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非硫醇法尼基转移酶抑制剂:基于二苯甲酮的双底物类似物法尼基转移酶抑制剂的法尼基转移酶抑制作用及细胞活性

Non-thiol farnesyltransferase inhibitors: FTase-inhibition and cellular activity of benzophenone-based bisubstrate analogue farnesyltransferase inhibitors.

作者信息

Mitsch Andreas, Bergemann Silke, Gust Ronald, Sattler Isabel, Schlitzer Martin

机构信息

Institut für Pharmazeutische Chemie, Philipps-Universität Marburg, Marburg, Germany.

出版信息

Arch Pharm (Weinheim). 2003 Jul;336(4-5):242-50. doi: 10.1002/ardp.200300758.

DOI:10.1002/ardp.200300758
PMID:12916059
Abstract

Some 5-acylaminoacylamino-benzophenone derivatives were designed as bisubstrate analogue farnesyltransferase inhibitors. These compounds turned out to be only weakly active against farnesyltransferase, but displayed an antiproliferative effect rendering them suitable for further development as a novel type of cytostatic agents.

摘要

一些5-酰基氨基酰基氨基二苯甲酮衍生物被设计为双底物类似物法尼基转移酶抑制剂。结果发现这些化合物对法尼基转移酶的活性较弱,但具有抗增殖作用,使其适合作为新型细胞抑制剂进一步开发。

相似文献

1
Non-thiol farnesyltransferase inhibitors: FTase-inhibition and cellular activity of benzophenone-based bisubstrate analogue farnesyltransferase inhibitors.非硫醇法尼基转移酶抑制剂:基于二苯甲酮的双底物类似物法尼基转移酶抑制剂的法尼基转移酶抑制作用及细胞活性
Arch Pharm (Weinheim). 2003 Jul;336(4-5):242-50. doi: 10.1002/ardp.200300758.
2
Non-thiol farnesyltransferase inhibitors: structure-activity relationships of benzophenone-based bisubstrate analogue farnesyltransferase inhibitors.非硫醇法尼基转移酶抑制剂:基于二苯甲酮的双底物类似物法尼基转移酶抑制剂的构效关系
Bioorg Med Chem. 2002 Mar;10(3):615-20. doi: 10.1016/s0968-0896(01)00312-1.
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Non-thiol farnesyltransferase inhibitors: N-(4-tolylacetylamino-3-benzoylphenyl)-3-arylfurylacrylic acid amides.非硫醇法尼基转移酶抑制剂:N-(4-甲苯基乙酰氨基-3-苯甲酰基苯基)-3-芳基呋喃基丙烯酸酰胺
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Non-thiol farnesyltransferase inhibitors: utilization of the far aryl binding site by 5-cinnamoylaminobenzophenones.非硫醇法尼基转移酶抑制剂:5-肉桂酰氨基二苯甲酮对远芳基结合位点的利用
Arch Pharm (Weinheim). 2004 Sep;337(9):493-501. doi: 10.1002/ardp.200400871.
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Non-thiol farnesyltransferase inhibitors: utilization of the near aryl binding site by 5-arylacetylaminobenzophenones.非硫醇法尼基转移酶抑制剂:5-芳基乙酰氨基二苯甲酮对近芳基结合位点的利用
Arch Pharm (Weinheim). 2004 Apr;337(4):213-8. doi: 10.1002/ardp.200300843.
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Non-thiol farnesyltransferase inhibitors: the concept of benzophenone-based bisubstrate analogue farnesyltransferase inhibitors.非硫醇法尼基转移酶抑制剂:基于二苯甲酮的双底物类似物法尼基转移酶抑制剂的概念
Eur J Med Chem. 2000 Jul-Aug;35(7-8):721-6. doi: 10.1016/s0223-5234(00)00162-8.
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Design, synthesis, and structure-activity relationships of tetrahydroquinoline-based farnesyltransferase inhibitors.基于四氢喹啉的法尼基转移酶抑制剂的设计、合成及构效关系
Bioorg Med Chem Lett. 2005 Apr 1;15(7):1895-9. doi: 10.1016/j.bmcl.2005.02.004.
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Non-thiol farnesyltransferase inhibitors: N-(4-aminoacylamino-3-benzoylphenyl)-3-[5-(4-nitrophenyl)-2 furyl]acrylic acid amides and their antimalarial activity.非硫醇法尼基转移酶抑制剂:N-(4-氨酰基氨基-3-苯甲酰基苯基)-3-[5-(4-硝基苯基)-2-呋喃基]丙烯酸酰胺及其抗疟活性。
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Non-thiol farnesyltransferase inhibitors: N-(4-Acylamino-3-benzoylphenyl)-4-nitrocinnamic acid amides.非硫醇法尼基转移酶抑制剂:N-(4-酰氨基-3-苯甲酰基苯基)-4-硝基肉桂酰胺
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Development of benzophenone-based farnesyltransferase inhibitors as novel antimalarials.基于二苯甲酮的法尼基转移酶抑制剂作为新型抗疟药的研发。
ChemMedChem. 2008 Aug;3(8):1217-31. doi: 10.1002/cmdc.200800043.

引用本文的文献

1
Protein farnesyltransferase-catalyzed isoprenoid transfer to peptide depends on lipid size and shape, not hydrophobicity.蛋白质法尼基转移酶催化的类异戊二烯向肽的转移取决于脂质的大小和形状,而非疏水性。
Chembiochem. 2008 Nov 24;9(17):2872-82. doi: 10.1002/cbic.200800248.
2
Unraveling the mechanism of the farnesyltransferase enzyme.解析法尼基转移酶的作用机制。
J Biol Inorg Chem. 2005 Jan;10(1):3-10. doi: 10.1007/s00775-004-0612-6. Epub 2004 Dec 21.