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The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer .

Folkes AJ, Ahmadi K, Alderton WK, Alix S, Baker SJ, Box G, Chuckowree IS, Clarke PA, Depledge P, Eccles SA, Friedman LS, Hayes A, Hancox TC, Kugendradas A, Lensun L, Moore P, Olivero AG, Pang J, Patel S, Pergl-Wilson GH, Raynaud FI, Robson A, Saghir N, Salphati L, Sohal S, Ultsch MH, Valenti M, Wallweber HJ, Wan NC, Wiesmann C, Workman P, Zhyvoloup A, Zvelebil MJ, Shuttleworth SJ
J Med Chem 51 5522-32 (2008)
Cited: 419 times
EuropePMC logo PMID: 18754654

Abstract

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.

Reviews - 3dbs mentioned but not cited (5)

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Articles - 3dbs mentioned but not cited (12)

  1. Discovery of 1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one as a highly potent, selective mammalian target of rapamycin (mTOR) inhibitor for the treatment of cancer. Liu Q, Chang JW, Wang J, Kang SA, Thoreen CC, Markhard A, Hur W, Zhang J, Sim T, Sabatini DM, Gray NS. J Med Chem 53 7146-7155 (2010)
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  3. Kinome-wide selectivity profiling of ATP-competitive mammalian target of rapamycin (mTOR) inhibitors and characterization of their binding kinetics. Liu Q, Kirubakaran S, Hur W, Niepel M, Westover K, Thoreen CC, Wang J, Ni J, Patricelli MP, Vogel K, Riddle S, Waller DL, Traynor R, Sanda T, Zhao Z, Kang SA, Zhao J, Look AT, Sorger PK, Sabatini DM, Gray NS. J Biol Chem 287 9742-9752 (2012)
  4. Why Some Targets Benefit from beyond Rule of Five Drugs. Egbert M, Whitty A, Keserű GM, Vajda S. J Med Chem 62 10005-10025 (2019)
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  8. CK-3, A Novel Methsulfonyl Pyridine Derivative, Suppresses Hepatocellular Carcinoma Proliferation and Invasion by Blocking the PI3K/AKT/mTOR and MAPK/ERK Pathways. Wu Q, Liu TY, Hu BC, Li X, Wu YT, Sun XT, Jiang XW, Wang S, Qin XC, Ding HW, Zhao QC. Front Oncol 11 717626 (2021)
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  10. Design, synthesis, and biological evaluation of new thieno[2,3-d] pyrimidine derivatives as targeted therapy for PI3K with molecular modelling study. Elmenier FM, Lasheen DS, Abouzid KAM. J Enzyme Inhib Med Chem 37 315-332 (2022)
  11. The Guareschi Pyridine Scaffold as a Valuable Platform for the Identification of Selective PI3K Inhibitors. Galli U, Ciraolo E, Massarotti A, Margaria JP, Sorba G, Hirsch E, Tron GC. Molecules 20 17275-17287 (2015)
  12. The mechanisms of Huangqi Guizhi Wuwu decoction in treating ischaemic stroke based on network pharmacology and experiment verification. Liao W, Wang M, Wu Y, Du J, Li Y, Su A, Zhong L, Xie Z, Gong M, Liang J, Wang P, Liu Z, Wang L. Pharm Biol 61 1014-1029 (2023)


Reviews citing this publication (94)

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Articles citing this publication (308)

  1. Ligand-independent HER2/HER3/PI3K complex is disrupted by trastuzumab and is effectively inhibited by the PI3K inhibitor GDC-0941. Junttila TT, Akita RW, Parsons K, Fields C, Lewis Phillips GD, Friedman LS, Sampath D, Sliwkowski MX. Cancer Cell 15 429-440 (2009)
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