114694-13-2Relevant academic research and scientific papers
Practical synthesis and evaluation of the biological activities of 1α,25-dihydroxyvitamin D3 antagonists, 1α,25- dihydroxyvitamin D3-26,23-lactams. Designed on the basis of the helix 12-folding inhibition hypothesis
Nakano, Yusuke,Kato, Yuko,Imai, Keisuke,Ochiai, Eiji,Namekawa, Jun-Ichi,Ishizuka, Seiichi,Takenouchi, Kazuya,Tanatani, Aya,Hashimoto, Yuichi,Nagasawa, Kazuo
, p. 2398 - 2406 (2007/10/03)
A practical synthetic route to novel vitamin D antagonists of DLAM (1α,25-dihydroxyvitamin D3-26,23-lactam) was developed from vitamin D2 via the 1,3-dipolar cycloaddition reaction as a key step. Six DLAM derivatives (24 compounds) w
VITAMIN D3 LACTONE DERIVATIVE
-
Page/Page column 29, (2010/02/14)
A compound represented by the following Formula (1) that is effective for the treatment of Paget's disease of bone or hypercalcemia or a medically acceptable solvate thereof; [wherein R1 refers to hydrogen atom, C1-C6 alky
VITAMIN D3 DERIVATIVES AND REMEDIES USING THE SAME
-
Page 30-31, (2010/02/09)
A vitamin D3 derivative expressed by the following general formula (1) [wherein, R is a hydrogen atom or a methyl group, and A is a single bond, -CH2-, -CH=CH-, -CH2-CH=CH-, -CH=CH-CH=CH-, -C=C- or -CH2-C≡C-; an
Synthesis and antiproliferative activity of side-chain unsaturated and homologated analogs of 1,25-dihydroxyvitamin D(2). (24E)-(1S)-24-Dehydro-24a-homo-1,25-dihydroxyergocalciferol and congeners.
Chodynski, Michal,Wietrzyk, Joanna,Marcinkowska, Ewa,Opolski, Adam,Szelejewski, Wieslaw,Kutner, Andrzej
, p. 789 - 798 (2007/10/03)
A series of analogs of 1,25-dihydroxyergocalciferol (1-4) was synthesized and screened for their antiproliferative activity in vitro. The structure of new analogs was designed based on biological activity of the previously obtained side-chain modified analogs of vitamin D(2) and D(3). The analogs were obtained by the Julia olefination of C(22)-vitamin D sulfone 11 with side-chain aldehyde 15. The analogs were tested for their antiproliferative activity against the cells of human breast cancer lines T47D and MCF7 as well as human and mouse leukemia lines, HL-60 and WEHI-3, respectively. Analog 2 (PRI-1907) showed the strongest antiproliferative activity out of the present series of analogs of 1,25-dihydroxyvitamin D(2) with the mono homologated and double unsaturated side chain. The activity of 2 was 3-150 times stronger, depending on the cell line, than that of 1,25-dihydroxycholecalciferol (calcitriol), used as standard. Copyright 2002 Elsevier Science Inc.
An improved synthesis of 24,24-difluoro-1α,25-dihydroxyvitamin D3 from readily available vitamin D2
Ando,Koike,Takayama
, p. 189 - 192 (2007/10/02)
An improved synthesis of a highly potent vitamin D3 analog, 24,24-difluoro-1α,25-dihydroxyvitamin D3 (1b) has been accomplished via vitamin D2-SO2 adducts. The introduction of fluorine atoms was performed by tre
An improved synthesis of 24,24-difluoro-1α,25-dihydroxy-vitamin D3 from vitamin D2
Ando,Kondo,Koike,Takayama
, p. 1662 - 1664 (2007/10/02)
An improved synthesis of a highly potent vitamin D3 analog, 24,24-difluoro-1α,25-dihydroxyvitamin D3 has been accomplished. The total yield was 9.3% from inexpensive vitamin D2 in 11 steps.
Novel Convergent Synthesis of Side-Chain-Modified Analogues of 1α,25-Dihydroxycholecalciferol and 1α,25-Dihydroxyergocalciferol
Kutner, Andrzej,Perlman, Kato L.,Lago, Amparo,Sicinski, Rafal R.,Schnoes, Heinhrich K.,DeLuca, H. F.
, p. 3450 - 3457 (2007/10/02)
A novel synthetic strategy for the preparation of side-chain-modified analogues of 1α,25-dihydroxycholecalciferol and 1α,25-dihydroxyergocalciferol was developed as a part of the extensive synthetic search for vitamin D analogues of potential anticancer a
