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The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-t hieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer .
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2008 Sep 25 , DOI: 10.1021/jm800295d Adrian J. Folkes 1 , Khatereh Ahmadi 1 , Wendy K. Alderton 1 , Sonia Alix 1 , Stewart J. Baker 1 , Gary Box 1 , Irina S. Chuckowree 1 , Paul A. Clarke 1 , Paul Depledge 1 , Suzanne A. Eccles 1 , Lori S. Friedman 1 , Angela Hayes 1 , Timothy C. Hancox 1 , Arumugam Kugendradas 1 , Letitia Lensun 1 , Pauline Moore 1 , Alan G. Olivero 1 , Jodie Pang 1 , Sonal Patel 1 , Giles H. Pergl-Wilson 1 , Florence I. Raynaud 1 , Anthony Robson 1 , Nahid Saghir 1 , Laurent Salphati 1 , Sukhjit Sohal 1 , Mark H. Ultsch 1 , Melanie Valenti 1 , Heidi J.A. Wallweber 1 , Nan Chi Wan 1 , Christian Wiesmann 1 , Paul Workman 1 , Alexander Zhyvoloup 1 , Marketa J. Zvelebil 1 , Stephen J. Shuttleworth 1
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2008 Sep 25 , DOI: 10.1021/jm800295d Adrian J. Folkes 1 , Khatereh Ahmadi 1 , Wendy K. Alderton 1 , Sonia Alix 1 , Stewart J. Baker 1 , Gary Box 1 , Irina S. Chuckowree 1 , Paul A. Clarke 1 , Paul Depledge 1 , Suzanne A. Eccles 1 , Lori S. Friedman 1 , Angela Hayes 1 , Timothy C. Hancox 1 , Arumugam Kugendradas 1 , Letitia Lensun 1 , Pauline Moore 1 , Alan G. Olivero 1 , Jodie Pang 1 , Sonal Patel 1 , Giles H. Pergl-Wilson 1 , Florence I. Raynaud 1 , Anthony Robson 1 , Nahid Saghir 1 , Laurent Salphati 1 , Sukhjit Sohal 1 , Mark H. Ultsch 1 , Melanie Valenti 1 , Heidi J.A. Wallweber 1 , Nan Chi Wan 1 , Christian Wiesmann 1 , Paul Workman 1 , Alexander Zhyvoloup 1 , Marketa J. Zvelebil 1 , Stephen J. Shuttleworth 1
Affiliation
Phosphatidylinositol-3-kinase (PI3K) is an important target in cancer due to the deregulation of the PI3K/ Akt signaling pathway in a wide variety of tumors. A series of thieno[3,2-d]pyrimidine derivatives were prepared and evaluated as inhibitors of PI3 kinase p110alpha. The synthesis, biological activity, and further profiling of these compounds are described. This work resulted in the discovery of 17, GDC-0941, which is a potent, selective, orally bioavailable inhibitor of PI3K and is currently being evaluated in human clinical trials for the treatment of cancer.
中文翻译：
2-（1H-吲唑-4-基）-6-（4-甲磺酰基-哌嗪-1-基甲基）-4-吗啉-4-基-t [[3,2-d]嘧啶（GDC- 0941）作为I类PI3激酶的有效，选择性，口服生物利用抑制剂，用于治疗癌症。
磷脂酰肌醇-3-激酶（PI3K）是癌症中的重要靶标，因为在多种肿瘤中，PI3K / Akt信号通路的失控。制备了一系列的噻吩并[3,2-d]嘧啶衍生物，并作为PI3激酶p110alpha的抑制剂进行了评估。描述了这些化合物的合成，生物学活性和进一步的概况分析。这项工作导致发现了17种GDC-0941，它是一种有效的，选择性的，口服生物利用的PI3K抑制剂，目前正在人类临床试验中评估其治疗癌症的能力。
更新日期：2017-01-31
中文翻译：
2-（1H-吲唑-4-基）-6-（4-甲磺酰基-哌嗪-1-基甲基）-4-吗啉-4-基-t [[3,2-d]嘧啶（GDC- 0941）作为I类PI3激酶的有效，选择性，口服生物利用抑制剂，用于治疗癌症。
磷脂酰肌醇-3-激酶（PI3K）是癌症中的重要靶标，因为在多种肿瘤中，PI3K / Akt信号通路的失控。制备了一系列的噻吩并[3,2-d]嘧啶衍生物，并作为PI3激酶p110alpha的抑制剂进行了评估。描述了这些化合物的合成，生物学活性和进一步的概况分析。这项工作导致发现了17种GDC-0941，它是一种有效的，选择性的，口服生物利用的PI3K抑制剂，目前正在人类临床试验中评估其治疗癌症的能力。
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