BIOMARKERS

Molecular Biopsy of Human Tumors

- a resource for Precision Medicine *

237 related articles for article (PubMed ID: 22342124)

  • 21. Optimization of a dihydropyrrolopyrazole series of transforming growth factor-beta type I receptor kinase domain inhibitors: discovery of an orally bioavailable transforming growth factor-beta receptor type I inhibitor as antitumor agent.
    Li HY; McMillen WT; Heap CR; McCann DJ; Yan L; Campbell RM; Mundla SR; King CH; Dierks EA; Anderson BD; Britt KS; Huss KL; Voss MD; Wang Y; Clawson DK; Yingling JM; Sawyer JS
    J Med Chem; 2008 Apr; 51(7):2302-6. PubMed ID: 18314943
    [TBL] [Abstract][Full Text] [Related]  

  • 22. Discovery of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as highly potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 6-aryl substituent.
    Verheijen JC; Richard DJ; Curran K; Kaplan J; Lefever M; Nowak P; Malwitz DJ; Brooijmans N; Toral-Barza L; Zhang WG; Lucas J; Hollander I; Ayral-Kaloustian S; Mansour TS; Yu K; Zask A
    J Med Chem; 2009 Dec; 52(24):8010-24. PubMed ID: 19894727
    [TBL] [Abstract][Full Text] [Related]  

  • 23. Discovery of potent and selective inhibitors of the mammalian target of rapamycin (mTOR) kinase.
    Nowak P; Cole DC; Brooijmans N; Bursavich MG; Curran KJ; Ellingboe JW; Gibbons JJ; Hollander I; Hu Y; Kaplan J; Malwitz DJ; Toral-Barza L; Verheijen JC; Zask A; Zhang WG; Yu K
    J Med Chem; 2009 Nov; 52(22):7081-9. PubMed ID: 19848404
    [TBL] [Abstract][Full Text] [Related]  

  • 24. Design, synthesis, and biological evaluation of pyrazolopyrimidine-sulfonamides as potent multiple-mitotic kinase (MMK) inhibitors (part I).
    Zhang L; Fan J; Chong JH; Cesena A; Tam BY; Gilson C; Boykin C; Wang D; Aivazian D; Marcotte D; Xiao G; Le Brazidec JY; Piao J; Lundgren K; Hong K; Vu K; Nguyen K; Gan LS; Silvian L; Ling L; Teng M; Reff M; Takeda N; Timple N; Wang Q; Morena R; Khan S; Zhao S; Li T; Lee WC; Taveras AG; Chao J
    Bioorg Med Chem Lett; 2011 Sep; 21(18):5633-7. PubMed ID: 21798738
    [TBL] [Abstract][Full Text] [Related]  

  • 25. Hybrid inhibitors of phosphatidylinositol 3-kinase (PI3K) and the mammalian target of rapamycin (mTOR): design, synthesis, and superior antitumor activity of novel wortmannin-rapamycin conjugates.
    Ayral-Kaloustian S; Gu J; Lucas J; Cinque M; Gaydos C; Zask A; Chaudhary I; Wang J; Di L; Young M; Ruppen M; Mansour TS; Gibbons JJ; Yu K
    J Med Chem; 2010 Jan; 53(1):452-9. PubMed ID: 19928864
    [TBL] [Abstract][Full Text] [Related]  

  • 26. Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors for the treatment of cancer.
    Sutherlin DP; Sampath D; Berry M; Castanedo G; Chang Z; Chuckowree I; Dotson J; Folkes A; Friedman L; Goldsmith R; Heffron T; Lee L; Lesnick J; Lewis C; Mathieu S; Nonomiya J; Olivero A; Pang J; Prior WW; Salphati L; Sideris S; Tian Q; Tsui V; Wan NC; Wang S; Wiesmann C; Wong S; Zhu BY
    J Med Chem; 2010 Feb; 53(3):1086-97. PubMed ID: 20050669
    [TBL] [Abstract][Full Text] [Related]  

  • 27. Discovery of pyrrolopyrimidine inhibitors of Akt.
    Blake JF; Kallan NC; Xiao D; Xu R; Bencsik JR; Skelton NJ; Spencer KL; Mitchell IS; Woessner RD; Gloor SL; Risom T; Gross SD; Martinson M; Morales TH; Vigers GP; Brandhuber BJ
    Bioorg Med Chem Lett; 2010 Oct; 20(19):5607-12. PubMed ID: 20810279
    [TBL] [Abstract][Full Text] [Related]  

  • 28. Phthalazinone pyrazoles as potent, selective, and orally bioavailable inhibitors of Aurora-A kinase.
    Prime ME; Courtney SM; Brookfield FA; Marston RW; Walker V; Warne J; Boyd AE; Kairies NA; von der Saal W; Limberg A; Georges G; Engh RA; Goller B; Rueger P; Rueth M
    J Med Chem; 2011 Jan; 54(1):312-9. PubMed ID: 21128645
    [TBL] [Abstract][Full Text] [Related]  

  • 29. Discovery of 4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide (AZD5363), an orally bioavailable, potent inhibitor of Akt kinases.
    Addie M; Ballard P; Buttar D; Crafter C; Currie G; Davies BR; Debreczeni J; Dry H; Dudley P; Greenwood R; Johnson PD; Kettle JG; Lane C; Lamont G; Leach A; Luke RW; Morris J; Ogilvie D; Page K; Pass M; Pearson S; Ruston L
    J Med Chem; 2013 Mar; 56(5):2059-73. PubMed ID: 23394218
    [TBL] [Abstract][Full Text] [Related]  

