Ligands with dual vitamin D3-agonistic and androgen-antagonistic activities

被引:40
作者
Hosoda, S
Tanatani, A
Wakabayashi, K
Nakano, Y
Miyachi, H
Nagasawa, K
Hashimoto, Y
机构
[1] Univ Tokyo, Inst Mol & Cellular Biosci, Bunkyo Ku, Tokyo 1130032, Japan
[2] Tokyo Univ Agr & Technol, Fac Technol, Dept Biotechnol & Life Sci, Tokyo 1848588, Japan
基金
日本学术振兴会;
关键词
vitamin D-3; androgen antagonist; bisphenylmethane;
D O I
10.1016/j.bmcl.2005.06.044
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Ligands possessing dual vitamin D-3-agonistic (estimated as HL-60 monocytic cell differentiation induction) and androgen-antagonistic (estimated as testosterone-induced SC-3 cell growth inhibition) activities with various activity spectra were prepared based on a substituted bis-phenylmethane skeleton. Some of them were revealed to be potent androgen antagonists with a nonsecosteroidal vitamin D-3 skeleton. (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码:4327 / 4331
页数:5
相关论文
共 21 条
  • [1] Androgen signaling is required for the vitamin D-mediated growth inhibition in human prostate cancer cells
    Bao, BY
    Hu, YC
    Ting, HJ
    Lee, YF
    [J]. ONCOGENE, 2004, 23 (19) : 3350 - 3360
  • [3] Novel nonsecosteroidal vitamin D mimics exert VDR-modulating activities with less calcium mobilization than 1,25-dihydroxyvitamin D3
    Boehm, MF
    Fitzgerald, P
    Zou, AH
    Elgort, MG
    Bischoff, ED
    Mere, L
    Mais, DE
    Bissonnette, RP
    Heyman, RA
    Nadzan, AM
    Reichman, M
    Allegretto, EA
    [J]. CHEMISTRY & BIOLOGY, 1999, 6 (05): : 265 - 275
  • [4] STRUCTURE-FUNCTION-RELATIONSHIPS IN THE VITAMIN-D ENDOCRINE SYSTEM
    BOUILLON, R
    OKAMURA, WH
    NORMAN, AW
    [J]. ENDOCRINE REVIEWS, 1995, 16 (02) : 200 - 257
  • [5] AN EVALUATION OF 1,25-DIHYDROXYVITAMIN-D3 ANALOGS ON THE PROLIFERATION AND DIFFERENTIATION OF CULTURED HUMAN KERATINOCYTES, CALCIUM-METABOLISM AND THE DIFFERENTIATION OF HUMAN HL-60 CELLS
    CHEN, TC
    PERSONS, K
    USKOKOVIC, MR
    HORST, RL
    HOLICK, MF
    [J]. JOURNAL OF NUTRITIONAL BIOCHEMISTRY, 1993, 4 (01) : 49 - 57
  • [6] HANCHETTE CL, 1992, CANCER, V70, P2861, DOI 10.1002/1097-0142(19921215)70:12<2861::AID-CNCR2820701224>3.0.CO
  • [7] 2-G
  • [8] HASHIMOTO Y, 2005, BIOORG MED CHEM, V13
  • [9] Anti-androgens with full antagonistic activity toward human prostate tumor LNCaP cells with mutated androgen receptor
    Ishioka, T
    Tanatani, A
    Nagasawa, K
    Hashimoto, Y
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2003, 13 (16) : 2655 - 2658
  • [10] Novel non-steroidal/non-anilide type androgen antagonists with an isoxazolone moiety
    Ishioka, T
    Kubo, A
    Koiso, Y
    Nagasawa, K
    Itai, A
    Hashimoto, Y
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY, 2002, 10 (05) : 1555 - 1566