Discovery and SAR of Thiazolidine-2,4-dione Analogues as Insulin-like Growth Factor-1 Receptor (IGF-1R) Inhibitors via Hierarchical Virtual Screening

机译：噻唑烷-2,4-二酮类似物作为胰岛素样生长因子-1受体（IGF-1R）抑制剂的发现和SAR通过分层虚拟筛选

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Insulin-like growth factor-1 receptor (IGF-1R) is a growth factor receptor tyrosine kinase acting as a critical mediator of cell proliferation and survival. Novel 5-benzylidenethiazolidine-2,4-dione (5) and 5(furan-2-ylmethylene)thiazolidine-2,4-dione (6) compounds were identified as potent and selective IGF-1R inhibitors via hierarchical virtual screening. Initial SAR and biological activity of the analogues of 5 and 6 with thiazolidine-2,4-dione template are presented, and several inhibitors with low nanomolar potency are reported.

机译：胰岛素样生长因子-1受体（IGF-1R）是一种生长因子受体酪氨酸激酶，是细胞增殖和存活的关键介质。通过分级虚拟筛选，鉴定出新颖的5-苄叉基噻唑烷-2,4-二酮（5）和5（呋喃-2-基亚甲基）噻唑烷-2,4-二酮（6）化合物为有效和选择性的IGF-1R抑制剂。介绍了具有噻唑烷-2,4-二酮模板的5和6类似物的初始SAR和生物活性，并报道了几种低纳摩尔效能的抑制剂。

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《ICMSI;International conference of molecular simulations and applied informatics technologies》|2010年|p.642-646|共5页
会议地点 Wuhan(CN);Wuhan(CN)
作者
Xiaofeng Liu; Hua Xie; Cheng Luo; Linjiang Tong; Yi Wang; Ting Peng; Jian Ding; Hualiang Jiang; Honglin Li;
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Drug Discovery and Design Center Shanghai Institute of Materia Medica Chinese Academy of Sciences Shanghai 201203 China Shanghai Key Laboratory of Chemical Biology School of Pharmacy East China University of Science and Technology Shanghai 200237 China;

Division of Anti-Tumor Pharmacology State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Chinese Academy of Sciences Shanghai 201203 China;

Drug Discovery and Design Center Shanghai Institute of Materia Medica Chinese Academy of Sciences Shanghai 201203 China;

Division of Anti-Tumor Pharmacology State Key Laboratory of Drug Research Shang;

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1. Discovery and SAR of Thiazolidine-2,4-dione Analogues as Insulin-like Growth Factor-1 Receptor (IGF-1R) Inhibitors via Hierarchical Virtual Screening [J] . Liu XF, Xie H, Luo C, Journal of Medicinal Chemistry . 2010,第6期

机译：噻唑烷-2,4-二酮类似物作为胰岛素样生长因子-1受体（IGF-1R）抑制剂的发现和SAR通过分层虚拟筛选
2. Insulin-like growth factor-1 receptor (IGF-1R) kinase inhibitors: SAR of a series of 3-(6-(4-substituted-piperazin-1-yl)-4-methyl-1H-benzimidazol-2-yl)-1H-pyridine-2- one. [J] . Velaparthi U, Saulnier MG, Wittman MD, Bioorganic and Medicinal Chemistry Letters . 2010,第10期

机译：胰岛素样生长因子1受体（IGF-1R）激酶抑制剂：一系列3-（6-（4-取代-哌嗪-1-基）-4-甲基-1H-苯并咪唑-2-基）的SAR -1H-吡啶-2-一。
3. Discovery of a Potent, Selective, Orally Bioavailable, and Efficacious Novel 2-(Pyrazol-4-ylamino)-pyrimidine Inhibitor of the Insulin-like Growth Factor-1 Receptor (IGF-1R) [J] . Degorce Sebastien L., Boyd Scott, Curwen Jon O., Journal of Medicinal Chemistry . 2016,第10期

机译：胰岛素样生长因子-1受体（IGF-1R）的有效，选择性，口服，生物有效的新型2-（Pyrazol-4-ylamino）-嘧啶抑制剂的发现。
4. Discovery and SAR of Thiazolidine-2,4-dione Analogues as Insulin-like Growth Factor-1 Receptor (IGF-1R) Inhibitors via Hierarchical Virtual Screening [C] . Xiaofeng Liu, Hua Xie, Cheng Luo, International conference of molecular simulations and applied informatics technologies . 2010

机译：噻唑烷-2,4-二酮类似物的发现和SAR作为胰岛素样生长因子-1受体（IGF-1R）抑制剂，通过分层虚拟筛选
5. Development of an insturmal method to evaluate insulin receptors and insulin-like growth factor-1 receptors homodimers and hybrid receptors in breast cancer. [D] . Shebani, Karima A. 2016

机译：开发了一种评估乳腺癌中胰岛素受体和胰岛素样生长因子-1受体同型二聚体和杂合受体的可靠方法。
6. Insulin-like growth factor-1 receptor (IGF-1R) as a biomarker for resistance to the tyrosine kinase inhibitor gefitinib in non-small cell lung cancer [O] . Nir Peled, Murry W. Wynes, Norihiko Ikeda, -1

机译：胰岛素样生长因子-1受体（IGF-1R）作为非小细胞肺癌对酪氨酸激酶抑制剂吉非替尼耐药的生物标志物
7. Discovery and SAR of Thiazolidine-2,4-dione Analogues as Insulin-like Growth Factor-1 Receptor (IGF-1R) Inhibitors via Hierarchical Virtual Screening [O] . Honglin Li 2009

机译：通过分层虚拟筛选发现噻唑烷-2,4-二酮类似物作为胰岛素样生长因子-1受体（IGF-1R）抑制剂

Discovery and SAR of Thiazolidine-2,4-dione Analogues as Insulin-like Growth Factor-1 Receptor (IGF-1R) Inhibitors via Hierarchical Virtual Screening

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