BIOMARKERS

Molecular Biopsy of Human Tumors

- a resource for Precision Medicine *

187 related articles for article (PubMed ID: 22524426)

  • 1. Discovery and optimization of new benzimidazole- and benzoxazole-pyrimidone selective PI3Kβ inhibitors for the treatment of phosphatase and TENsin homologue (PTEN)-deficient cancers.
    Certal V; Halley F; Virone-Oddos A; Delorme C; Karlsson A; Rak A; Thompson F; Filoche-Rommé B; El-Ahmad Y; Carry JC; Abecassis PY; Lejeune P; Vincent L; Bonnevaux H; Nicolas JP; Bertrand T; Marquette JP; Michot N; Benard T; Below P; Vade I; Chatreaux F; Lebourg G; Pilorge F; Angouillant-Boniface O; Louboutin A; Lengauer C; Schio L
    J Med Chem; 2012 May; 55(10):4788-805. PubMed ID: 22524426
    [TBL] [Abstract][Full Text] [Related]  

  • 2. Discovery and optimization of pyrimidone indoline amide PI3Kβ inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers.
    Certal V; Carry JC; Halley F; Virone-Oddos A; Thompson F; Filoche-Rommé B; El-Ahmad Y; Karlsson A; Charrier V; Delorme C; Rak A; Abecassis PY; Amara C; Vincent L; Bonnevaux H; Nicolas JP; Mathieu M; Bertrand T; Marquette JP; Michot N; Benard T; Perrin MA; Lemaitre O; Guerif S; Perron S; Monget S; Gruss-Leleu F; Doerflinger G; Guizani H; Brollo M; Delbarre L; Bertin L; Richepin P; Loyau V; Garcia-Echeverria C; Lengauer C; Schio L
    J Med Chem; 2014 Feb; 57(3):903-20. PubMed ID: 24387221
    [TBL] [Abstract][Full Text] [Related]  

  • 3. Concomitant Inhibition of PI3Kβ and BRAF or MEK in PTEN-Deficient/BRAF-Mutant Melanoma Treatment: Preclinical Assessment of SAR260301 Oral PI3Kβ-Selective Inhibitor.
    Bonnevaux H; Lemaitre O; Vincent L; Levit MN; Windenberger F; Halley F; Delorme C; Lengauer C; Garcia-Echeverria C; Virone-Oddos A
    Mol Cancer Ther; 2016 Jul; 15(7):1460-71. PubMed ID: 27196754
    [TBL] [Abstract][Full Text] [Related]  

  • 4. Rational design of phosphoinositide 3-kinase α inhibitors that exhibit selectivity over the phosphoinositide 3-kinase β isoform.
    Heffron TP; Wei B; Olivero A; Staben ST; Tsui V; Do S; Dotson J; Folkes AJ; Goldsmith P; Goldsmith R; Gunzner J; Lesnick J; Lewis C; Mathieu S; Nonomiya J; Shuttleworth S; Sutherlin DP; Wan NC; Wang S; Wiesmann C; Zhu BY
    J Med Chem; 2011 Nov; 54(22):7815-33. PubMed ID: 21985639
    [TBL] [Abstract][Full Text] [Related]  

  • 5. Preparation and optimization of new 4-(morpholin-4-yl)-(6-oxo-1,6-dihydropyrimidin-2-yl)amide derivatives as PI3Kβ inhibitors.
    Certal V; Halley F; Virone-Oddos A; Thompson F; Filoche-Rommé B; El-Ahmad Y; Carry JC; Delorme C; Karlsson A; Abecassis PY; Vincent L; Bonnevaux H; Nicolas JP; Morales R; Michot N; Vade I; Louboutin A; Perron S; Doerflinger G; Tric B; Monget S; Lengauer C; Schio L
    Bioorg Med Chem Lett; 2012 Oct; 22(20):6381-4. PubMed ID: 22981333
    [TBL] [Abstract][Full Text] [Related]  

  • 6. Discovery of 9-(1-anilinoethyl)-2-morpholino-4-oxo-pyrido[1,2-a]pyrimidine-7-carboxamides as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours.
    Barlaam B; Cosulich S; Degorce S; Fitzek M; Giordanetto F; Green S; Inghardt T; Hennequin L; Hancox U; Lambert-van der Brempt C; Morgentin R; Pass S; Plé P; Saleh T; Ward L
    Bioorg Med Chem Lett; 2014 Aug; 24(16):3928-35. PubMed ID: 24992874
    [TBL] [Abstract][Full Text] [Related]  

