The discovery of novel benzofuran-2-carboxylic acids as potent Pim-1 inhibitors.

Xiang Y; Hirth B; Asmussen G; Biemann HP; Bishop KA; Good A; Fitzgerald M; Gladysheva T; Jain A; Jancsics K; Liu J; Metz M; Papoulis A; Skerlj R; Stepp JD; Wei RR

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The discovery of novel benzofuran-2-carboxylic acids as potent Pim-1 inhibitors.

机译：新型苯并呋喃-2-羧酸作为有效的Pim-1抑制剂的发现。

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Novel benzofuran-2-carboxylic acids, exemplified by 29, 38 and 39, have been discovered as potent Pim-1 inhibitors using fragment based screening followed by X-ray structure guided medicinal chemistry optimization. The compounds demonstrate potent inhibition against Pim-1 and Pim-2 in enzyme assays. Compound 29 has been tested in the Ambit 442 kinase panel and demonstrates good selectivity for the Pim kinase family. X-ray structures of the inhibitor/Pim-1 binding complex reveal important salt-bridge and hydrogen bond interactions mediated by the compound's carboxylic acid and amino groups.

机译：使用基于片段的筛选，然后通过X射线结构指导药物化学优化，发现了新型的苯并呋喃-2-羧酸，以29、38和39为例，是有效的Pim-1抑制剂。该化合物在酶分析中显示出对Pim-1和Pim-2的有效抑制作用。化合物29已在Ambit 442激酶面板中进行测试，证明对Pim激酶家族具有良好的选择性。抑制剂/ Pim-1结合复合物的X射线结构揭示了化合物的羧酸和氨基介导的重要的盐桥和氢键相互作用。

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《Bioorganic and Medicinal Chemistry Letters》 |2011年第10期|共7页
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Xiang Y; Hirth B; Asmussen G; Biemann HP; Bishop KA; Good A; Fitzgerald M; Gladysheva T; Jain A; Jancsics K; Liu J; Metz M; Papoulis A; Skerlj R; Stepp JD; Wei RR;
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1. The discovery of novel benzofuran-2-carboxylic acids as potent Pim-1 inhibitors. [J] . Xiang Y, Hirth B, Asmussen G, Bioorganic and Medicinal Chemistry Letters . 2011,第10期

机译：新型苯并呋喃-2-羧酸作为有效的Pim-1抑制剂的发现。
2. Discovery of beta-benzamido hydroxamic acids as potent, selective, and orally bioavailable TACE inhibitors. [J] . Duan JJ, Chen L, Lu Z, Bioorganic and Medicinal Chemistry Letters . 2008,第1期

机译：发现了β-苯甲酰胺基异羟肟酸作为有效，选择性和口服可生物利用的TACE抑制剂。
3. Discovery of pyrimidyl-5-hydroxamic acids as new potent histone deacetylase inhibitors. [J] . Angibaud P, Arts J, Van Emelen K, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2005,第6期

机译：发现嘧啶基-5-异羟肟酸作为新型有效的组蛋白脱乙酰基酶抑制剂。
4. Ultrafiltration Tandem Mass Spectrometry Based Screening Assay for the Discovery of Bcl-2 Family Antiapoptotic Protein Inhibitors. [C] . Suma Ramagiri, Fei Ma, Eldon Geisert, ASMS Conference on Mass Spectrometry and Allied Topics . 2008

机译：超滤串联质谱基于Bcl-2家族抗凋亡蛋白抑制剂发现的筛选试验。
5. Biochemical Characterization of FIKK Kinase from Cryptosporidium parvum and Discovery of Potent Inhibitors. [D] . Osman, Khan Tanjid. 2016

机译：小隐隐孢子虫FIKK激酶的生化特征和有效抑制剂的发现。
6. Discovery and Optimization of Macrocyclic Quinoxaline-pyrrolo-dihydropiperidinonesas Potent Pim-1/2 Kinase Inhibitors [O] . Victor J. Cee, *, Frank Chavez Jr., 2016

机译：大环喹喔啉-吡咯并-二氢哌啶子酮的发现和优化作为有效的Pim-1 / 2激酶抑制剂
7. Fragment-hopping-based discovery of a novel chemical series of proto-oncogene PIM-1 kinase inhibitors. [O] . Gustavo Saluste, Maria I Albarran, Rosa M Alvarez, 2012

机译：基于片段跳跃的新型化学系列原癌基因pIm-1激酶抑制剂的发现。

The discovery of novel benzofuran-2-carboxylic acids as potent Pim-1 inhibitors.

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