of 14-epi-1α,25(OH) 2previtamin D 3, 14-epi-19-nor-1α,25(OH) 2previtamin D 3, and their 2-substituted analogs is described. The vitamin D receptor (VDR) binding affinity was further evaluated and 2α-methyl substituted 14-epi-1α,25(OH) 2previtamin D 3 had 17-fold more potent affinity than 14-epi-1α25(OH) 2previtamin D 3. In the comparison of these compounds, the effects of thermal equilibrium, with or without 19-carbon at the A-ring, and their CD-ring structures are discussed.
KW - 14-Epi-19-norprevitamin D
KW - 14-Epi-previtamin D
KW - VDR binding affinity
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M3 - Article
C2 - 22213322
AN - SCOPUS:84856015543
VL - 32
SP - 319
EP - 326
JO - Anticancer Research
JF - Anticancer Research
SN - 0250-7005
IS - 1 PART 2
ER -