Year |
Citation |
Score |
2022 |
Eno MS, Brubaker JD, Campbell JE, De Savi C, Guzi TJ, Williams BD, Wilson D, Wilson K, Brooijmans N, Kim J, Özen A, Perola E, Hsieh J, Brown V, Fetalvero K, ... ... Dineen TA, et al. Discovery of BLU-945, a Reversible, Potent, and Wild-Type-Sparing Next-Generation EGFR Mutant Inhibitor for Treatment-Resistant Non-Small-Cell Lung Cancer. Journal of Medicinal Chemistry. PMID 35838760 DOI: 10.1021/acs.jmedchem.2c00704 |
0.578 |
|
2017 |
Graceffa RF, Boezio AA, Able J, Altmann S, Berry LM, Boezio CM, Butler JR, Chu-Moyer MY, Cooke M, DiMauro EF, Dineen TA, Feric Bojic E, Foti RS, Fremeau RT, Guzman-Perez A, et al. Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency, Pharmacokinetics, and Metabolic Properties to Obtain Atropisomeric Quinolinone (AM-0466) that Affords Robust In Vivo Activity. Journal of Medicinal Chemistry. PMID 28324649 DOI: 10.1021/Acs.Jmedchem.6B01850 |
0.368 |
|
2017 |
Weiss MM, Dineen TA, Marx IE, Altmann S, Boezio AA, Bregman H, Chu-Moyer MY, DiMauro EF, Feric Bojic E, Foti RS, Gao H, Graceffa RF, Gunaydin H, Guzman-Perez A, Huang H, et al. Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics While Mitigating Metabolic Liabilities. Journal of Medicinal Chemistry. PMID 28287723 DOI: 10.1021/Acs.Jmedchem.6B01851 |
0.334 |
|
2016 |
Marx IE, Dineen TA, Able J, Bode C, Bregman H, Chu-Moyer M, DiMauro EF, Du B, Foti RS, Fremeau RT, Gao H, Gunaydin H, Hall BE, Huang L, Kornecook T, et al. Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics to Enable in Vivo Target Engagement. Acs Medicinal Chemistry Letters. 7: 1062-1067. PMID 27994738 DOI: 10.1021/Acsmedchemlett.6B00243 |
0.307 |
|
2015 |
Chen JJ, Liu Q, Yuan C, Gore V, Lopez P, Ma V, Amegadzie A, Qian W, Judd TC, Minatti AE, Brown J, Cheng Y, Xue M, Zhong W, Dineen TA, et al. Development of 2-aminooxazoline 3-azaxanthenes as orally efficacious β-secretase inhibitors for the potential treatment of Alzheimer's disease. Bioorganic & Medicinal Chemistry Letters. 25: 767-74. PMID 25613679 DOI: 10.1016/J.Bmcl.2014.12.092 |
0.314 |
|
2014 |
Epstein O, Bryan MC, Cheng AC, Derakhchan K, Dineen TA, Hickman D, Hua Z, Human JB, Kreiman C, Marx IE, Weiss MM, Wahl RC, Wen PH, Whittington DA, Wood S, et al. Lead optimization and modulation of hERG activity in a series of aminooxazoline xanthene β-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors. Journal of Medicinal Chemistry. 57: 9796-810. PMID 25389560 DOI: 10.1021/Jm501266W |
0.353 |
|
2014 |
Dineen TA, Chen K, Cheng AC, Derakhchan K, Epstein O, Esmay J, Hickman D, Kreiman CE, Marx IE, Wahl RC, Wen PH, Weiss MM, Whittington DA, Wood S, Fremeau RT, et al. Inhibitors of β-site amyloid precursor protein cleaving enzyme (BACE1): identification of (S)-7-(2-fluoropyridin-3-yl)-3-((3-methyloxetan-3-yl)ethynyl)-5'H-spiro[chromeno[2,3-b]pyridine-5,4'-oxazol]-2'-amine (AMG-8718). Journal of Medicinal Chemistry. 57: 9811-31. PMID 25363711 DOI: 10.1021/Jm5012676 |
0.331 |
|
2012 |
