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172 results

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Page 1
New IDH1 mutant inhibitors for treatment of acute myeloid leukemia.
Okoye-Okafor UC, Bartholdy B, Cartier J, Gao EN, Pietrak B, Rendina AR, Rominger C, Quinn C, Smallwood A, Wiggall KJ, Reif AJ, Schmidt SJ, Qi H, Zhao H, Joberty G, Faelth-Savitski M, Bantscheff M, Drewes G, Duraiswami C, Brady P, Groy A, Narayanagari SR, Antony-Debre I, Mitchell K, Wang HR, Kao YR, Christopeit M, Carvajal L, Barreyro L, Paietta E, Makishima H, Will B, Concha N, Adams ND, Schwartz B, McCabe MT, Maciejewski J, Verma A, Steidl U. Okoye-Okafor UC, et al. Among authors: smallwood a. Nat Chem Biol. 2015 Nov;11(11):878-86. doi: 10.1038/nchembio.1930. Epub 2015 Oct 5. Nat Chem Biol. 2015. PMID: 26436839 Free PMC article.
Discovery of a Novel 2,6-Disubstituted Glucosamine Series of Potent and Selective Hexokinase 2 Inhibitors.
Lin H, Zeng J, Xie R, Schulz MJ, Tedesco R, Qu J, Erhard KF, Mack JF, Raha K, Rendina AR, Szewczuk LM, Kratz PM, Jurewicz AJ, Cecconie T, Martens S, McDevitt PJ, Martin JD, Chen SB, Jiang Y, Nickels L, Schwartz BJ, Smallwood A, Zhao B, Campobasso N, Qian Y, Briand J, Rominger CM, Oleykowski C, Hardwicke MA, Luengo JI. Lin H, et al. Among authors: smallwood a. ACS Med Chem Lett. 2015 Dec 28;7(3):217-22. doi: 10.1021/acsmedchemlett.5b00214. eCollection 2016 Mar 10. ACS Med Chem Lett. 2015. PMID: 26985301 Free PMC article.
Long-Range Inhibitor-Induced Conformational Regulation of Human IRE1α Endoribonuclease Activity.
Concha NO, Smallwood A, Bonnette W, Totoritis R, Zhang G, Federowicz K, Yang J, Qi H, Chen S, Campobasso N, Choudhry AE, Shuster LE, Evans KA, Ralph J, Sweitzer S, Heerding DA, Buser CA, Su DS, DeYoung MP. Concha NO, et al. Among authors: smallwood a. Mol Pharmacol. 2015 Dec;88(6):1011-23. doi: 10.1124/mol.115.100917. Epub 2015 Oct 5. Mol Pharmacol. 2015. PMID: 26438213
Discovery of renin inhibitors containing a simple aspartate binding moiety that imparts reduced P450 inhibition.
Lawhorn BG, Tran T, Hong VS, Morgan LA, Le BT, Harpel MR, Jolivette L, Diaz E, Schwartz B, Gross JW, Tomaszek T, Semus S, Concha N, Smallwood A, Holt DA, Kallander LS. Lawhorn BG, et al. Among authors: smallwood a. Bioorg Med Chem Lett. 2017 Nov 1;27(21):4838-4843. doi: 10.1016/j.bmcl.2017.09.046. Epub 2017 Sep 23. Bioorg Med Chem Lett. 2017. PMID: 28985999
Kinetic mechanism and rate-limiting steps of focal adhesion kinase-1.
Schneck JL, Briand J, Chen S, Lehr R, McDevitt P, Zhao B, Smallwood A, Concha N, Oza K, Kirkpatrick R, Yan K, Villa JP, Meek TD, Thrall SH. Schneck JL, et al. Among authors: smallwood a. Biochemistry. 2010 Aug 24;49(33):7151-63. doi: 10.1021/bi100824v. Biochemistry. 2010. PMID: 20597513
Synthesis and SAR of potent LXR agonists containing an indole pharmacophore.
Washburn DG, Hoang TH, Campobasso N, Smallwood A, Parks DJ, Webb CL, Frank KA, Nord M, Duraiswami C, Evans C, Jaye M, Thompson SK. Washburn DG, et al. Among authors: smallwood a. Bioorg Med Chem Lett. 2009 Feb 15;19(4):1097-100. doi: 10.1016/j.bmcl.2009.01.004. Epub 2009 Jan 9. Bioorg Med Chem Lett. 2009. PMID: 19167885
Achieving structural diversity using the perpendicular conformation of alpha-substituted phenylcyclopropanes to mimic the bioactive conformation of ortho-substituted biphenyl P4 moieties: discovery of novel, highly potent inhibitors of Factor Xa.
Qiao JX, Cheney DL, Alexander RS, Smallwood AM, King SR, He K, Rendina AR, Luettgen JM, Knabb RM, Wexler RR, Lam PY. Qiao JX, et al. Bioorg Med Chem Lett. 2008 Jul 15;18(14):4118-23. doi: 10.1016/j.bmcl.2008.05.095. Epub 2008 May 29. Bioorg Med Chem Lett. 2008. PMID: 18550370
Discovery of 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide (apixaban, BMS-562247), a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa.
Pinto DJ, Orwat MJ, Koch S, Rossi KA, Alexander RS, Smallwood A, Wong PC, Rendina AR, Luettgen JM, Knabb RM, He K, Xin B, Wexler RR, Lam PY. Pinto DJ, et al. Among authors: smallwood a. J Med Chem. 2007 Nov 1;50(22):5339-56. doi: 10.1021/jm070245n. Epub 2007 Oct 3. J Med Chem. 2007. PMID: 17914785
1-[3-Aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa.
Pinto DJ, Orwat MJ, Quan ML, Han Q, Galemmo RA Jr, Amparo E, Wells B, Ellis C, He MY, Alexander RS, Rossi KA, Smallwood A, Wong PC, Luettgen JM, Rendina AR, Knabb RM, Mersinger L, Kettner C, Bai S, He K, Wexler RR, Lam PY. Pinto DJ, et al. Among authors: smallwood a. Bioorg Med Chem Lett. 2006 Aug 1;16(15):4141-7. doi: 10.1016/j.bmcl.2006.02.069. Epub 2006 May 30. Bioorg Med Chem Lett. 2006. PMID: 16730984
172 results