BIOMARKERS

Molecular Biopsy of Human Tumors

- a resource for Precision Medicine *

213 related articles for article (PubMed ID: 24387221)

  • 1. 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]  

  • 2. 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]  

  • 3. 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]  

  • 4. 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]  

  • 5. 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]  

  • 6. 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]  

  • 7. The discovery of Polo-like kinase 4 inhibitors: design and optimization of spiro[cyclopropane-1,3'[3H]indol]-2'(1'H).ones as orally bioavailable antitumor agents.
    Sampson PB; Liu Y; Patel NK; Feher M; Forrest B; Li SW; Edwards L; Laufer R; Lang Y; Ban F; Awrey DE; Mao G; Plotnikova O; Leung G; Hodgson R; Mason JM; Wei X; Kiarash R; Green E; Qiu W; Chirgadze NY; Mak TW; Pan G; Pauls HW
    J Med Chem; 2015 Jan; 58(1):130-46. PubMed ID: 24867403
    [TBL] [Abstract][Full Text] [Related]  

  • 8. 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]  

  • 9. 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]  

  • 10. The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor agent.
    Sampson PB; Liu Y; Forrest B; Cumming G; Li SW; Patel NK; Edwards L; Laufer R; Feher M; Ban F; Awrey DE; Mao G; Plotnikova O; Hodgson R; Beletskaya I; Mason JM; Luo X; Nadeem V; Wei X; Kiarash R; Madeira B; Huang P; Mak TW; Pan G; Pauls HW
    J Med Chem; 2015 Jan; 58(1):147-69. PubMed ID: 25723005
    [TBL] [Abstract][Full Text] [Related]  

  • 11. 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]  

  • 12. Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK).
    Axten JM; Medina JR; Feng Y; Shu A; Romeril SP; Grant SW; Li WH; Heerding DA; Minthorn E; Mencken T; Atkins C; Liu Q; Rabindran S; Kumar R; Hong X; Goetz A; Stanley T; Taylor JD; Sigethy SD; Tomberlin GH; Hassell AM; Kahler KM; Shewchuk LM; Gampe RT
    J Med Chem; 2012 Aug; 55(16):7193-207. PubMed ID: 22827572
    [TBL] [Abstract][Full Text] [Related]  

  • 13. Discovery of 1-(4-(5-(5-amino-6-(5-tert-butyl-1,3,4-oxadiazol-2-yl)pyrazin-2-yl)-1-ethyl-1,2,4-triazol-3-yl)piperidin-1-yl)-3-hydroxypropan-1-one (AZD8835): A potent and selective inhibitor of PI3Kα and PI3Kδ for the treatment of cancers.
    Barlaam B; Cosulich S; Delouvrié B; Ellston R; Fitzek M; Germain H; Green S; Hancox U; Harris CS; Hudson K; Lambert-van der Brempt C; Lebraud H; Magnien F; Lamorlette M; Le Griffon A; Morgentin R; Ouvry G; Page K; Pasquet G; Polanska U; Ruston L; Saleh T; Vautier M; Ward L
    Bioorg Med Chem Lett; 2015 Nov; 25(22):5155-62. PubMed ID: 26475521
    [TBL] [Abstract][Full Text] [Related]  

  • 14. Discovery of (+)-N-(3-aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-[1,2]thiazolo[5,4-d]pyrimidin-6-yl)-2-methylpropyl]-4-methylbenzamide (AZD4877), a kinesin spindle protein inhibitor and potential anticancer agent.
    Theoclitou ME; Aquila B; Block MH; Brassil PJ; Castriotta L; Code E; Collins MP; Davies AM; Deegan T; Ezhuthachan J; Filla S; Freed E; Hu H; Huszar D; Jayaraman M; Lawson D; Lewis PM; Nadella MV; Oza V; Padmanilayam M; Pontz T; Ronco L; Russell D; Whitston D; Zheng X
    J Med Chem; 2011 Oct; 54(19):6734-50. PubMed ID: 21899292
    [TBL] [Abstract][Full Text] [Related]  

  • 15. Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disorders.
    Verhoest PR; Fonseca KR; Hou X; Proulx-Lafrance C; Corman M; Helal CJ; Claffey MM; Tuttle JB; Coffman KJ; Liu S; Nelson F; Kleiman RJ; Menniti FS; Schmidt CJ; Vanase-Frawley M; Liras S
    J Med Chem; 2012 Nov; 55(21):9045-54. PubMed ID: 22780914
    [TBL] [Abstract][Full Text] [Related]  

  • 16. Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
    Wang H; Yu N; Chen D; Lee KC; Lye PL; Chang JW; Deng W; Ng MC; Lu T; Khoo ML; Poulsen A; Sangthongpitag K; Wu X; Hu C; Goh KC; Wang X; Fang L; Goh KL; Khng HH; Goh SK; Yeo P; Liu X; Bonday Z; Wood JM; Dymock BW; Kantharaj E; Sun ET
    J Med Chem; 2011 Jul; 54(13):4694-720. PubMed ID: 21634430
    [TBL] [Abstract][Full Text] [Related]  

  • 17. 3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 2. Lead optimization.
    Pevarello P; Brasca MG; Orsini P; Traquandi G; Longo A; Nesi M; Orzi F; Piutti C; Sansonna P; Varasi M; Cameron A; Vulpetti A; Roletto F; Alzani R; Ciomei M; Albanese C; Pastori W; Marsiglio A; Pesenti E; Fiorentini F; Bischoff JR; Mercurio C
    J Med Chem; 2005 Apr; 48(8):2944-56. PubMed ID: 15828833
    [TBL] [Abstract][Full Text] [Related]  

  • 18. 2-Substituted aminopyrido[2,3-d]pyrimidin-7(8H)-ones. structure-activity relationships against selected tyrosine kinases and in vitro and in vivo anticancer activity.
    Klutchko SR; Hamby JM; Boschelli DH; Wu Z; Kraker AJ; Amar AM; Hartl BG; Shen C; Klohs WD; Steinkampf RW; Driscoll DL; Nelson JM; Elliott WL; Roberts BJ; Stoner CL; Vincent PW; Dykes DJ; Panek RL; Lu GH; Major TC; Dahring TK; Hallak H; Bradford LA; Showalter HD; Doherty AM
    J Med Chem; 1998 Aug; 41(17):3276-92. PubMed ID: 9703473
    [TBL] [Abstract][Full Text] [Related]  

  • 19. Discovery of 2-(6-{[(6-fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor.
    Moffat D; Patel S; Day F; Belfield A; Donald A; Rowlands M; Wibawa J; Brotherton D; Stimson L; Clark V; Owen J; Bawden L; Box G; Bone E; Mortenson P; Hardcastle A; van Meurs S; Eccles S; Raynaud F; Aherne W
    J Med Chem; 2010 Dec; 53(24):8663-78. PubMed ID: 21080647
    [TBL] [Abstract][Full Text] [Related]  

  • 20. Discovery of a First-in-Class, Potent, Selective, and Orally Bioavailable Inhibitor of the p97 AAA ATPase (CB-5083).
    Zhou HJ; Wang J; Yao B; Wong S; Djakovic S; Kumar B; Rice J; Valle E; Soriano F; Menon MK; Madriaga A; Kiss von Soly S; Kumar A; Parlati F; Yakes FM; Shawver L; Le Moigne R; Anderson DJ; Rolfe M; Wustrow D
    J Med Chem; 2015 Dec; 58(24):9480-97. PubMed ID: 26565666
    [TBL] [Abstract][Full Text] [Related]  

    [Next]    [New Search]
    of 11.