  • 30. Identification of aminopyrazolopyridine ureas as potent VEGFR/PDGFR multitargeted kinase inhibitors.
    Dai Y; Hartandi K; Soni NB; Pease LJ; Reuter DR; Olson AM; Osterling DJ; Doktor SZ; Albert DH; Bouska JJ; Glaser KB; Marcotte PA; Stewart KD; Davidsen SK; Michaelides MR
    Bioorg Med Chem Lett; 2008 Jan; 18(1):386-90. PubMed ID: 18023347
    [TBL] [Abstract][Full Text] [Related]  

  • 31. AT7867 is a potent and oral inhibitor of AKT and p70 S6 kinase that induces pharmacodynamic changes and inhibits human tumor xenograft growth.
    Grimshaw KM; Hunter LJ; Yap TA; Heaton SP; Walton MI; Woodhead SJ; Fazal L; Reule M; Davies TG; Seavers LC; Lock V; Lyons JF; Thompson NT; Workman P; Garrett MD
    Mol Cancer Ther; 2010 May; 9(5):1100-10. PubMed ID: 20423992
    [TBL] [Abstract][Full Text] [Related]  

  • 32. Identification of N,1,4,4-tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a potent, orally available cyclin dependent kinase inhibitor.
    Brasca MG; Amboldi N; Ballinari D; Cameron A; Casale E; Cervi G; Colombo M; Colotta F; Croci V; D'Alessio R; Fiorentini F; Isacchi A; Mercurio C; Moretti W; Panzeri A; Pastori W; Pevarello P; Quartieri F; Roletto F; Traquandi G; Vianello P; Vulpetti A; Ciomei M
    J Med Chem; 2009 Aug; 52(16):5152-63. PubMed ID: 19603809
    [TBL] [Abstract][Full Text] [Related]  

  • 33. 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]  

  • 34. Design and synthesis of orally bioavailable benzimidazoles as Raf kinase inhibitors.
    Ramurthy S; Subramanian S; Aikawa M; Amiri P; Costales A; Dove J; Fong S; Jansen JM; Levine B; Ma S; McBride CM; Michaelian J; Pick T; Poon DJ; Girish S; Shafer CM; Stuart D; Sung L; Renhowe PA
    J Med Chem; 2008 Nov; 51(22):7049-52. PubMed ID: 18942827
    [TBL] [Abstract][Full Text] [Related]  

  • 35. 2-Hydroxypropyl-β-cyclodextrin strongly improves water solubility and anti-proliferative activity of pyrazolo[3,4-d]pyrimidines Src-Abl dual inhibitors.
    Dreassi E; Zizzari AT; Mori M; Filippi I; Belfiore A; Naldini A; Carraro F; Santucci A; Schenone S; Botta M
    Eur J Med Chem; 2010 Dec; 45(12):5958-64. PubMed ID: 20970221
    [TBL] [Abstract][Full Text] [Related]  

  • 36. 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]  

  • 37. The discovery and optimization of a novel class of potent, selective, and orally bioavailable anaplastic lymphoma kinase (ALK) inhibitors with potential utility for the treatment of cancer.
    Lewis RT; Bode CM; Choquette DM; Potashman M; Romero K; Stellwagen JC; Teffera Y; Moore E; Whittington DA; Chen H; Epstein LF; Emkey R; Andrews PS; Yu VL; Saffran DC; Xu M; Drew A; Merkel P; Szilvassy S; Brake RL
    J Med Chem; 2012 Jul; 55(14):6523-40. PubMed ID: 22734674
    [TBL] [Abstract][Full Text] [Related]  

  • 38. 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]  

  • 39. Discovery and optimization of a series of 3-(3-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amines: orally bioavailable, selective, and potent ATP-independent Akt inhibitors.
    Ashwell MA; Lapierre JM; Brassard C; Bresciano K; Bull C; Cornell-Kennon S; Eathiraj S; France DS; Hall T; Hill J; Kelleher E; Khanapurkar S; Kizer D; Koerner S; Link J; Liu Y; Makhija S; Moussa M; Namdev N; Nguyen K; Nicewonger R; Palma R; Szwaya J; Tandon M; Uppalapati U; Vensel D; Volak LP; Volckova E; Westlund N; Wu H; Yang RY; Chan TC
    J Med Chem; 2012 Jun; 55(11):5291-310. PubMed ID: 22533986
    [TBL] [Abstract][Full Text] [Related]  

  • 40. Design and synthesis of novel 3-sulfonylpyrazol-4-amino pyrimidines as potent anaplastic lymphoma kinase (ALK) inhibitors.
    Zhang P; Dong J; Zhong B; Zhang D; Yuan H; Jin C; Xu X; Li H; Zhou Y; Liang Z; Ji M; Xu T; Song G; Zhang L; Chen G; Meng X; Sun D; Shih J; Zhang R; Hou G; Wang C; Jin Y; Yang Q
    Bioorg Med Chem Lett; 2016 Apr; 26(8):1910-8. PubMed ID: 26979157
    [TBL] [Abstract][Full Text] [Related]  

    [Previous]   [Next]    [New Search]
    of 12.