用于成像研究的不可逆结合比卡鲁胺类似物的合成。
Synthesis of irreversibly binding bicalutamide analogs for imaging studies.
作者信息
Nair Vipin A, Mustafa Suni M, Mohler Michael L, Yang Jun, Kirkovsky Leonid I, Dalton James T, Miller Duane D
机构信息
Department of Pharmaceutical Sciences, University of Tennessee, The Health Science Center, 847 Monroe Avenue, RM 227 C, Memphis, TN 38163, USA.
出版信息
Tetrahedron Lett. 2005 Jul 11;46(28):4821-4823. doi: 10.1016/j.tetlet.2005.04.143.
Abstract
A new synthetic methodology for preparing radioactive androgen receptor binding compounds in order to determine receptor-ligands interactions has been developed.
摘要
为了确定受体-配体相互作用，已开发出一种制备放射性雄激素受体结合化合物的新合成方法。
相似文献
1
Synthesis of irreversibly binding bicalutamide analogs for imaging studies.用于成像研究的不可逆结合比卡鲁胺类似物的合成。
Tetrahedron Lett. 2005 Jul 11;46(28):4821-4823. doi: 10.1016/j.tetlet.2005.04.143.
2
Optical biosensor analysis in studying new synthesized bicalutamide analogs binding to androgen receptor.用于研究新合成的比卡鲁胺类似物与雄激素受体结合的光学生物传感器分析。
J Pharm Biomed Anal. 2014 Jul;95:151-7. doi: 10.1016/j.jpba.2014.03.002. Epub 2014 Mar 12.
3
Synthesis and biological evaluation of [18F]bicalutamide, 4-[76Br]bromobicalutamide, and 4-[76Br]bromo-thiobicalutamide as non-steroidal androgens for prostate cancer imaging.[18F]比卡鲁胺、4-[76Br]溴比卡鲁胺和4-[76Br]溴硫比卡鲁胺作为用于前列腺癌成像的非甾体雄激素的合成及生物学评价
J Med Chem. 2007 Mar 8;50(5):1028-40. doi: 10.1021/jm060847r.
4
Affinity labeling of the androgen receptor with nonsteroidal chemoaffinity ligands.用非甾体化学亲和配体对雄激素受体进行亲和标记。
Biochem Pharmacol. 1999 Oct 15;58(8):1259-67. doi: 10.1016/s0006-2952(99)00218-x.
5
Bicalutamide functions as an androgen receptor antagonist by assembly of a transcriptionally inactive receptor.比卡鲁胺通过组装转录无活性受体发挥雄激素受体拮抗剂的作用。
J Biol Chem. 2002 Jul 19;277(29):26321-6. doi: 10.1074/jbc.M203310200. Epub 2002 May 15.
6
Switch from antagonist to agonist of the androgen receptor bicalutamide is associated with prostate tumour progression in a new model system.在一个新的模型系统中，雄激素受体拮抗剂比卡鲁胺向激动剂的转变与前列腺肿瘤进展相关。
Br J Cancer. 1999 Sep;81(2):242-51. doi: 10.1038/sj.bjc.6690684.
7
Interaction mechanism exploration of R-bicalutamide/S-1 with WT/W741L AR using molecular dynamics simulations.使用分子动力学模拟探索R-比卡鲁胺/S-1与野生型/ W741L雄激素受体的相互作用机制
Mol Biosyst. 2015 Dec;11(12):3347-54. doi: 10.1039/c5mb00499c. Epub 2015 Oct 7.
8
Chiral nonsteroidal affinity ligands for the androgen receptor. 1. Bicalutamide analogues bearing electrophilic groups in the B aromatic ring.用于雄激素受体的手性非甾体亲和配体。1. B芳香环带有亲电基团的比卡鲁胺类似物。
J Med Chem. 2000 Feb 24;43(4):581-90. doi: 10.1021/jm990027x.
9
In silico and in vitro assessment of androgen receptor antagonists.雄激素受体拮抗剂的计算机模拟和体外评估。
Comput Biol Chem. 2021 Jun;92:107490. doi: 10.1016/j.compbiolchem.2021.107490. Epub 2021 Apr 23.
10
Novel nonsteroidal ligands with high binding affinity and potent functional activity for the androgen receptor.对雄激素受体具有高结合亲和力和强功能活性的新型非甾体配体。
Eur J Med Chem. 2002 Aug;37(8):619-34. doi: 10.1016/s0223-5234(02)01335-1.
