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Items: 1 to 20 of 104

1.

Discovery of 4-phenyl-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and orally active PI3K/mTOR dual inhibitors.

Yan G, Pu C, Lan S, Zhong X, Zhou M, Hou X, Yang J, Shan H, Zhao L, Li R.

Eur J Med Chem. 2019 Sep 15;178:667-686. doi: 10.1016/j.ejmech.2019.06.021. Epub 2019 Jun 13.

PMID:
31228810
2.

Discovery of 2-(2-aminopyrimidin-5-yl)-4-morpholino-N-(pyridin-3-yl)quinazolin-7-amines as novel PI3K/mTOR inhibitors and anticancer agents.

Peng W, Tu ZC, Long ZJ, Liu Q, Lu G.

Eur J Med Chem. 2016 Jan 27;108:644-654. doi: 10.1016/j.ejmech.2015.11.038. Epub 2015 Dec 2.

PMID:
26731167
3.

Characterization of LY3023414, a Novel PI3K/mTOR Dual Inhibitor Eliciting Transient Target Modulation to Impede Tumor Growth.

Smith MC, Mader MM, Cook JA, Iversen P, Ajamie R, Perkins E, Bloem L, Yip YY, Barda DA, Waid PP, Zeckner DJ, Young DA, Sanchez-Felix M, Donoho GP, Wacheck V.

Mol Cancer Ther. 2016 Oct;15(10):2344-2356. Epub 2016 Jul 20.

4.

4-methylpteridinones as orally active and selective PI3K/mTOR dual inhibitors.

Liu KK, Bagrodia S, Bailey S, Cheng H, Chen H, Gao L, Greasley S, Hoffman JE, Hu Q, Johnson TO, Knighton D, Liu Z, Marx MA, Nambu MD, Ninkovic S, Pascual B, Rafidi K, Rodgers CM, Smith GL, Sun S, Wang H, Yang A, Yuan J, Zou A.

Bioorg Med Chem Lett. 2010 Oct 15;20(20):6096-9. doi: 10.1016/j.bmcl.2010.08.045. Epub 2010 Aug 14.

PMID:
20817449
5.

Structure-based optimization leads to the discovery of NSC765844, a highly potent, less toxic and orally efficacious dual PI3K/mTOR inhibitor.

Han J, Chen Y, Yang C, Liu T, Wang M, Xu H, Zhang L, Zheng C, Song Y, Zhu J.

Eur J Med Chem. 2016 Oct 21;122:684-701. doi: 10.1016/j.ejmech.2016.06.030. Epub 2016 Jun 23.

PMID:
27448924
6.

Discovery of 1-(3-aryl-4-chlorophenyl)-3-(p-aryl)urea derivatives against breast cancer by inhibiting PI3K/Akt/mTOR and Hedgehog signalings.

Li W, Sun Q, Song L, Gao C, Liu F, Chen Y, Jiang Y.

Eur J Med Chem. 2017 Dec 1;141:721-733. doi: 10.1016/j.ejmech.2017.09.002. Epub 2017 Oct 6.

PMID:
29107429
7.

Novel anti-prostate cancer scaffold identified by the combination of in silico and cell-based assays targeting the PI3K-AKT-mTOR pathway.

Saidel MÉ, Dos Santos KC, Nagano LFP, Montanari CA, Leitão A.

Bioorg Med Chem Lett. 2017 Sep 1;27(17):4001-4006. doi: 10.1016/j.bmcl.2017.07.061. Epub 2017 Jul 24.

PMID:
28774426
8.

Discovery of benzenesulfonamide derivatives as potent PI3K/mTOR dual inhibitors with in vivo efficacies against hepatocellular carcinoma.

Chen Y, Zhang L, Yang C, Han J, Wang C, Zheng C, Zhou Y, Lv J, Song Y, Zhu J.

Bioorg Med Chem. 2016 Mar 1;24(5):957-66. doi: 10.1016/j.bmc.2016.01.008. Epub 2016 Jan 6.

PMID:
26819001
9.

Design, synthesis and biological evaluation of novel series of 2H-benzo[b][1,4]oxazin-3(4H)-one and 2H-benzo[b][1,4]oxazine scaffold derivatives as PI3Kα inhibitors.

Dong FD, Liu DD, Deng CL, Qin XC, Chen K, Wang J, Song HR, Ding HW.

Bioorg Med Chem. 2018 Aug 7;26(14):3982-3991. doi: 10.1016/j.bmc.2018.06.022. Epub 2018 Jun 18.

PMID:
29937355
10.

Benzo[b]furan derivatives induces apoptosis by targeting the PI3K/Akt/mTOR signaling pathway in human breast cancer cells.

Kamal A, Lakshma Nayak V, Nagesh N, Vishnuvardhan MV, Subba Reddy NV.

