Design, synthesis and biological evaluation of novel 1α,25-dihydroxyvitamin D3 analogues possessing aromatic ring on 2α-position

Autor:	Nozomi Saito, Seishi Kishimoto, Keizo Waku, Hiroaki Takayama, Masaaki Kurihara, Shinobu Honzawa, Yasuhiro Yamamoto, Takayuki Sugiura, Sara Peleg, Atsushi Kittaka, Toshie Fujishima, Koshiro Hirasaka
Rok vydání:	2005
Předmět:	Vitamin Stereochemistry Cellular differentiation Organic Chemistry Mutant Wild type Rickets medicine.disease Ring (chemistry) Biochemistry Calcitriol receptor chemistry.chemical_compound chemistry Drug Discovery polycyclic compounds medicine Potency
Zdroj:	Tetrahedron. 61:11253-11263
ISSN:	0040-4020
DOI:	10.1016/j.tet.2005.08.116
Popis:	In the present study, we describe the synthesis of new analogues of 1α,25-dihydroxyvitamin D 3 ( 1 ), which possess hydrophobic aromatic ring on the 2α position. Among these analogues, 2α-benzyl analogue showed the highest potency in the affinity for the wild type vitamin D receptor (VDR) and induction of HL-60 cell differentiation as well as transcriptional activity. Affinity for the mutant VDR related to hereditary vitamin D-resistant rickets (R274L) was also examined.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::fa9ff8c8f7704c2b0f8dd6eec0cc7a07 https://doi.org/10.1016/j.tet.2005.08.116 Zobrazit plný text záznamu Full Text from ScienceDirect