Philip A MacFaul
Overview
Explore the profile of Philip A MacFaul including associated specialties, affiliations and a list of published articles.
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Articles
16
Citations
139
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Recent Articles
1.
Barlaam B, Cadogan E, Campbell A, Colclough N, Dishington A, Durant S, et al.
ACS Med Chem Lett
. 2018 Aug;
9(8):809-814.
PMID: 30128072
We report the discovery of a novel series of 3-cinnoline carboxamides as highly potent and selective ataxia telangiectasia mutated (ATM) kinase inhibitors. Optimization of this series focusing on potency and...
2.
Pike K, Barlaam B, Cadogan E, Campbell A, Chen Y, Colclough N, et al.
J Med Chem
. 2018 Apr;
61(9):3823-3841.
PMID: 29683659
ATM inhibitors, such as 7, have demonstrated the antitumor potential of ATM inhibition when combined with DNA double-strand break-inducing agents in mouse xenograft models. However, the properties of 7 result...
3.
Scott J, Bailey A, Davies R, Degorce S, MacFaul P, Gingell H, et al.
ACS Med Chem Lett
. 2016 Jan;
7(1):94-9.
PMID: 26819673
A series of tetrahydroisoquinoline phenols was modified to give an estrogen receptor downregulator-antagonist profile. Optimization around the core, alkyl side chain, and pendant aryl ring resulted in compounds with subnanomolar...
4.
Bragg R, Brocklehurst S, Gustafsson F, Goodman J, Hickling K, MacFaul P, et al.
Chem Res Toxicol
. 2015 Sep;
28(10):1991-9.
PMID: 26351880
The oral dipeptidyl peptidase 1 (DPP1) inhibitor AZD5248 showed aortic binding in a rat quantitative whole-body autoradiography (QWBA) study, and its development was terminated prior to human dosing. A mechanistic...
5.
Scott J, Bowker S, