3-(5-Chloro-2,4-dihydroxyphenyl)-pyrazole-4-carboxamides as inhibitors of the Hsp90 molecular chaperone.

Brough PA; Barril X; Beswick M; Dymock BW; Drysdale MJ; Wright L; Grant K; Massey A; Surgenor A; Workman P

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3-(5-Chloro-2,4-dihydroxyphenyl)-pyrazole-4-carboxamides as inhibitors of the Hsp90 molecular chaperone.

机译：3-（5-氯-2,4-二羟基苯基）-吡唑-4-羧酰胺作为Hsp90分子伴侣的抑制剂。

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Information from X-ray crystal structures of Hsp90 inhibitors bound to the human Hsp90 molecular chaperone was used to assist in the design of 3-(5-chloro-2,4-dihydroxyphenyl)-pyrazole-4-carboxamides as novel inhibitors of Hsp90. Accessing an extra interaction with the protein via Phe138 gave a significant increase in binding potency compared to similar analogues that do not make this interaction.

机译：Hsp90抑制剂与人Hsp90分子伴侣结合的X射线晶体结构信息被用来协助设计3-（5-氯-2,4-二羟基苯基）-吡唑-4-羧酰胺作为Hsp90的新型抑制剂。与不进行这种相互作用的类似类似物相比，通过Phe138与蛋白质进行额外的相互作用可使结合力显着提高。

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《Bioorganic and Medicinal Chemistry Letters》 |2005年第23期|共5页
作者
Brough PA; Barril X; Beswick M; Dymock BW; Drysdale MJ; Wright L; Grant K; Massey A; Surgenor A; Workman P;
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正文语种 eng
中图分类基础医学;
关键词
inhibitors; Molecular Chaperones; pyrazole; Information; novel; 分子监控蛋白类;

机译：inhibitors;Molecular Chaperones;pyrazole;Information;novel;分子监控蛋白类;

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1. 3-(5-Chloro-2,4-dihydroxyphenyl)-pyrazole-4-carboxamides as inhibitors of the Hsp90 molecular chaperone. [J] . Brough PA, Barril X, Beswick M, Bioorganic and Medicinal Chemistry Letters . 2005,第23期

机译：3-（5-氯-2,4-二羟基苯基）-吡唑-4-羧酰胺作为Hsp90分子伴侣的抑制剂。
2. 5-Aryl-4-(5-substituted-2,4-dihydroxyphenyl)-1,2,3-thiadiazoles as inhibitors of Hsp90 chaperone. [J] . Cikotiene I, Kazlauskas E, Matuliene J, Bioorganic and Medicinal Chemistry Letters . 2009,第4期

机译：5-芳基-4-（5-取代的2,4-二羟基苯基）-1,2,3-噻二唑作为Hsp90伴侣的抑制剂。
3. 5-Aryl-4-(5-substituted-2,4-dihydroxyphenyl)-1,2,3-thiadiazoles as inhibitors of Hsp90 chaperone. [J] . Cikotiene I, Kazlauskas E, Matuliene J, Bioorganic and Medicinal Chemistry Letters . 2009,第4期

机译：5-芳基-4-（5-取代的2,4-二羟基苯基）-1,2,3-噻二唑作为Hsp90伴侣的抑制剂。
4. Blocking the protein folding machinery. Rational design of inhibitors of the molecular chaperone Hsp90 as new anticancer agents [C] . G. COLOMBO International School of Physics "Enrico Fermi" . 2007

机译：阻止蛋白质折叠机械。作为新抗癌剂的分子伴侣HSP90抑制剂的理性设计
5. The role of NQO1 in the metabolism of benzoquinone ansamycin Hsp90 inhibitors and development of novel Hsp90 inhibitors as anticancer agents. [D] . Guo, Wenchang. 2007

机译：NQO1在苯醌安沙霉素Hsp90抑制剂的代谢中的作用以及新型Hsp90抑制剂作为抗癌剂的开发。
6. 3-(3,4-Dihydroxyphenyl)-1-methoxy-1-oxopropan-2-aminium chloride [O] . Ze-Feng Hou, Juan Feng, Jing-Tian Liu, 2015

机译：3-（3,4-二羟基苯基）-1-甲氧基-1-氧丙烷-2-氯化铵
7. A comprehensive study on the immunological reactivity of the Hsp90 molecular chaperone. [O] . Kawano Toshihiro, Kobayakawa Takeshi, Fukuma Yutaka, 2004

机译：关于Hsp90分子伴侣的免疫反应性的综合研究。
8. Boranametallacarboranes. 2. Crystal and Molecular Structures of (2, 3-(C2H5)2C2B4H4)-5-Co(B9H12-1-O(CH2)4), (2,3-(CH3)2C2B3H5)-5-Co(B9H12-1-O(CH2)4), and (1,2-(C2H5)2C2B7H7)-6-Co(B9H12-2-O(CH2)4) [R] . Borodinsky, L., Sinn, E., Grimes, R. N. 1981

机译：Boranametallacarboranes。 2.（2,3-（C2H5）2C2B4H4）-5-Co（B9H12-1-O（CH2）4），（2,3-（CH3）2C2B3H5）-5-Co（B9H12-）的晶体和分子结构1-O（CH2）4）和（1,2-（C2H5）2C2B7H7）-6-Co（B9H12-2-O（CH2）4）

3-(5-Chloro-2,4-dihydroxyphenyl)-pyrazole-4-carboxamides as inhibitors of the Hsp90 molecular chaperone.

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