  • 7. Discovery of (R)-8-(1-(3,5-difluorophenylamino)ethyl)-N,N-dimethyl-2-morpholino-4-oxo-4H-chromene-6-carboxamide (AZD8186): a potent and selective inhibitor of PI3Kβ and PI3Kδ for the treatment of PTEN-deficient cancers.
    Barlaam B; Cosulich S; Degorce S; Fitzek M; Green S; Hancox U; Lambert-van der Brempt C; Lohmann JJ; Maudet M; Morgentin R; Pasquet MJ; Péru A; Plé P; Saleh T; Vautier M; Walker M; Ward L; Warin N
    J Med Chem; 2015 Jan; 58(2):943-62. PubMed ID: 25514658
    [TBL] [Abstract][Full Text] [Related]  

  • 8. Synthesis and biological evaluation of novel analogues of the pan class I phosphatidylinositol 3-kinase (PI3K) inhibitor 2-(difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-1H-benzimidazole (ZSTK474).
    Rewcastle GW; Gamage SA; Flanagan JU; Frederick R; Denny WA; Baguley BC; Kestell P; Singh R; Kendall JD; Marshall ES; Lill CL; Lee WJ; Kolekar S; Buchanan CM; Jamieson SM; Shepherd PR
    J Med Chem; 2011 Oct; 54(20):7105-26. PubMed ID: 21882832
    [TBL] [Abstract][Full Text] [Related]  

  • 9. Design, synthesis, and evaluation of orally active benzimidazoles and benzoxazoles as vascular endothelial growth factor-2 receptor tyrosine kinase inhibitors.
    Potashman MH; Bready J; Coxon A; DeMelfi TM; DiPietro L; Doerr N; Elbaum D; Estrada J; Gallant P; Germain J; Gu Y; Harmange JC; Kaufman SA; Kendall R; Kim JL; Kumar GN; Long AM; Neervannan S; Patel VF; Polverino A; Rose P; Plas Sv; Whittington D; Zanon R; Zhao H
    J Med Chem; 2007 Sep; 50(18):4351-73. PubMed ID: 17696416
    [TBL] [Abstract][Full Text] [Related]  

  • 10. Discovery and optimization of a series of benzothiazole phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors.
    D'Angelo ND; Kim TS; Andrews K; Booker SK; Caenepeel S; Chen K; D'Amico D; Freeman D; Jiang J; Liu L; McCarter JD; San Miguel T; Mullady EL; Schrag M; Subramanian R; Tang J; Wahl RC; Wang L; Whittington DA; Wu T; Xi N; Xu Y; Yakowec P; Yang K; Zalameda LP; Zhang N; Hughes P; Norman MH
    J Med Chem; 2011 Mar; 54(6):1789-811. PubMed ID: 21332118
    [TBL] [Abstract][Full Text] [Related]  

  • 11. Discovery of a Phosphoinositide 3-Kinase (PI3K) β/δ Inhibitor for the Treatment of Phosphatase and Tensin Homolog (PTEN) Deficient Tumors: Building PI3Kβ Potency in a PI3Kδ-Selective Template by Targeting Nonconserved Asp856.
    Perreault S; Chandrasekhar J; Cui ZH; Evarts J; Hao J; Kaplan JA; Kashishian A; Keegan KS; Kenney T; Koditek D; Lad L; Lepist EI; McGrath ME; Patel L; Phillips B; Therrien J; Treiberg J; Yahiaoui A; Phillips G
    J Med Chem; 2017 Feb; 60(4):1555-1567. PubMed ID: 28106991
    [TBL] [Abstract][Full Text] [Related]  

  • 12. Synthesis and structure-activity relationships of imidazo[1,2-a]pyrimidin-5(1H)-ones as a novel series of beta isoform selective phosphatidylinositol 3-kinase inhibitors.
    Lin H; Erhard K; Hardwicke MA; Luengo JI; Mack JF; McSurdy-Freed J; Plant R; Raha K; Rominger CM; Sanchez RM; Schaber MD; Schulz MJ; Spengler MD; Tedesco R; Xie R; Zeng JJ; Rivero RA
    Bioorg Med Chem Lett; 2012 Mar; 22(6):2230-4. PubMed ID: 22361133
    [TBL] [Abstract][Full Text] [Related]  

  • 13. Discovery of (2S)-8-[(3R)-3-methylmorpholin-4-yl]-1-(3-methyl-2-oxobutyl)-2-(trifluoromethyl)-3,4-dihydro-2H-pyrimido[1,2-a]pyrimidin-6-one: a novel potent and selective inhibitor of Vps34 for the treatment of solid tumors.
    Pasquier B; El-Ahmad Y; Filoche-Rommé B; Dureuil C; Fassy F; Abecassis PY; Mathieu M; Bertrand T; Benard T; Barrière C; El Batti S; Letallec JP; Sonnefraud V; Brollo M; Delbarre L; Loyau V; Pilorge F; Bertin L; Richepin P; Arigon J; Labrosse JR; Clément J; Durand F; Combet R; Perraut P; Leroy V; Gay F; Lefrançois D; Bretin F; Marquette JP; Michot N; Caron A; Castell C; Schio L; McCort G; Goulaouic H; Garcia-Echeverria C; Ronan B
    J Med Chem; 2015 Jan; 58(1):376-400. PubMed ID: 25402320
    [TBL] [Abstract][Full Text] [Related]  

