Design, Synthesis, and Evaluation of Tricyclic, Conformationally Constrained Small-Molecule Mimetics of Second Mitochondria-Derived Activator of Caspases

Zhang B; Nikolovska-Coleska Z; Zhang Y; Bai LC; Qiu S; Yang CY; Sun HY; Wang SM; Wu YK

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Design, Synthesis, and Evaluation of Tricyclic, Conformationally Constrained Small-Molecule Mimetics of Second Mitochondria-Derived Activator of Caspases

机译：第二个线粒体衍生的胱天蛋白酶激活剂的三环，构象受限的小分子模拟物的设计，合成和评估

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A series of tricyclic, conformationally constrained Smac mimetics have been designed, synthesized, and evaluated. The most potent compound 6 (WS-5) binds to XIAP, cIAP-1, and cIAP-2 with K-i of 18, 1.1, and 4.2 nM, respectively. Compound 6 antagonizes XIAP in a functional assay, induces cIAP-1 degradation, inhibits cell growth with an IC50 of 68 nM in the MDA-MB-231 cancer cell line, and effectively induces cancer cells to undergo apoptosis.

机译：设计，合成和评估了一系列三环，构象受限的Smac模拟物。最有效的化合物6（WS-5）与XIAP，cIAP-1和cIAP-2结合，K-i分别为18、1.1和4.2 nM。在功能测定中，化合物6拮抗XIAP，诱导cIAP-1降解，在MDA-MB-231癌细胞系中以68 nM的IC50抑制细胞生长，并有效诱导癌细胞凋亡。

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《Journal of Medicinal Chemistry》 |2008年第23期|共4页
作者
Zhang B; Nikolovska-Coleska Z; Zhang Y; Bai LC; Qiu S; Yang CY; Sun HY; Wang SM; Wu YK;
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正文语种 eng
中图分类药学;
关键词
ALPHA-DEPENDENT APOPTOSIS; XIAP BIR3 DOMAIN; STRUCTURAL BASIS; IAP PROTEINS; SMAC/DIABLO; POTENT; ANTAGONISTS; INHIBITION; BINDING; TARGET;

机译：依赖于细胞凋亡;XIAP BIR3域;结构基础;IAP蛋白质;SMAC /双抗体;强力;拮抗剂;抑制作用;结合;目标;

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1. Design, Synthesis, and Evaluation of Tricyclic, Conformationally Constrained Small-Molecule Mimetics of Second Mitochondria-Derived Activator of Caspases [J] . Zhang B, Nikolovska-Coleska Z, Zhang Y, Journal of Medicinal Chemistry . 2008,第23期

机译：第二个线粒体衍生的胱天蛋白酶激活剂的三环，构象受限的小分子模拟物的设计，合成和评估
2. Structure-based design, synthesis, and evaluation of conformationally constrained mimetics of the second mitochondria-derived activator of caspase that target the x-linked inhibitor of apoptosis protein/caspase-9 interaction site. [J] . Sun H, Nikolovska Coleska Z, Yang CY, Journal of Medicinal Chemistry . 2004,第17期

机译：基于结构的设计，合成和评估第二个线粒体衍生的caspase激活剂的构象约束模拟物，该模拟物靶向凋亡蛋白/ caspase-9相互作用位点的x连锁抑制剂。
3. Design, synthesis, and evaluation of a potent, cell-permeable, conformationally constrained second mitochondria derived activator of caspase (Smac) mimetic [J] . Sun HY, Nikolovska-Coleska Z, Lu JF, Journal of Medicinal Chemistry . 2006,第26期

机译：设计，合成和评估有效的，可渗透细胞的，受构象约束的第二个线粒体半胱天冬酶（Smac）模拟激活剂
4. Synthesis of Antagonistic Conformationally Constrained Lipid A Mimetics [C] . Artner D., Oblak A., Jerala R. International Carbohydrate Symposium . 2013

机译：拮抗构象的合成脂质的模拟方法
5. Design, synthesis, and evaluation of novel irreversible inhibitors for caspases. [D] . Dogan Ekici, Ozlem. 2003

机译：设计，合成和评估新型半胱氨酸蛋白酶不可逆抑制剂。
6. Design Synthesis and Evaluation of Tricyclic Conformationally Constrained Small-Molecule Mimetics of Second Mitochondria-derived Activator of Caspases [O] . Bin Zhang, Zaneta Nikolovska-Coleska, Yan Zhang, -1

机译：第二个线粒体衍生的胱天蛋白酶激活剂的三环构象受限的小分子模拟物的设计合成和评估
7. Design, Synthesis, and Evaluation of Potent, Nonpeptidic Mimetics of Second Mitochondria-Derived Activator of Caspases [O] . Wei Sun, Zaneta Nikolovska-Coleska, Dongguang Qin, 2009

机译：患有胱天术二线粒体衍生激活剂的有效，非肽模拟物的设计，合成和评价

Design, Synthesis, and Evaluation of Tricyclic, Conformationally Constrained Small-Molecule Mimetics of Second Mitochondria-Derived Activator of Caspases

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