BIOMARKERS

Molecular Biopsy of Human Tumors

- a resource for Precision Medicine *

249 related articles for article (PubMed ID: 15546730)

  • 1. Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56(Lck) inhibitors.
    Chen P; Norris D; Das J; Spergel SH; Wityak J; Leith L; Zhao R; Chen BC; Pitt S; Pang S; Shen DR; Zhang R; De Fex HF; Doweyko AM; McIntyre KW; Shuster DJ; Behnia K; Schieven GL; Barrish JC
    Bioorg Med Chem Lett; 2004 Dec; 14(24):6061-6. PubMed ID: 15546730
    [TBL] [Abstract][Full Text] [Related]  

  • 2. Structure-guided design of aminopyrimidine amides as potent, selective inhibitors of lymphocyte specific kinase: synthesis, structure-activity relationships, and inhibition of in vivo T cell activation.
    DiMauro EF; Newcomb J; Nunes JJ; Bemis JE; Boucher C; Chai L; Chaffee SC; Deak HL; Epstein LF; Faust T; Gallant P; Gore A; Gu Y; Henkle B; Hsieh F; Huang X; Kim JL; Lee JH; Martin MW; McGowan DC; Metz D; Mohn D; Morgenstern KA; Oliveira-dos-Santos A; Patel VF; Powers D; Rose PE; Schneider S; Tomlinson SA; Tudor YY; Turci SM; Welcher AA; Zhao H; Zhu L; Zhu X
    J Med Chem; 2008 Mar; 51(6):1681-94. PubMed ID: 18321037
    [TBL] [Abstract][Full Text] [Related]  

  • 3. Imidazoquinoxaline Src-family kinase p56Lck inhibitors: SAR, QSAR, and the discovery of (S)-N-(2-chloro-6-methylphenyl)-2-(3-methyl-1-piperazinyl)imidazo- [1,5-a]pyrido[3,2-e]pyrazin-6-amine (BMS-279700) as a potent and orally active inhibitor with excellent in vivo antiinflammatory activity.
    Chen P; Doweyko AM; Norris D; Gu HH; Spergel SH; Das J; Moquin RV; Lin J; Wityak J; Iwanowicz EJ; McIntyre KW; Shuster DJ; Behnia K; Chong S; de Fex H; Pang S; Pitt S; Shen DR; Thrall S; Stanley P; Kocy OR; Witmer MR; Kanner SB; Schieven GL; Barrish JC
    J Med Chem; 2004 Aug; 47(18):4517-29. PubMed ID: 15317463
    [TBL] [Abstract][Full Text] [Related]  

  • 4. 2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase inhibitor.
    Das J; Chen P; Norris D; Padmanabha R; Lin J; Moquin RV; Shen Z; Cook LS; Doweyko AM; Pitt S; Pang S; Shen DR; Fang Q; de Fex HF; McIntyre KW; Shuster DJ; Gillooly KM; Behnia K; Schieven GL; Wityak J; Barrish JC
    J Med Chem; 2006 Nov; 49(23):6819-32. PubMed ID: 17154512
    [TBL] [Abstract][Full Text] [Related]  

  • 5. Structure-based design of novel 2-amino-6-phenyl-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as potent and orally active inhibitors of lymphocyte specific kinase (Lck): synthesis, SAR, and in vivo anti-inflammatory activity.
    Martin MW; Newcomb J; Nunes JJ; Boucher C; Chai L; Epstein LF; Faust T; Flores S; Gallant P; Gore A; Gu Y; Hsieh F; Huang X; Kim JL; Middleton S; Morgenstern K; Oliveira-dos-Santos A; Patel VF; Powers D; Rose P; Tudor Y; Turci SM; Welcher AA; Zack D; Zhao H; Zhu L; Zhu X; Ghiron C; Ermann M; Johnston D; Saluste CG
    J Med Chem; 2008 Mar; 51(6):1637-48. PubMed ID: 18278858
    [TBL] [Abstract][Full Text] [Related]  

