Discovering and developing PI3 kinase inhibitors for cancer: Rapid progress through academic-biotech-pharma interactions

Molecular Cancer Therapeutics

Volumn 10, Issue 11, 2011, Pages 2017-2018

  Raynaud, Florence I ^a   Workman, Paul ^a  

^a INSTITUTE OF CANCER RESEARCH   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

2 (1H INDAZOL 4 YL) 6 (4 METHANESULFONYL 1 PIPERAZINYLMETHYL) 4 MORPHOLINOTHIENO[3,2 D]PYRIMIDINE; 2 (4 HYDROXYPHENYL) 4 MORPHOLINOPYRIDO[3',2':4,5]FURO[3,2 D]PYRIMIDINE; MAMMALIAN TARGET OF RAPAMYCIN; PHOSPHATIDYLINOSITOL 3 KINASE; PHOSPHATIDYLINOSITOL 3 KINASE INHIBITOR; PHOSPHATIDYLINOSITOL 3,4,5 TRISPHOSPHATE 3 PHOSPHATASE; PI 540; PI 620; PROTEIN P110; PROTEIN P110ALPHA; PROTEIN P110BETA; PROTEIN P110DELTA; PROTEIN P110GAMMA; UNCLASSIFIED DRUG;

ANTINEOPLASTIC ACTIVITY; CANCER CELL CULTURE; CANCER RESEARCH; CLINICAL RESEARCH; DRUG INDUSTRY; GENE; GENE FREQUENCY; GENE MUTATION; GENE SILENCING; GLIOBLASTOMA; HUMAN; NEOPLASM; NONHUMAN; PRIORITY JOURNAL; SHORT SURVEY; TUMOR SUPPRESSOR GENE; TUMOR XENOGRAFT;

ANIMALS; ENZYME INHIBITORS; FEMALE; FURANS; GLIOBLASTOMA; HUMANS; INDAZOLES; OVARIAN NEOPLASMS; PHOSPHATIDYLINOSITOL 3-KINASES; PYRIDINES; PYRIMIDINES; SULFONAMIDES; THIOPHENES;

EID: 81055150380     PISSN: 15357163     EISSN: 15388514     Source Type: Journal    
DOI: 10.1158/1535-7163.MCT-11-0739     Document Type: Short Survey

References (5)

1. Hayakawa M, Kaizawa H, Moritomo H, Koizumi T, Ohishi T, Yamano M, et al. Synthesis and biological evaluation of pyrido[3′,2′:4,5]furo[3,2-d] pyrimidine derivatives as novel PI3 kinase p110alpha inhibitors. Bioorg Med Chem Lett 2007;17:2438-42. (Pubitemid 46507793)
2. Raynaud FI, Eccles S, Clarke PA, Hayes A, Nutley B, Alix S, et al. Pharmacologic characterization of a potent inhibitor of class I phosphatidylinositide 3-kinases. Cancer Res 2007;67:5840-50. (Pubitemid 46985018)
3. Folkes AJ, Ahmadi K, Alderton WK, Alix S, Baker SJ, Box G, et al. 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. J Med Chem 2008;51: 5522-32.
4. Workman P, Clarke PA, Raynaud FI, van Montfort RL. Drugging the PI3 kinome: from chemical tools to drugs in the clinic. Cancer Res 2010;70: 2146-57.
5. Shuttleworth SJ, Silva FA, Cecil AR, Tomassi CD, Hill TJ, Raynaud FI, et al. Progress in the preclinical discovery and clinical development of class I and dual class I/IV phosphoinositide 3-kinase (PI3K) inhibitors. Curr Med Chem 2011;18:2686-2714.