664978-86-3Relevant academic research and scientific papers
Synthesis of novel 1α,25-dihydroxy-19-norvitamin D3 with an amide conjugate
Suhara, Yoshitomo,Ono, Keiichiro,Yoshida, Akihiro,Fujishima, Toshie,Saito, Nozomi,Honzawa, Shinobu,Kishimoto, Seishi,Sugiura, Takayuki,Waku, Keizo,Takayama, Hiroaki,Kittaka, Atsushi
, p. 423 - 436 (2007/10/03)
The diene system of 1α,25-dihydroxy-19-norvitamin D3 was replaced by a stable amide bond. A 3-hydroxypropoxy group, which was effective on enhancing binding affinity of 1α,25-dihydroxyvitamin D3 for vitamin D receptor (VDR), was introduced to the C2-position of the amide type analogue of 1α,25-dihydroxy-19-norvitamin D3. The amide analogue was found to be not suitable for binding to the ligand binding domain of the bovine thymus VDR, and additional modification at the C2-position did not improve the affinity. Potency in induction of HL-60 cell differentiation was evaluated for the novel amide analogues (3a-c).