引用本文的文献
1
Organophotoredox Hydrodefluorination of Trifluoromethylarenes with Translational Applicability to Drug Discovery.具有药物发现转化应用潜力的三氟甲基芳烃的有机光氧化还原氢氟化反应。
J Am Chem Soc. 2020 May 20;142(20):9181-9187. doi: 10.1021/jacs.0c03881. Epub 2020 May 11.
2
Asymmetric synthesis of host-directed inhibitors of myxoviruses.针对粘液病毒的宿主定向抑制剂的不对称合成。
Beilstein J Org Chem. 2013;9:197-203. doi: 10.3762/bjoc.9.23. Epub 2013 Jan 30.
3
Synthesis of purine modified 2'-C-methyl nucleosides as potential anti-HCV agents.嘌呤修饰的 2'-C-甲基核苷的合成作为潜在的抗 HCV 药物。
Bioorg Med Chem Lett. 2011 Nov 15;21(22):6788-92. doi: 10.1016/j.bmcl.2011.09.034. Epub 2011 Sep 20.
4
Synthesis of oxazolidinedione derived bicalutamide analogs.恶唑烷二酮衍生的比卡鲁胺类似物的合成。
Tetrahedron Lett. 2006 Jun 5;47(23):3953-3955. doi: 10.1016/j.tetlet.2006.03.146.
本文引用的文献
1
A ligand-based approach to identify quantitative structure-activity relationships for the androgen receptor.一种基于配体的方法来确定雄激素受体的定量构效关系。
J Med Chem. 2004 Jul 15;47(15):3765-76. doi: 10.1021/jm0499007.
2
Design, synthesis, and biological characterization of metabolically stable selective androgen receptor modulators.代谢稳定的选择性雄激素受体调节剂的设计、合成及生物学特性研究
J Med Chem. 2004 Feb 12;47(4):993-8. doi: 10.1021/jm030336u.
3
Pharmacodynamics of selective androgen receptor modulators.选择性雄激素受体调节剂的药效学
J Pharmacol Exp Ther. 2003 Mar;304(3):1334-40. doi: 10.1124/jpet.102.040840.
4
Pharmacology, pharmacokinetics, and metabolism of acetothiolutamide, a novel nonsteroidal agonist for the androgen receptor.乙酰硫代鲁米特的药理学、药代动力学及代谢，一种新型雄激素受体非甾体激动剂
J Pharmacol Exp Ther. 2003 Mar;304(3):1323-33. doi: 10.1124/jpet.102.040832.
5
Homology modeling using multiple molecular dynamics simulations and docking studies of the human androgen receptor ligand binding domain bound to testosterone and nonsteroidal ligands.利用多分子动力学模拟和对接研究对与睾酮及非甾体配体结合的人雄激素受体配体结合域进行同源建模。
J Med Chem. 2001 May 24;44(11):1729-40. doi: 10.1021/jm0005353.
6
Design, synthesis, and pharmacological characterization of 4-[4, 4-dimethyl-3-(4-hydroxybutyl)-5-oxo-2-thioxo-1-imidazolidinyl]- 2-iodobenzonitrile as a high-affinity nonsteroidal androgen receptor ligand.4-[4,4-二甲基-3-(4-羟基丁基)-5-氧代-2-硫代-1-咪唑烷基]-2-碘苯甲腈作为高亲和力非甾体雄激素受体配体的设计、合成及药理特性研究
J Med Chem. 2000 Aug 24;43(17):3344-7. doi: 10.1021/jm000163y.
7
Chiral nonsteroidal affinity ligands for the androgen receptor. 1. Bicalutamide analogues bearing electrophilic groups in the B aromatic ring.用于雄激素受体的手性非甾体亲和配体。1. B芳香环带有亲电基团的比卡鲁胺类似物。
J Med Chem. 2000 Feb 24;43(4):581-90. doi: 10.1021/jm990027x.
8
Affinity labeling of the androgen receptor with nonsteroidal chemoaffinity ligands.用非甾体化学亲和配体对雄激素受体进行亲和标记。
Biochem Pharmacol. 1999 Oct 15;58(8):1259-67. doi: 10.1016/s0006-2952(99)00218-x.
9
Discovery of nonsteroidal androgens.非甾体雄激素的发现。
Biochem Biophys Res Commun. 1998 Mar 6;244(1):1-4. doi: 10.1006/bbrc.1998.8209.
10
Intracellular receptors and signal transducers and activators of transcription superfamilies: novel targets for small-molecule drug discovery.细胞内受体以及信号转导与转录激活因子超家族：小分子药物研发的新靶点。
J Med Chem. 1995 Dec 8;38(25):4855-74. doi: 10.1021/jm00025a001.
Zotero 插件