  • 14. Enhancement of DC vaccine potency by activating the PI3K/AKT pathway with a small interfering RNA targeting PTEN.
    Kim JH; Kang TH; Noh KH; Kim SH; Lee YH; Kim KW; Bae HC; Ahn YH; Choi EY; Kim JS; Lee KM; Kim TW
    Immunol Lett; 2010 Nov; 134(1):47-54. PubMed ID: 20727912
    [TBL] [Abstract][Full Text] [Related]  

  • 15. Design of selective, ATP-competitive inhibitors of Akt.
    Freeman-Cook KD; Autry C; Borzillo G; Gordon D; Barbacci-Tobin E; Bernardo V; Briere D; Clark T; Corbett M; Jakubczak J; Kakar S; Knauth E; Lippa B; Luzzio MJ; Mansour M; Martinelli G; Marx M; Nelson K; Pandit J; Rajamohan F; Robinson S; Subramanyam C; Wei L; Wythes M; Morris J
    J Med Chem; 2010 Jun; 53(12):4615-22. PubMed ID: 20481595
    [TBL] [Abstract][Full Text] [Related]  

  • 16. CEP-7055: a novel, orally active pan inhibitor of vascular endothelial growth factor receptor tyrosine kinases with potent antiangiogenic activity and antitumor efficacy in preclinical models.
    Ruggeri B; Singh J; Gingrich D; Angeles T; Albom M; Yang S; Chang H; Robinson C; Hunter K; Dobrzanski P; Jones-Bolin S; Pritchard S; Aimone L; Klein-Szanto A; Herbert JM; Bono F; Schaeffer P; Casellas P; Bourie B; Pili R; Isaacs J; Ator M; Hudkins R; Vaught J; Mallamo J; Dionne C
    Cancer Res; 2003 Sep; 63(18):5978-91. PubMed ID: 14522925
    [TBL] [Abstract][Full Text] [Related]  

  • 17. Discovery of 3H-benzo[4,5]thieno[3,2-d]pyrimidin-4-ones as potent, highly selective, and orally bioavailable inhibitors of the human protooncogene proviral insertion site in moloney murine leukemia virus (PIM) kinases.
    Tao ZF; Hasvold LA; Leverson JD; Han EK; Guan R; Johnson EF; Stoll VS; Stewart KD; Stamper G; Soni N; Bouska JJ; Luo Y; Sowin TJ; Lin NH; Giranda VS; Rosenberg SH; Penning TD
    J Med Chem; 2009 Nov; 52(21):6621-36. PubMed ID: 19842661
    [TBL] [Abstract][Full Text] [Related]  

  • 18. Structure-based design of potent and selective 3-phosphoinositide-dependent kinase-1 (PDK1) inhibitors.
    Medina JR; Becker CJ; Blackledge CW; Duquenne C; Feng Y; Grant SW; Heerding D; Li WH; Miller WH; Romeril SP; Scherzer D; Shu A; Bobko MA; Chadderton AR; Dumble M; Gardiner CM; Gilbert S; Liu Q; Rabindran SK; Sudakin V; Xiang H; Brady PG; Campobasso N; Ward P; Axten JM
    J Med Chem; 2011 Mar; 54(6):1871-95. PubMed ID: 21341675
    [TBL] [Abstract][Full Text] [Related]  

  • 19. Pyrrole-3-carboxamides as potent and selective JAK2 inhibitors.
    Brasca MG; Nesi M; Avanzi N; Ballinari D; Bandiera T; Bertrand J; Bindi S; Canevari G; Carenzi D; Casero D; Ceriani L; Ciomei M; Cirla A; Colombo M; Cribioli S; Cristiani C; Della Vedova F; Fachin G; Fasolini M; Felder ER; Galvani A; Isacchi A; Mirizzi D; Motto I; Panzeri A; Pesenti E; Vianello P; Gnocchi P; Donati D
    Bioorg Med Chem; 2014 Sep; 22(17):4998-5012. PubMed ID: 25009002
    [TBL] [Abstract][Full Text] [Related]  

  • 20. Discovery of a series of 8-(1-phenylpyrrolidin-2-yl)-6-carboxamide-2-morpholino-4H-chromen-4-one as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours.
    Barlaam B; Cosulich S; Degorce S; Ellston R; Fitzek M; Green S; Hancox U; Lambert-van der Brempt C; Lohmann JJ; Maudet M; Morgentin R; Plé P; Ward L; Warin N
    Bioorg Med Chem Lett; 2017 May; 27(9):1949-1954. PubMed ID: 28347666
    [TBL] [Abstract][Full Text] [Related]  

    [Next]    [New Search]
    of 10.