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Volume 76, Issue 11
Displaying 1-29 of 29 articles from this issue
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Hiroaki TAKAYAMA, Atsushi KITTAKA, Toshie FUJISHIMA, Yoshitomo SUHARAArticle type: Article
2002 Volume 76 Issue 11 Pages 491-505
Published: November 25, 2002
Released on J-STAGE: December 26, 2017
JOURNAL FREE ACCESSRecently, structure-activity relationships on the A-ring moiety of 1α, 25-dihydroxyvitamin D_3 (1) are one of the major topics of vitamin D_3 research field. Discussions on this context have been enthusiastic, however, the A-ring modified analogue of 1, which induces markedly stronger biological activities than 1, was very rare so far. We are interested in chemical synthesis of the A-ring modified 1, 25 (OH)_2D_3, especially in C2 modification together with C1 and C3 epimerization of the two hydroxyl groups, to understand how the A-ring is responsible for the D_3 biological activities. First, we synthesized all eight possible diastereomers of the 2-methyl analogues 3a-h due to a series of three chiral centers of C1, C2, and C3, systematically. Next, on the basis of unprecedented, strong and unique biological profile of the 2α-methyl analogue 3g, the other 2α-functional groups in three categories, i. e., 2α-alkyl (18a-c) , 2α-hydroxyalkyl (19a-d) , and 2α-hydroxyalkoxyl groups (30a-c) , were introduced into 1 stereoselectively. We found that five of our new 2α-modified analogues (3g, 19c, d, 30a, b) possess higher vitamin D receptor (VDR) binding affinity than that of 1. Docking studies of the synthetic ligands to VDR and remarkably high potency with some separated D_3-activities are described.View full abstractDownload PDF (1338K) -
[in Japanese]Article type: Article
2002 Volume 76 Issue 11 Pages 507-
Published: November 25, 2002
Released on J-STAGE: December 26, 2017
JOURNAL FREE ACCESSDownload PDF (122K) -
[in Japanese]Article type: Article
2002 Volume 76 Issue 11 Pages 509-514
Published: November 25, 2002
Released on J-STAGE: December 26, 2017
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[in Japanese], [in Japanese]Article type: Article
2002 Volume 76 Issue 11 Pages 515-519
Published: November 25, 2002
Released on J-STAGE: December 26, 2017
JOURNAL FREE ACCESS -
[in Japanese], [in Japanese]Article type: Article
2002 Volume 76 Issue 11 Pages 521-524
Published: November 25, 2002
Released on J-STAGE: December 26, 2017
JOURNAL FREE ACCESSDownload PDF (434K) -
[in Japanese]Article type: Article
2002 Volume 76 Issue 11 Pages 525-533
Published: November 25, 2002
Released on J-STAGE: December 26, 2017
JOURNAL FREE ACCESS -
[in Japanese], [in Japanese], [in Japanese], [in Japanese]Article type: Article
2002 Volume 76 Issue 11 Pages 535-543
Published: November 25, 2002
Released on J-STAGE: December 26, 2017
JOURNAL FREE ACCESS -
[in Japanese], [in Japanese]Article type: Article
2002 Volume 76 Issue 11 Pages 545-549
Published: November 25, 2002
Released on J-STAGE: December 26, 2017
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[in Japanese]Article type: Article
2002 Volume 76 Issue 11 Pages 551-553
Published: November 25, 2002
Released on J-STAGE: December 26, 2017
JOURNAL FREE ACCESSDownload PDF (384K) -
[in Japanese], [in Japanese], [in Japanese]Article type: Article
2002 Volume 76 Issue 11 Pages 553-554
Published: November 25, 2002
Released on J-STAGE: December 26, 2017
JOURNAL FREE ACCESSDownload PDF (260K) -
[in Japanese]Article type: Article
2002 Volume 76 Issue 11 Pages 555-558
Published: November 25, 2002