  • 6. Novel 2-aminopyrimidine carbamates as potent and orally active inhibitors of Lck: synthesis, SAR, and in vivo antiinflammatory activity.
    Martin MW; Newcomb J; Nunes JJ; McGowan DC; Armistead DM; Boucher C; Buchanan JL; Buckner W; Chai L; Elbaum D; Epstein LF; Faust T; Flynn S; Gallant P; Gore A; Gu Y; Hsieh F; Huang X; Lee JH; Metz D; Middleton S; Mohn D; Morgenstern K; Morrison MJ; Novak PM; Oliveira-dos-Santos A; Powers D; Rose P; Schneider S; Sell S; Tudor Y; Turci SM; Welcher AA; White RD; Zack D; Zhao H; Zhu L; Zhu X; Ghiron C; Amouzegh P; Ermann M; Jenkins J; Johnston D; Napier S; Power E
    J Med Chem; 2006 Aug; 49(16):4981-91. PubMed ID: 16884310
    [TBL] [Abstract][Full Text] [Related]  

  • 7. N-(3-(phenylcarbamoyl)arylpyrimidine)-5-carboxamides as potent and selective inhibitors of Lck: structure, synthesis and SAR.
    Deak HL; Newcomb JR; Nunes JJ; Boucher C; Cheng AC; DiMauro EF; Epstein LF; Gallant P; Hodous BL; Huang X; Lee JH; Patel VF; Schneider S; Turci SM; Zhu X
    Bioorg Med Chem Lett; 2008 Feb; 18(3):1172-6. PubMed ID: 18083554
    [TBL] [Abstract][Full Text] [Related]  

  • 8. Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity.
    DiMauro EF; Newcomb J; Nunes JJ; Bemis JE; Boucher C; Buchanan JL; Buckner WH; Cee VJ; Chai L; Deak HL; Epstein LF; Faust T; Gallant P; Geuns-Meyer SD; Gore A; Gu Y; Henkle B; Hodous BL; Hsieh F; Huang X; Kim JL; Lee JH; Martin MW; Masse CE; McGowan DC; Metz D; Mohn D; Morgenstern KA; Oliveira-dos-Santos A; Patel VF; Powers D; Rose PE; Schneider S; Tomlinson SA; Tudor YY; Turci SM; Welcher AA; White RD; Zhao H; Zhu L; Zhu X
    J Med Chem; 2006 Sep; 49(19):5671-86. PubMed ID: 16970394
    [TBL] [Abstract][Full Text] [Related]  

  • 9. Development of N-4,6-pyrimidine-N-alkyl-N'-phenyl ureas as orally active inhibitors of lymphocyte specific tyrosine kinase.
    Maier JA; Brugel TA; Sabat M; Golebiowski A; Laufersweiler MJ; VanRens JC; Hopkins CR; De B; Hsieh LC; Brown KK; Easwaran V; Janusz MJ
    Bioorg Med Chem Lett; 2006 Jul; 16(14):3646-50. PubMed ID: 16682201
    [TBL] [Abstract][Full Text] [Related]  

  • 10. Discovery of thienopyridines as Src-family selective Lck inhibitors.
    Abbott L; Betschmann P; Burchat A; Calderwood DJ; Davis H; Hrnciar P; Hirst GC; Li B; Morytko M; Mullen K; Yang B
    Bioorg Med Chem Lett; 2007 Mar; 17(5):1167-71. PubMed ID: 17234410
    [TBL] [Abstract][Full Text] [Related]  

  • 11. Discovery and initial SAR of 2-amino-5-carboxamidothiazoles as inhibitors of the Src-family kinase p56(Lck).
    Wityak J; Das J; Moquin RV; Shen Z; Lin J; Chen P; Doweyko AM; Pitt S; Pang S; Shen DR; Fang Q; de Fex HF; Schieven GL; Kanner SB; Barrish JC
    Bioorg Med Chem Lett; 2003 Nov; 13(22):4007-10. PubMed ID: 14592495
    [TBL] [Abstract][Full Text] [Related]  

  • 12. Structural basis of Src tyrosine kinase inhibition with a new class of potent and selective trisubstituted purine-based compounds.
    Dalgarno D; Stehle T; Narula S; Schelling P; van Schravendijk MR; Adams S; Andrade L; Keats J; Ram M; Jin L; Grossman T; MacNeil I; Metcalf C; Shakespeare W; Wang Y; Keenan T; Sundaramoorthi R; Bohacek R; Weigele M; Sawyer T
    Chem Biol Drug Des; 2006 Jan; 67(1):46-57. PubMed ID: 16492148
    [TBL] [Abstract][Full Text] [Related]  

