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Page 1
Lead Optimization to Advance Protease-Activated Receptor-1 Antagonists in Early Discovery.
Mandal M, Madeira M, Amin RP, Buevich AV, Cheng A, Labroli M, Liu X, Acton J, Pio B, Basso A, Chobanian H, Dong G, Dropinski J, Guo Y, Guo Z, Kurowski S, Korfmacher W, Lee S, Meng D, Ondeyka D, Yang Z, Zhang R, Wei H, Wu Z, Zhang F, Wollenberg G, Biftu T, Greenlee WJ, Chintala M, Maletic M, Zhu Z. Mandal M, et al. Among authors: biftu t. J Med Chem. 2022 Apr 14;65(7):5575-5592. doi: 10.1021/acs.jmedchem.1c02048. Epub 2022 Mar 29. J Med Chem. 2022. PMID: 35349275
Improved Stability of Proline-Derived Direct Thrombin Inhibitors through Hydroxyl to Heterocycle Replacement.
Chobanian HR, Pio B, Guo Y, Shen H, Huffman MA, Madeira M, Salituro G, Terebetski JL, Ormes J, Jochnowitz N, Hoos L, Zhou Y, Lewis D, Hawes B, Mitnaul L, O'Neill K, Ellsworth K, Wang L, Biftu T, Duffy JL. Chobanian HR, et al. Among authors: biftu t. ACS Med Chem Lett. 2015 Mar 13;6(5):553-7. doi: 10.1021/acsmedchemlett.5b00047. eCollection 2015 May 14. ACS Med Chem Lett. 2015. PMID: 26005532 Free PMC article.
Development, synthesis, and biological evaluation of (-)-trans-(2S,5S)-2-[3-[(2-oxopropyl)sulfonyl]-4-n-propoxy-5-(3- hydroxypropoxy)-phenyl]-5-(3,4,5-trimethoxyphenyl)tetrahydrofuran, a potent orally active platelet-activating factor (PAF) antagonist and its water-soluble prodrug phosphate ester.
Girotra NN, Biftu T, Ponpipom MM, Acton JJ, Alberts AW, Bach TN, Ball RG, Bugianesi RL, Parsons WH, Chabala JC, et al. Girotra NN, et al. Among authors: biftu t. J Med Chem. 1992 Sep 18;35(19):3474-82. doi: 10.1021/jm00097a005. J Med Chem. 1992. PMID: 1404229
Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes.
Biftu T, Sinha-Roy R, Chen P, Qian X, Feng D, Kuethe JT, Scapin G, Gao YD, Yan Y, Krueger D, Bak A, Eiermann G, He J, Cox J, Hicks J, Lyons K, He H, Salituro G, Tong S, Patel S, Doss G, Petrov A, Wu J, Xu SS, Sewall C, Zhang X, Zhang B, Thornberry NA, Weber AE. Biftu T, et al. J Med Chem. 2014 Apr 24;57(8):3205-12. doi: 10.1021/jm401992e. Epub 2014 Apr 2. J Med Chem. 2014. PMID: 24660890
Diminishing GSH-Adduct Formation of Tricyclic Diazepine-based Mutant IDH1 Inhibitors.
Huang C, Fischer C, Machacek MR, Bogen S, Biftu T, Huang X, Reutershan MH, Otte R, Hong Q, Wu Z, Yu Y, Park M, Chen L, Biju P, Knemeyer I, Lu P, Kochansky CJ, Hicks MB, Liu Y, Helmy R, Fradera X, Donofrio A, Close J, Maddess ML, White C, Sloman DL, Sciammetta N, Lu J, Gibeau C, Simov V, Zhang H, Fuller P, Witter D. Huang C, et al. Among authors: biftu t. ACS Med Chem Lett. 2022 Mar 28;13(4):734-741. doi: 10.1021/acsmedchemlett.2c00089. eCollection 2022 Apr 14. ACS Med Chem Lett. 2022. PMID: 35450359 Free PMC article.
(+/-)-trans-2-(3-Methoxy-5-methylsulfonyl-4-propoxyphenyl)-5-(3,4,5- trimethoxyphenyl)tetrahydrofuran (L-659,989), a novel, potent PAF receptor antagonist.
Ponpipom MM, Hwang SB, Doebber TW, Acton JJ, Alberts AW, Biftu T, Brooker DR, Bugianesi RL, Chabala JC, Gamble NL, et al. Ponpipom MM, et al. Among authors: biftu t. Biochem Biophys Res Commun. 1988 Feb 15;150(3):1213-20. doi: 10.1016/0006-291x(88)90758-9. Biochem Biophys Res Commun. 1988. PMID: 2829894
Discovery of MK-8722: A Systemic, Direct Pan-Activator of AMP-Activated Protein Kinase.
Feng D, Biftu T, Romero FA, Kekec A, Dropinski J, Kassick A, Xu S, Kurtz MM, Gollapudi A, Shao Q, Yang X, Lu K, Zhou G, Kemp D, Myers RW, Guan HP, Trujillo ME, Li C, Weber A, Sebhat IK. Feng D, et al. Among authors: biftu t. ACS Med Chem Lett. 2017 Dec 1;9(1):39-44. doi: 10.1021/acsmedchemlett.7b00417. eCollection 2018 Jan 11. ACS Med Chem Lett. 2017. PMID: 29348809 Free PMC article.
Novel tetrahydropyran analogs as dipeptidyl peptidase IV inhibitors: Profile of clinical candidate (2R,3S,5R)-2- (2,5-difluorophenyl)-5-(4,6-dihydropyrrolo [3,4-c]pyrazol-5-(1H)-yl)tetrahydro-2H-pyran-3-amine (23) [corrected].
Biftu T, Qian X, Chen P, Feng D, Scapin G, Gao YD, Cox J, Roy RS, Eiermann G, He H, Lyons K, Salituro G, Patel S, Petrov A, Xu F, Xu SS, Zhang B, Caldwell C, Wu JK, Lyons K, Weber AE. Biftu T, et al. Bioorg Med Chem Lett. 2013 Oct 1;23(19):5361-6. doi: 10.1016/j.bmcl.2013.07.061. Epub 2013 Aug 5. Bioorg Med Chem Lett. 2013. PMID: 23972441
40 results