Optimization of pyrazole-containing 1,2,4-triazolo-[3,4-b]thiadiazines, a new class of STAT3 pathway inhibitors

LaPorte Matthew G.; Wang Zhuzhu; Colombo Raffaele; Garzan Atefeh; Peshkov Vsevolod A.; Liang Mary; Johnston Paul A.; Schurdak Mark E.; Sen Malabika; Camarco Daniel P.; Hua Yun; Pollock Netanya I.; Lazo John S.; Grandis Jennifer R.; Wipf Peter; Huryn Donna M.

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Optimization of pyrazole-containing 1,2,4-triazolo-[3,4-b]thiadiazines, a new class of STAT3 pathway inhibitors

机译：新型STAT3途径抑制剂-含吡唑的1,2,4-三唑-[3,4-b]噻二嗪的优化

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Structure-activity relationship studies of a 1,2,4-triazolo-[3,4-b] thiadiazine scaffold, identified in an HTS campaign for selective STAT3 pathway inhibitors, determined that a pyrazole group and specific aryl substitution on the thiadiazine were necessary for activity. Improvements in potency and metabolic stability were accomplished by the introduction of an a-methyl group on the thiadiazine. Optimized compounds exhibited anti-proliferative activity, reduction of phosphorylated STAT3 levels and effects on STAT3 target genes. These compounds represent a starting point for further drug discovery efforts targeting the STAT3 pathway. (C) 2016 Elsevier Ltd. All rights reserved.

机译：在HTS运动中针对选择性STAT3途径抑制剂确定的1,2,4-三唑并-[3,4-b]噻二嗪支架的结构活性关系研究确定，噻二嗪上的吡唑基和特定的芳基取代是必要的活动。通过在噻二嗪上引入α-甲基来实现效力和代谢稳定性的改善。优化的化合物具有抗增殖活性，磷酸化的STAT3水平降低以及对STAT3目标基因的影响。这些化合物代表了针对STAT3途径的进一步药物发现努力的起点。（C）2016 Elsevier Ltd.保留所有权利。

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《Bioorganic and Medicinal Chemistry Letters》 |2016年第15期|共5页
作者
LaPorte Matthew G.; Wang Zhuzhu; Colombo Raffaele; Garzan Atefeh; Peshkov Vsevolod A.; Liang Mary; Johnston Paul A.; Schurdak Mark E.; Sen Malabika; Camarco Daniel P.; Hua Yun; Pollock Netanya I.; Lazo John S.; Grandis Jennifer R.; Wipf Peter; Huryn Donna M.;
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STAT3 inhibitor; Triazolo-thiadiazines; Anti-cancer agents; STAT1;

机译：STAT3抑制剂;三唑并噻二嗪;抗癌药;STAT1;

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1. Optimization of pyrazole-containing 1,2,4-triazolo-[3,4-b]thiadiazines, a new class of STAT3 pathway inhibitors [J] . LaPorte Matthew G., Wang Zhuzhu, Colombo Raffaele, Bioorganic and Medicinal Chemistry Letters . 2016,第15期

机译：新型STAT3途径抑制剂-含吡唑的1,2,4-三唑-[3,4-b]噻二嗪的优化
2. Design, Synthesis, and Biological Evaluation of Novel 7H-[1,2,4]Triazolo[3,4-b][1,3,4]thiadiazine Inhibitors as Antitumor Agents [J] . Muhammad I. Ismail, Samy Mohamady, Nermin Samir, ACS Omega . 2020,第32期

机译：新型7H-[1,2,4]三唑唑[3,4-B] [1,3,4]噻二嗪抑制剂作为抗肿瘤剂的设计，合成和生物学评价
3. Safety and Efficacy of New 3,6-diaryl-7H- [1,2,4]triazolo[3,4-b][1,3,4]thiadiazine Analogs as Potential Phosphodiesterase-4 Inhibitors in NIH- 3T3 Mouse Fibroblastic Cells [J] . Maryam Baeeri, Alireza Foroumadi, Maryam Motamedi, Chemical biology and drug design . 2011,第3期

机译：新的3,6-二芳基-7H- [1,2,4]三唑[3,4-b] [1,3,4]噻二嗪类似物作为潜在的磷酸二酯酶-4抑制剂在NIH-3T3小鼠成纤维细胞中的安全性和有效性
4. A New Method for the Synthesis of Novel S-Triazolo3,4-b 1,3,4Thiadiazines [C] . Sattar Ebrahimi, Naser Foroughifar, Akbar Mobinikhaledi European Symposium on Organic Chemistry . 2009

机译：新型S-Tri唑的合成方法3,4-B 1,3,4噻二嗪
5. Silibinin Inhibits Glioblastoma Cell Proliferation via AKT/S6/4EBP1 and STAT3 Signaling Pathways In Vitro. [D] . Us, Ilkay. 2014

机译：水飞蓟宾通过AKT / S6 / 4EBP1和STAT3信号通路体外抑制胶质母细胞瘤细胞增殖。
6. Optimization of pyrazole-containing 124-triazolo-34-bthiadiazines a new class of STAT3 pathway inhibitors [O] . Matthew G. LaPorte, Zhuzhu Wang, Raffaele Colombo, -1

机译：新型STAT3途径抑制剂-含吡唑的124-三唑-34-b噻二嗪的优化
7. Synthesis of 4-amino-5-(3-chlorobenzo[b]thien-2-yl)-3-mercapto-1,2,4-triazolo[3,4-b][1,3,4]thiadiazoles and triazolo[3,4,b][1,3,4]thiadiazines under classical and microwave conditions [O] . E. S. H. El Ashry, A. A. Kassem, H. Abdel-Hamid, 2006

机译：4-氨基-5-（3-氯苯并[b]噻吩-2-基）-3-巯基-1,2,4-三唑并[3,4-b] [1,3,4]噻二唑和三唑并吡喃的合成在经典和微波条件下[3,4，b] [1,3,4]噻二嗪

Optimization of pyrazole-containing 1,2,4-triazolo-[3,4-b]thiadiazines, a new class of STAT3 pathway inhibitors

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