Released on J-STAGE: December 26, 2017
JOURNAL FREE ACCESSDownload PDF (475K) -
Article type: Article
2002 Volume 76 Issue 11 Pages 559-
Published: November 25, 2002
Released on J-STAGE: December 26, 2017
JOURNAL FREE ACCESSDownload PDF (160K) -
[in Japanese]Article type: Article
2002 Volume 76 Issue 11 Pages 559-560
Published: November 25, 2002
Released on J-STAGE: December 26, 2017
JOURNAL FREE ACCESSDownload PDF (302K) -
[in Japanese]Article type: Article
2002 Volume 76 Issue 11 Pages 560-562
Published: November 25, 2002
Released on J-STAGE: December 26, 2017
JOURNAL FREE ACCESSDownload PDF (462K) -
[in Japanese]Article type: Article
2002 Volume 76 Issue 11 Pages 562-563
Published: November 25, 2002
Released on J-STAGE: December 26, 2017
JOURNAL FREE ACCESSDownload PDF (312K) -
[in Japanese], [in Japanese], [in Japanese], [in Japanese], [in Japane ...Article type: Article
2002 Volume 76 Issue 11 Pages 563-564
Published: November 25, 2002
Released on J-STAGE: December 26, 2017
JOURNAL FREE ACCESSDownload PDF (314K) -
[in Japanese]Article type: Article
2002 Volume 76 Issue 11 Pages 564-565
Published: November 25, 2002
Released on J-STAGE: December 26, 2017
JOURNAL FREE ACCESSDownload PDF (317K) -
[in Japanese]Article type: Article
2002 Volume 76 Issue 11 Pages 565-566
Published: November 25, 2002
Released on J-STAGE: December 26, 2017
JOURNAL FREE ACCESSDownload PDF (297K) -
Article type: Article
2002 Volume 76 Issue 11 Pages 566-567
Published: November 25, 2002
Released on J-STAGE: December 26, 2017
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[in Japanese], [in Japanese], Abdul Jahlil, Laila Begum, [in Japanese] ...Article type: Article
2002 Volume 76 Issue 11 Pages 568-
Published: November 25, 2002
Released on J-STAGE: December 26, 2017
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[in Japanese]Article type: Article
2002 Volume 76 Issue 11 Pages 568-569
Published: November 25, 2002
Released on J-STAGE: December 26, 2017
JOURNAL FREE ACCESSDownload PDF (299K) -
[in Japanese]Article type: Article
2002 Volume 76 Issue 11 Pages 569-
Published: November 25, 2002
Released on J-STAGE: December 26, 2017
JOURNAL FREE ACCESSDownload PDF (168K) -
[in Japanese], [in Japanese], [in Japanese], [in Japanese], [in Japane ...Article type: Article
2002 Volume 76 Issue 11 Pages 569-570
Published: November 25, 2002
Released on J-STAGE: December 26, 2017
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[in Japanese]Article type: Article
2002 Volume 76 Issue 11 Pages 570-571
Published: November 25, 2002
Released on J-STAGE: December 26, 2017
JOURNAL FREE ACCESSDownload PDF (310K) -
[in Japanese]Article type: Article
2002 Volume 76 Issue 11 Pages 571-572
Published: November 25, 2002
Released on J-STAGE: December 26, 2017
JOURNAL FREE ACCESSDownload PDF (302K) -
Article type: Article
2002 Volume 76 Issue 11 Pages 572-573
Published: November 25, 2002
Released on J-STAGE: December 26, 2017
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[in Japanese]Article type: Article
2002 Volume 76 Issue 11 Pages 573-
Published: November 25, 2002
Released on J-STAGE: December 26, 2017
JOURNAL FREE ACCESSDownload PDF (179K) -
[in Japanese]Article type: Article
2002 Volume 76 Issue 11 Pages 573-574
Published: November 25, 2002
Released on J-STAGE: December 26, 2017
JOURNAL FREE ACCESSDownload PDF (317K) -
[in Japanese]Article type: Article
2002 Volume 76 Issue 11 Pages 574-575
Published: November 25, 2002
Released on J-STAGE: December 26, 2017
JOURNAL FREE ACCESSDownload PDF (223K)
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