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Structure-based design of an organoruthenium phosphatidyl-inositol-3-kinase inhibitor reveals a switch governing lipid kinase potency and selectivity.

Xie P, Williams DS, Atilla-Gokcumen GE, Milk L, Xiao M, Smalley KS, Herlyn M, Meggers E, Marmorstein R.

ACS Chem Biol. 2008 May 16;3(5):305-16. doi: 10.1021/cb800039y.


A novel inhibitor of the PI3K/Akt pathway based on the structure of inositol 1,3,4,5,6-pentakisphosphate.

Falasca M, Chiozzotto D, Godage HY, Mazzoletti M, Riley AM, Previdi S, Potter BV, Broggini M, Maffucci T.

Br J Cancer. 2010 Jan 5;102(1):104-14. doi: 10.1038/sj.bjc.6605408.


Maleimide-functionalised organoruthenium anticancer agents and their binding to thiol-containing biomolecules.

Hanif M, Nazarov AA, Legin A, Groessl M, Arion VB, Jakupec MA, Tsybin YO, Dyson PJ, Keppler BK, Hartinger CG.

Chem Commun (Camb). 2012 Feb 1;48(10):1475-7. doi: 10.1039/c1cc14713g.


Structure of anticancer ruthenium half-sandwich complex bound to glycogen synthase kinase 3β.

Atilla-Gokcumen GE, Di Costanzo L, Meggers E.

J Biol Inorg Chem. 2011 Jan;16(1):45-50. doi: 10.1007/s00775-010-0699-x.


Complexation with organometallic ruthenium pharmacophores enhances the ability of 4-anilinoquinazolines inducing apoptosis.

Zheng W, Luo Q, Lin Y, Zhao Y, Wang X, Du Z, Hao X, Yu Y, Lü S, Ji L, Li X, Yang L, Wang F.

Chem Commun (Camb). 2013 Nov 11;49(87):10224-6. doi: 10.1039/c3cc43000f. Erratum in: Chem Commun (Camb). 2013 Dec 28;49(100):11826.


Design, synthesis and biological evaluation of novel 4-alkynyl-quinoline derivatives as PI3K/mTOR dual inhibitors.

Lv X, Ying H, Ma X, Qiu N, Wu P, Yang B, Hu Y.

Eur J Med Chem. 2015 Jun 24;99:36-50. doi: 10.1016/j.ejmech.2015.05.025.


Structure guided optimization of a fragment hit to imidazopyridine inhibitors of PI3K.

Pecchi S, Ni ZJ, Han W, Smith A, Lan J, Burger M, Merritt H, Wiesmann M, Chan J, Kaufman S, Knapp MS, Janssen J, Huh K, Voliva CF.

Bioorg Med Chem Lett. 2013 Aug 15;23(16):4652-6. doi: 10.1016/j.bmcl.2013.06.010.


Synthesis and characterization of a novel prostate cancer-targeted phosphatidylinositol-3-kinase inhibitor prodrug.

Baiz D, Pinder TA, Hassan S, Karpova Y, Salsbury F, Welker ME, Kulik G.

J Med Chem. 2012 Sep 27;55(18):8038-46.


Rational design of selective organoruthenium inhibitors of protein tyrosine phosphatase 1B.

Ong JX, Yap CW, Ang WH.

Inorg Chem. 2012 Nov 19;51(22):12483-92. doi: 10.1021/ic301884j.


The Selective PI3K Inhibitor XL147 (SAR245408) Inhibits Tumor Growth and Survival and Potentiates the Activity of Chemotherapeutic Agents in Preclinical Tumor Models.

Foster P, Yamaguchi K, Hsu PP, Qian F, Du X, Wu J, Won KA, Yu P, Jaeger CT, Zhang W, Marlowe CK, Keast P, Abulafia W, Chen J, Young J, Plonowski A, Yakes FM, Chu F, Engell K, Bentzien F, Lam ST, Dale S, Yturralde O, Matthews DJ, Lamb P, Laird AD.

Mol Cancer Ther. 2015 Apr;14(4):931-40. doi: 10.1158/1535-7163.MCT-14-0833.


Multi-targeted organometallic ruthenium(II)-arene anticancer complexes bearing inhibitors of poly(ADP-ribose) polymerase-1: A strategy to improve cytotoxicity.

Wang Z, Qian H, Yiu SM, Sun J, Zhu G.

J Inorg Biochem. 2014 Feb;131:47-55. doi: 10.1016/j.jinorgbio.2013.10.017.


Identification and structure-activity relationship of 2-morpholino 6-(3-hydroxyphenyl) pyrimidines, a class of potent and selective PI3 kinase inhibitors.

Pecchi S, Renhowe PA, Taylor C, Kaufman S, Merritt H, Wiesmann M, Shoemaker KR, Knapp MS, Ornelas E, Hendrickson TF, Fantl W, Voliva CF.

Bioorg Med Chem Lett. 2010 Dec 1;20(23):6895-8. doi: 10.1016/j.bmcl.2010.10.021.


WJD008, a dual phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin inhibitor, prevents PI3K signaling and inhibits the proliferation of transformed cells with oncogenic PI3K mutant.

Li T, Wang J, Wang X, Yang N, Chen SM, Tong LJ, Yang CH, Meng LH, Ding J.

J Pharmacol Exp Ther. 2010 Sep 1;334(3):830-8. doi: 10.1124/jpet.110.167940.


GDC-0980 is a novel class I PI3K/mTOR kinase inhibitor with robust activity in cancer models driven by the PI3K pathway.

Wallin JJ, Edgar KA, Guan J, Berry M, Prior WW, Lee L, Lesnick JD, Lewis C, Nonomiya J, Pang J, Salphati L, Olivero AG, Sutherlin DP, O'Brien C, Spoerke JM, Patel S, Lensun L, Kassees R, Ross L, Lackner MR, Sampath D, Belvin M, Friedman LS.

Mol Cancer Ther. 2011 Dec;10(12):2426-36. doi: 10.1158/1535-7163.MCT-11-0446.


DW09849, a selective phosphatidylinositol 3-kinase (PI3K) inhibitor, prevents PI3K signaling and preferentially inhibits proliferation of cells containing the oncogenic mutation p110α (H1047R).

Liu JL, Gao GR, Zhang X, Cao SF, Guo CL, Wang X, Tong LJ, Ding J, Duan WH, Meng LH.

J Pharmacol Exp Ther. 2014 Mar;348(3):432-41. doi: 10.1124/jpet.113.210724.


Antitumor activity of ZSTK474, a new phosphatidylinositol 3-kinase inhibitor.

Yaguchi S, Fukui Y, Koshimizu I, Yoshimi H, Matsuno T, Gouda H, Hirono S, Yamazaki K, Yamori T.

J Natl Cancer Inst. 2006 Apr 19;98(8):545-56.


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.


Organometallic compounds with biological activity: a very selective and highly potent cellular inhibitor for glycogen synthase kinase 3.

Atilla-Gokcumen GE, Williams DS, Bregman H, Pagano N, Meggers E.

Chembiochem. 2006 Sep;7(9):1443-50.


Synthesis and cancer stem cell-based activity of substituted 5-morpholino-7H-thieno[3,2-b]pyran-7-ones designed as next generation PI3K inhibitors.

Morales GA, Garlich JR, Su J, Peng X, Newblom J, Weber K, Durden DL.

J Med Chem. 2013 Mar 14;56(5):1922-39. doi: 10.1021/jm301522m.

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