Bioorg Chem. 2016 Jun;66:124-31. doi: 10.1016/j.bioorg.2016.04.004. Epub 2016 Apr 26.

PMID:
27149364
11.

5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology.

Beaufils F, Cmiljanovic N, Cmiljanovic V, Bohnacker T, Melone A, Marone R, Jackson E, Zhang X, Sele A, Borsari C, Mestan J, Hebeisen P, Hillmann P, Giese B, Zvelebil M, Fabbro D, Williams RL, Rageot D, Wymann MP.

J Med Chem. 2017 Sep 14;60(17):7524-7538. doi: 10.1021/acs.jmedchem.7b00930. Epub 2017 Sep 1.

12.

2-Arylthiazolidine-4-carboxylic acid amides (ATCAA) target dual pathways in cancer cells: 5'-AMP-activated protein kinase (AMPK)/mTOR and PI3K/Akt/mTOR pathways.

Li CM, Narayanan R, Lu Y, Hurh E, Coss CC, Barrett CM, Miller DD, Dalton JT.

Int J Oncol. 2010 Oct;37(4):1023-30.

PMID:
20811725
13.

Biological characterization of SN32976, a selective inhibitor of PI3K and mTOR with preferential activity to PI3Kα, in comparison to established pan PI3K inhibitors.

Rewcastle GW, Kolekar S, Buchanan CM, Gamage SA, Giddens AC, Tsang KY, Kendall JD, Singh R, Lee WJ, Smith GC, Han W, Matthews DJ, Denny WA, Shepherd PR, Jamieson SMF.

Oncotarget. 2017 Jul 18;8(29):47725-47740. doi: 10.18632/oncotarget.17730.

14.

Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Leukemia.

Liang X, Liu X, Wang B, Zou F, Wang A, Qi S, Chen C, Zhao Z, Wang W, Qi Z, Lv F, Hu Z, Wang L, Zhang S, Liu Q, Liu J.

J Med Chem. 2016 Mar 10;59(5):1984-2004. doi: 10.1021/acs.jmedchem.5b01618. Epub 2016 Feb 5.

PMID:
26789553
15.

Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity.

Maira SM, Stauffer F, Brueggen J, Furet P, Schnell C, Fritsch C, Brachmann S, Chène P, De Pover A, Schoemaker K, Fabbro D, Gabriel D, Simonen M, Murphy L, Finan P, Sellers W, García-Echeverría C.

Mol Cancer Ther. 2008 Jul;7(7):1851-63. doi: 10.1158/1535-7163.MCT-08-0017. Epub 2008 Jul 7.

16.

Pro-apoptotic and pro-autophagic effects of the Aurora kinase A inhibitor alisertib (MLN8237) on human osteosarcoma U-2 OS and MG-63 cells through the activation of mitochondria-mediated pathway and inhibition of p38 MAPK/PI3K/Akt/mTOR signaling pathway.

Niu NK, Wang ZL, Pan ST, Ding HQ, Au GH, He ZX, Zhou ZW, Xiao G, Yang YX, Zhang X, Yang T, Chen XW, Qiu JX, Zhou SF.

Drug Des Devel Ther. 2015 Mar 12;9:1555-84. doi: 10.2147/DDDT.S74197. eCollection 2015.

17.

Efficacy of the dual PI3K and mTOR inhibitor NVP-BEZ235 in combination with imatinib mesylate against chronic myelogenous leukemia cell lines.

Xin P, Li C, Zheng Y, Peng Q, Xiao H, Huang Y, Zhu X.

Drug Des Devel Ther. 2017 Apr 3;11:1115-1126. doi: 10.2147/DDDT.S132092. eCollection 2017.

18.
19.

Antitumor activity and induction of TP53-dependent apoptosis toward ovarian clear cell adenocarcinoma by the dual PI3K/mTOR inhibitor DS-7423.

Kashiyama T, Oda K, Ikeda Y, Shiose Y, Hirota Y, Inaba K, Makii C, Kurikawa R, Miyasaka A, Koso T, Fukuda T, Tanikawa M, Shoji K, Sone K, Arimoto T, Wada-Hiraike O, Kawana K, Nakagawa S, Matsuda K, McCormick F, Aburatani H, Yano T, Osuga Y, Fujii T.

PLoS One. 2014 Feb 4;9(2):e87220. doi: 10.1371/journal.pone.0087220. eCollection 2014.

20.

Identification of 2-oxatriazines as highly potent pan-PI3K/mTOR dual inhibitors.

Dehnhardt CM, Venkatesan AM, Chen Z, Delos-Santos E, Ayral-Kaloustian S, Brooijmans N, Yu K, Hollander I, Feldberg L, Lucas J, Mallon R.

Bioorg Med Chem Lett. 2011 Aug 15;21(16):4773-8. doi: 10.1016/j.bmcl.2011.06.063. Epub 2011 Jun 21.

PMID:
21763134

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