Syntheses and biological evaluation of novel 2α-substituted 1α,25-dihydroxyvitamin D3 analogues

Yoshitomo Suhara; Ken Ichi Nihei; Hirokazu Tanigawa; Toshie Fujishima; Katsuhiro Konno; Kimie Nakagawa; Toshio Okano; Hiroaki Takayama

doi:10.1016/S0960-894X(00)00189-X

Syntheses and biological evaluation of novel 2α-substituted 1α,25-dihydroxyvitamin D₃ analogues

Yoshitomo Suhara, Ken Ichi Nihei, Hirokazu Tanigawa, Toshie Fujishima, Katsuhiro Konno, Kimie Nakagawa, Toshio Okano, Hiroaki Takayama

Research output: Contribution to journal › Article

64 Citations (Scopus)

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	https://doi.org/10.1016/S0960-894X(00)00189-X
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

Suhara, Y., Nihei, K. I., Tanigawa, H., Fujishima, T., Konno, K., Nakagawa, K., ... Takayama, H. (2000). Syntheses and biological evaluation of novel 2α-substituted 1α,25-dihydroxyvitamin D₃ analogues. Bioorganic and Medicinal Chemistry Letters, 10(10), 1129-1132. https://doi.org/10.1016/S0960-894X(00)00189-X

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

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10.1016/S0960-894X(00)00189-X