Year |
Citation |
Score |
2016 |
Jia Y, Yun CH, Park E, Ercan D, Manuia M, Juarez J, Xu C, Rhee K, Chen T, Zhang H, Palakurthi S, Jang J, Lelais G, DiDonato M, Bursulaya B, ... ... Marsilje TH, et al. Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors. Nature. 534: 129-32. PMID 27251290 DOI: 10.1038/Nature17960 |
0.464 |
|
2016 |
Fairhurst RA, Marsilje TH, Stutz S, Boos A, Niklaus M, Chen B, Jiang S, Lu W, Furet P, McCarthy C, Stauffer F, Guagnano V, Vaupel A, Michellys PY, Schnell C, et al. Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors. Bioorganic & Medicinal Chemistry Letters. PMID 26951753 DOI: 10.1016/j.bmcl.2016.02.075 |
0.354 |
|
2016 |
Jia Y, Juarez J, Li J, Manuia M, Niederst MJ, Tompkins C, Timple N, Vaillancourt MT, Culazzo Pferdekamper A, Lockerman EL, Li C, Anderson J, Costa C, Liao D, Murphy E, ... ... Marsilje TH, et al. EGF816 exerts anticancer effects in non-small cell lung cancer by irreversibly and selectively targeting primary and acquired activating mutations in the EGF receptor. Cancer Research. PMID 26825170 DOI: 10.1158/0008-5472.Can-15-2581 |
0.307 |
|
2015 |
Michellys PY, Chen B, Jiang T, Jin Y, Lu W, Marsilje TH, Pei W, Uno T, Zhu X, Wu B, Nguyen TN, Bursulaya B, Lee C, Li N, Kim S, et al. Design and synthesis of novel selective anaplastic lymphoma kinase inhibitors. Bioorganic & Medicinal Chemistry Letters. PMID 26750252 DOI: 10.1016/j.bmcl.2015.11.049 |
0.509 |
|
2013 |
Marsilje TH, Pei W, Chen B, Lu W, Uno T, Jin Y, Jiang T, Kim S, Li N, Warmuth M, Sarkisova Y, Sun F, Steffy A, Pferdekamper AC, Li AG, et al. Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials. Journal of Medicinal Chemistry. 56: 5675-90. PMID 23742252 DOI: 10.1021/Jm400402Q |
0.398 |
|
2003 |
Marsilje TH, Hedrick MP, Desharnais J, Capps K, Tavassoli A, Zhang Y, Wilson IA, Benkovic SJ, Boger DL. 10-(2-benzoxazolcarbonyl)-5,10-dideaza-acyclic-5,6,7,8-tetrahydrofolic acid: a potential inhibitor of GAR transformylase and AICAR transformylase. Bioorganic & Medicinal Chemistry. 11: 4503-9. PMID 13129586 DOI: 10.1016/S0968-0896(03)00457-7 |
0.404 |
|
2003 |
Marsilje TH, Hedrick MP, Desharnais J, Tavassoli A, Zhang Y, Wilson IA, Benkovic SJ, Boger DL. Design, synthesis, and biological evaluation of simplified alpha-keto heterocycle, trifluoromethyl ketone, and formyl substituted folate analogues as potential inhibitors of GAR transformylase and AICAR transformylase. Bioorganic & Medicinal Chemistry. 11: 4487-501. PMID 13129585 DOI: 10.1016/S0968-0896(03)00456-5 |
0.304 |
|
2003 |
Zhang Y, Desharnais J, Marsilje TH, Li C, Hedrick MP, Gooljarsingh LT, Tavassoli A, Benkovic SJ, Olson AJ, Boger DL, Wilson IA. Rational design, synthesis, evaluation, and crystal structure of a potent inhibitor of human GAR Tfase: 10-(trifluoroacetyl)-5,10-dideazaacyclic-5,6,7,8-tetrahydrofolic acid. Biochemistry. 42: 6043-56. PMID 12755606 DOI: 10.1021/Bi034219C |
0.411 |
|
2001 |
Greasley SE, Marsilje TH, Cai H, Baker S, Benkovic SJ, Boger DL, Wilson IA. Unexpected formation of an epoxide-derived multisubstrate adduct inhibitor on the active site of GAR transformylase Biochemistry. 40: 13538-13547. PMID 11695901 DOI: 10.1021/Bi011482+ |
0.343 |
|
2000 |
Boger DL, Marsilje TH, Castro RA, Hedrick MP, Jin Q, Baker SJ, Shim JH, Benkovic SJ. Design, synthesis, and biological evaluation of fluoronitrophenyl substituted folate analogues as potential inhibitors of GAR transformylase and AICAR transformylase Bioorganic and Medicinal Chemistry Letters. 10: 1471-1475. PMID 10888335 DOI: 10.1016/S0960-894X(00)00271-7 |
0.435 |
|
2000 |
Boger DL, Labroli MA, Marsilje TH, Jin Q, Hedrick MP, Baker SJ, Shim JH, Benkovic SJ. Conformationally restricted analogues designed for selective inhibition of GAR Tfase versus thymidylate synthase or dihydrofolate reductase Bioorganic and Medicinal Chemistry. 8: 1075-1086. PMID 10882019 DOI: 10.1016/S0968-0896(00)00051-1 |
0.475 |
|
2000 |
Milkiewicz KL, Marsilje TH, Woodworth RP, Bifulco N, Hangauer MJ, Hangauer DG. The design, synthesis and activity of non-ATP competitive inhibitors of pp60(c-src) tyrosine kinase. Part 2: hydroxyindole derivatives. Bioorganic & Medicinal Chemistry Letters. 10: 483-6. PMID 10743953 DOI: 10.1016/S0960-894X(00)00040-8 |
0.555 |
|
2000 |
Marsilje TH, Milkiewicz KL, Hangauer DG. The design, synthesis and activity of non-ATP competitive inhibitors of pp60(c-src) tyrosine kinase. Part 1: hydroxynaphthalene derivatives. Bioorganic & Medicinal Chemistry Letters. 10: 477-81. PMID 10743952 DOI: 10.1016/S0960-894X(00)00039-1 |
0.536 |
|
1998 |
Lai JH, Marsilje TH, Choi S, Nair SA, Hangauer DG. The design, synthesis and activity of pentapeptide pp60c-src inhibitors containing L-phosphotyrosine mimics. The Journal of Peptide Research : Official Journal of the American Peptide Society. 51: 271-81. PMID 9560002 DOI: 10.1111/J.1399-3011.1998.Tb00424.X |
0.619 |
|
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