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Page 1
Discovery and Preclinical Pharmacology of an Oral Bromodomain and Extra-Terminal (BET) Inhibitor Using Scaffold-Hopping and Structure-Guided Drug Design.
Gavai AV, Norris D, Delucca G, Tortolani D, Tokarski JS, Dodd D, O'Malley D, Zhao Y, Quesnelle C, Gill P, Vaccaro W, Huynh T, Ahuja V, Han WC, Mussari C, Harikrishnan L, Kamau M, Poss M, Sheriff S, Yan C, Marsilio F, Menard K, Wen ML, Rampulla R, Wu DR, Li J, Zhang H, Li P, Sun D, Yip H, Traeger SC, Zhang Y, Mathur A, Zhang H, Huang C, Yang Z, Ranasinghe A, Everlof G, Raghavan N, Tye CK, Wee S, Hunt JT, Vite G, Westhouse R, Lee FY. Gavai AV, et al. Among authors: poss m. J Med Chem. 2021 Oct 14;64(19):14247-14265. doi: 10.1021/acs.jmedchem.1c00625. Epub 2021 Sep 20. J Med Chem. 2021. PMID: 34543572
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. Chen P, et al. Among authors: poss ma. Bioorg Med Chem Lett. 2002 May 20;12(10):1361-4. doi: 10.1016/s0960-894x(02)00191-9. Bioorg Med Chem Lett. 2002. PMID: 11992777
Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: synthesis, X-ray crystallographic analysis, and biological activities.
Kim KS, Kimball SD, Misra RN, Rawlins DB, Hunt JT, Xiao HY, Lu S, Qian L, Han WC, Shan W, Mitt T, Cai ZW, Poss MA, Zhu H, Sack JS, Tokarski JS, Chang CY, Pavletich N, Kamath A, Humphreys WG, Marathe P, Bursuker I, Kellar KA, Roongta U, Batorsky R, Mulheron JG, Bol D, Fairchild CR, Lee FY, Webster KR. Kim KS, et al. J Med Chem. 2002 Aug 29;45(18):3905-27. doi: 10.1021/jm0201520. J Med Chem. 2002. PMID: 12190313
Identification of purine inhibitors of phosphodiesterase 7 (PDE7).
Pitts WJ, Vaccaro W, Huynh T, Leftheris K, Roberge JY, Barbosa J, Guo J, Brown B, Watson A, Donaldson K, Starling GC, Kiener PA, Poss MA, Dodd JH, Barrish JC. Pitts WJ, et al. Bioorg Med Chem Lett. 2004 Jun 7;14(11):2955-8. doi: 10.1016/j.bmcl.2004.03.021. Bioorg Med Chem Lett. 2004. PMID: 15125967
Aminotriazine 5-HT7 antagonists.
Mattson RJ, Denhart DJ, Catt JD, Dee MF, Deskus JA, Ditta JL, Epperson J, Dalton King H, Gao A, Poss MA, Purandare A, Tortolani D, Zhao Y, Yang H, Yeola S, Palmer J, Torrente J, Stark A, Johnson G. Mattson RJ, et al. Bioorg Med Chem Lett. 2004 Aug 16;14(16):4245-8. doi: 10.1016/j.bmcl.2004.06.008. Bioorg Med Chem Lett. 2004. PMID: 15261279
Addition of benzylic and allylic organozinc and Grignard reagents to resin-bound imines to provide alpha-branched secondary amines bearing a wide variety of functional groups. Utility in the synthesis of beta-3 adrenergic receptor agonists.
Wu G, Cai ZW, Bednarz MS, Kocy OR, Gavai AV, Godfrey JD Jr, Washburn WN, Poss MA, Sher PM. Wu G, et al. Among authors: poss ma. J Comb Chem. 2005 Jan-Feb;7(1):99-108. doi: 10.1021/cc0498682. J Comb Chem. 2005. PMID: 15638488
Identification of chemokine receptor CCR4 antagonist.
Purandare AV, Gao A, Wan H, Somerville J, Burke C, Seachord C, Vaccaro W, Wityak J, Poss MA. Purandare AV, et al. Bioorg Med Chem Lett. 2005 May 16;15(10):2669-72. doi: 10.1016/j.bmcl.2005.02.084. Bioorg Med Chem Lett. 2005. PMID: 15863339
Solid-phase synthesis of 5-substituted amino pyrazoles.
Dodd DS, Martinez RL, Kamau M, Ruan Z, Van Kirk K, Cooper CB, Hermsmeier MA, Traeger SC, Poss MA. Dodd DS, et al. Among authors: poss ma. J Comb Chem. 2005 Jul-Aug;7(4):584-8. doi: 10.1021/cc049814s. J Comb Chem. 2005. PMID: 16004502
165 results