| [1] | Vivanco I, Sawyers CL, The phosphatidylinositol 3,kinase AKT pathway in human cancer[J]. Nat Rev Cancer, 2002,2(7):489-501. |
| [2] | Bjornsti MA, Houghton PJ, The TOR pathway:a target for cancer therapy[J]. Nat Rev Cancer, 2004,4(5):335-348. |
| [3] | Workman P, Clarke PA, Raynaud FI,et al.Drugging the PI3 kinome:from chemical tools to drugs in the clinic[J]. Cancer Res, 2010,70(6):2146-2157. |
| [4] | Denley A, Kang S, Karst U,et al.Oncogenic signaling of class I PI3K isoforms[J]. Oncogene, 2008, 27(18):2561-2574. |
| [5] | Falasca M, Maffucci T, Role of class Ⅱ phosphoinositide 3-kinase in cell signalling[J]. Biochem Soc Trans, 2007,35(Pt 2):211-214. |
| [6] | Guertin DA, Sabatini DM. Defining the role of mTOR in cancer[J]. Cancer Cell, 2007,12(1):9-22. |
| [7] | Bunney TD, Katan M.Phosphoinositide signalling in cancer:beyond PI3K and PTEN[J]. Nat Rev Cancer, 2010,10(5):342-352. |
| [8] | Bussink J, van der Kogel AJ, Kaanders JH, Activation of the PI3,K/AKT pathway and implications for radioresistance mechanisms in head and neck cancer[J]. Lancet Oncol, 2008,9(3):288-296. |
| [9] | Massion PP, Kuo WL, Stokoe D,et al. Genomic copy number analysis of non-small cell lung cancer using array comparative genomic hybridization:implications of the phosphatidylinositol 3-kinase pathway[J]. Cancer Res, 2002,62(13):3636-3640. |
| [10] | Sutherlin DP, Bao L, Berry M,et al. Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer[J]. J Med Chem, 2011,54(21):7579-7587. |
| [11] | Wu P, Hu YZ.Small molecules targeting phosphoinositide 3-kinases[J]. Med Chem Comm, 2012,3(11):1337-1355. |
| [12] | Garlich JR, De P, Dey N,et al. A vascular targeted pan phosphoinositide 3-kinase inhibitor prodrug, SF1126, with antitumor and antiangiogenic activity[J]. Cancer Res, 2008,68(1):206-215. |
| [13] | Ozbay T, Durden DL, Liu T,et al. In vitro evaluation of pan-PI3-kinase inhibitor SF1126 in trastuzumab-sensitive and trastuzumab-resistant HER2-over-expressing breast cancer cells[J]. Cancer Chemother Pharmacol, 2010,65(4):697-706. |
| [14] | Stauffer F, Maira SM, Furet P,et al. Imidazo[4,5-c]quinolines as inhibitors of the PI3K/PKB-pathway[J]. Bioorg Med Chem Lett, 2008,18(3):1027-1030. |
| [15] | Knight SD, Adams ND, Burgess JL,et al. Discovery of GSK2126458, a highly potent Inhibitor of PI3K and the mammalian target of rapamycin[J]. Acs Med Chem Lett, 2010,1(1):39-43. |
| [16] | Venkatesan AM, Dehnhardt CM, Delos SE,et al. Bis(morpholino-1,3,5-triazine)derivatives:potent adenosine 5'-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors:discovery of compound 26(PKI-587), a highly efficacious dual Inhibitor[J]. J Med Chem, 2010,53(6):2636-2645. |
| [17] | Dehnhardt CM, Venkatesan AM, Delos SE,et al. Lead optimization of N-3-substituted 7-morpholinotriazolopyrimidines as dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors:discovery of PKI-402[J]. J Med Chem, 2010,53(2):798-810. |
| [18] | Mallon R, Feldberg LR, Lucas J, et al.Antitumor efficacy of PKI-587, a highly potent dual PI3K/mTOR kinase inhibitor[J]. Clin Cancer Res, 2011,17(10):3193-3203. |
| [19] | Cheng HM, Bagrodia S, Bailey S,et al. Discovery of the highly potent PI3K/mTOR dual inhibitor PF-04691502 through structure based drug design[J]. Med Chem Comm, 2010,1(2):139-144. |
| [20] | Markman B, Tabernero J,Krop I,et al. Phase I safety, pharmacokinetic, and pharmacodynamic study of the oral phosphatidylinositol-3-kinase and mTOR inhibitor BGT226 in patients with advanced solid tumors[J]. Ann Oncol, 2012,23(9):2399-2408. |
| [21] | Heffron TP, Berry M, Castanedo G,et al. Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor[J]. Bioorg Med Chem Lett, 2010,20(8):2408-2411. |
| [22] | Kashiyama T, Oda K, Ikeda Y,et al.Antitumor efficacy of DS-7423, a novel PI3K/mTOR dual inhibitor, in ovarian clear cell adenocarcinoma[J]. Eur J Cancer, 2012,48:110-111. |