Huang H, La DS, Cheng AC, Whittington DA, Patel VF, Chen K, Dineen TA, Epstein O, Graceffa R, Hickman D, Kiang YH, Louie S, Luo Y, Wahl RC, Wen PH, et al. Structure- and property-based design of aminooxazoline xanthenes as selective, orally efficacious, and CNS penetrable BACE inhibitors for the treatment of Alzheimer's disease. Journal of Medicinal Chemistry. 55: 9156-69. PMID 22928914 DOI: 10.1021/Jm300598E |
0.357 |
|
2012 |
Wood S, Wen PH, Zhang J, Zhu L, Luo Y, Babu-Khan S, Chen K, Pham R, Esmay J, Dineen TA, Kaller MR, Weiss MM, Hitchcock SA, Citron M, Zhong W, et al. Establishing the relationship between in vitro potency, pharmacokinetic, and pharmacodynamic parameters in a series of orally available, hydroxyethylamine-derived β-secretase inhibitors. The Journal of Pharmacology and Experimental Therapeutics. 343: 460-7. PMID 22911925 DOI: 10.1124/Jpet.112.197954 |
0.337 |
|
2012 |
Dineen TA, Weiss MM, Williamson T, Acton P, Babu-Khan S, Bartberger MD, Brown J, Chen K, Cheng Y, Citron M, Croghan MD, Dunn RT, Esmay J, Graceffa RF, Harried SS, et al. Design and synthesis of potent, orally efficacious hydroxyethylamine derived β-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors. Journal of Medicinal Chemistry. 55: 9025-44. PMID 22468684 DOI: 10.1021/Jm300118S |
0.346 |
|
2012 |
Weiss MM, Williamson T, Babu-Khan S, Bartberger MD, Brown J, Chen K, Cheng Y, Citron M, Croghan MD, Dineen TA, Esmay J, Graceffa RF, Harried SS, Hickman D, Hitchcock SA, et al. Design and preparation of a potent series of hydroxyethylamine containing β-secretase inhibitors that demonstrate robust reduction of central β-amyloid. Journal of Medicinal Chemistry. 55: 9009-24. PMID 22468639 DOI: 10.1021/Jm300119P |
0.318 |
|
2009 |
Michaelis DJ, Dineen TA. Ring opening of aziridines with ortho-bromophenyl metal reagents: synthesis of 2-substituted indolines Tetrahedron Letters. 50: 1920-1923. DOI: 10.1016/J.Tetlet.2009.02.047 |
0.344 |
|
2006 |
Dineen TA, Zajac MA, Myers AG. Efficient transamidation of primary carboxamides by in situ activation with N,N-dialkylformamide dimethyl acetals. Journal of the American Chemical Society. 128: 16406-9. PMID 17165798 DOI: 10.1021/Ja066728I |
0.594 |
|
2005 |
Dineen TA, Roush WR. Stereoselective synthesis of the octahydronaphthalene unit of integramycin via an intramolecular Diels-Alder reaction. Organic Letters. 7: 1355-8. PMID 15787505 DOI: 10.1021/Ol050191G |
0.364 |
|
2004 |
Dineen TA, Roush WR. Total synthesis of cochleamycin A. Organic Letters. 6: 2043-6. PMID 15176814 DOI: 10.1021/Ol049331X |
0.43 |
|
2003 |
Dineen TA, Roush WR. Probing the Lewis acid-catalyzed intramolecular Diels-Alder cyclizations of allylic alkoxy-substituted (Z)-1,3-dienes. Organic Letters. 5: 4725-8. PMID 14627425 DOI: 10.1021/Ol035900+ |
0.424 |
|
2003 |
Boitano A, Emal CD, Leonetti F, Blatt NB, Dineen TA, Ellman JA, Roush WR, Opipari AW, Glick GD. Structure activity studies of a novel cytotoxic benzodiazepine. Bioorganic & Medicinal Chemistry Letters. 13: 3327-30. PMID 12951119 DOI: 10.1016/S0960-894X(03)00683-8 |
0.551 |
|
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