  • 13. Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection.
    Burchat A; Borhani DW; Calderwood DJ; Hirst GC; Li B; Stachlewitz RF
    Bioorg Med Chem Lett; 2006 Jan; 16(1):118-22. PubMed ID: 16216497
    [TBL] [Abstract][Full Text] [Related]  

  • 14. Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.
    Goldberg DR; Butz T; Cardozo MG; Eckner RJ; Hammach A; Huang J; Jakes S; Kapadia S; Kashem M; Lukas S; Morwick TM; Panzenbeck M; Patel U; Pav S; Peet GW; Peterson JD; Prokopowicz AS; Snow RJ; Sellati R; Takahashi H; Tan J; Tschantz MA; Wang XJ; Wang Y; Wolak J; Xiong P; Moss N
    J Med Chem; 2003 Apr; 46(8):1337-49. PubMed ID: 12672234
    [TBL] [Abstract][Full Text] [Related]  

  • 15. Discovery of pyrimidine benzimidazoles as Src-family selective Lck inhibitors. Part II.
    Zhang G; Ren P; Gray NS; Sim T; Wang X; Liu Y; Che J; Dong W; Tian SS; Sandberg ML; Spalding TA; Romeo R; Iskandar M; Wang Z; Seidel HM; Karanewsky DS; He Y
    Bioorg Med Chem Lett; 2009 Dec; 19(23):6691-5. PubMed ID: 19854052
    [TBL] [Abstract][Full Text] [Related]  

  • 16. Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.
    Lombardo LJ; Lee FY; Chen P; Norris D; Barrish JC; Behnia K; Castaneda S; Cornelius LA; Das J; Doweyko AM; Fairchild C; Hunt JT; Inigo I; Johnston K; Kamath A; Kan D; Klei H; Marathe P; Pang S; Peterson R; Pitt S; Schieven GL; Schmidt RJ; Tokarski J; Wen ML; Wityak J; Borzilleri RM
    J Med Chem; 2004 Dec; 47(27):6658-61. PubMed ID: 15615512
    [TBL] [Abstract][Full Text] [Related]  

  • 17. Discovery and initial SAR of imidazoquinoxalines as inhibitors of the Src-family kinase p56(Lck).
    Chen P; Norris D; Iwanowicz EJ; Spergel SH; Lin J; Gu HH; Shen Z; Wityak J; Lin TA; Pang S; De Fex HF; Pitt S; Shen DR; Doweyko AM; Bassolino DA; Roberge JY; Poss MA; Chen BC; Schieven GL; Barrish JC
    Bioorg Med Chem Lett; 2002 May; 12(10):1361-4. PubMed ID: 11992777
    [TBL] [Abstract][Full Text] [Related]  

  • 18. The development of 2-benzimidazole substituted pyrimidine based inhibitors of lymphocyte specific kinase (Lck).
    Sabat M; VanRens JC; Laufersweiler MJ; Brugel TA; Maier J; Golebiowski A; De B; Easwaran V; Hsieh LC; Walter RL; Mekel MJ; Evdokimov A; Janusz MJ
    Bioorg Med Chem Lett; 2006 Dec; 16(23):5973-7. PubMed ID: 16997556
    [TBL] [Abstract][Full Text] [Related]  

  • 19. Discovery of 2-amino-heteroaryl-benzothiazole-6-anilides as potent p56(lck) inhibitors.
    Das J; Moquin RV; Lin J; Liu C; Doweyko AM; DeFex HF; Fang Q; Pang S; Pitt S; Shen DR; Schieven GL; Barrish JC; Wityak J
    Bioorg Med Chem Lett; 2003 Aug; 13(15):2587-90. PubMed ID: 12852972
    [TBL] [Abstract][Full Text] [Related]  

  • 20. Discovery of pyrimidine benzimidazoles as Lck inhibitors: part I.
    Zhang G; Ren P; Gray NS; Sim T; Liu Y; Wang X; Che J; Tian SS; Sandberg ML; Spalding TA; Romeo R; Iskandar M; Chow D; Martin Seidel H; Karanewsky DS; He Y
    Bioorg Med Chem Lett; 2008 Oct; 18(20):5618-21. PubMed ID: 18793846
    [TBL] [Abstract][Full Text] [Related]  

    [Next]    [New Search]
    of 13.