John Woolfrey
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Explore the profile of John Woolfrey including associated specialties, affiliations and a list of published articles.
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14
Citations
70
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Recent Articles
1.
Li D, Woolfrey J, Jiang S, Jensen C, Zhao W, Kakar S, et al.
Gastrointest Endosc
. 2017 Aug;
87(3):755-765.e1.
PMID: 28843582
Background And Aims: Sessile serrated adenomas (SSAs) are precursors of 15% to 30% of colorectal cancers but are frequently underdiagnosed. We sought to measure the SSA detection rate (SDR) and...
2.
Takeuchi C, Kim B, Blazey C, Ma S, Johnson H, Anand N, et al.
J Med Chem
. 2013 Feb;
56(6):2218-34.
PMID: 23394126
A series of novel, highly potent, selective, and ATP-competitive mammalian target of rapamycin (mTOR) inhibitors based on a benzoxazepine scaffold have been identified. Lead optimization resulted in the discovery of...
3.
Forsyth T, Kearney P, Kim B, Johnson H, Aay N, Arcalas A, et al.
Bioorg Med Chem Lett
. 2012 Nov;
22(24):7653-8.
PMID: 23127890
We report the discovery of a series of 4-aryl-2-aminoalkylpyrimidine derivatives as potent and selective JAK2 inhibitors. High throughput screening of our in-house compound library led to the identification of hit...
4.
Ibrahim M, Johnson H, Jeong J, Lewis G, Shi X, Noguchi R, et al.
J Med Chem
. 2012 Jan;
55(3):1368-81.
PMID: 22214363
A series of subtype selective sphingosine 1-phosphate receptor 1 (S1P(1)) antagonists are disclosed. Our high-throughput screening campaign revealed hit 1 for which an increase in potency and mouse oral exposure...
5.
Zhang P, Huang W, Wang L, Bao L, Jia Z, Bauer S, et al.
Bioorg Med Chem Lett
. 2009 Mar;
19(8):2179-85.
PMID: 19297154
Systematic SAR studies of in vitro factor Xa inhibitory activity around compound 1 were performed by modifying each of the three phenyl rings. A class of highly potent, selective, efficacious...
6.
Bauer S, Goldman E, Huang W, Su T, Wang L, Woolfrey J, et al.
Bioorg Med Chem Lett
. 2004 Jul;
14(15):4045-50.
PMID: 15225723
Parallel synthesis and iterative optimization led to the discovery of a series of potent and specific factor Xa inhibitors demonstrating excellent in vitro activity with promising pharmacokinetics.
7.
Jia Z, Su T, Zuckett J, Wu Y, Goldman E, Li W, et al.
Bioorg Med Chem Lett
. 2004 Apr;
14(9):2073-8.
PMID: 15080981
A class of N,N-dialkylated 4-(4-arylsulfonylpiperazine-1-carbonyl)-benzamidines and 4-((4-arylsulfonyl)-2-oxo-piperazin-1-ylmethyl)-benzamidines has been discovered as potent factor Xa inhibitors with desirable in vitro and in vivo anticoagulant activity, but with low oral bioavailability. The...
8.
Zhang P, Bao L, Zuckett J, Jia Z, Woolfrey J, Arfsten A, et al.
Bioorg Med Chem Lett
. 2004 Mar;
14(4):989-93.
PMID: 15013007
Compound 2 containing an aminomethylbenzoyl moiety as the S4 binding motif was synthesized in order to modulate hydrophlicity of anthranilamide-based factor Xa inhibitors with substituted biphenyl P4 groups. Structure-activity relationship...
9.
Jia Z, Wu Y, Huang W, Zhang P, Song Y, Woolfrey J, et al.
Bioorg Med Chem Lett
. 2004 Feb;
14(5):1229-34.
PMID: 14980671
Using N,N-dialkylated benzamidines as the novel P4 motifs, we have designed and synthesized a class of 1-(2-naphthyl)-1H-pyrazole-5-carboxylamides as highly potent and selective fXa inhibitors with significantly improved hydrophilicity and in...
10.
Su T, Yang H, Volkots D, Woolfrey J, Dam S, Wong P, et al.
Bioorg Med Chem Lett
. 2003 Mar;
13(4):729-32.
PMID: 12639568
The structure-activity relationship of a novel series of substituted piperazinone-based factor Xa inhibitors is described. The most potent compound 34 displays IC(50) of 0.9 nM.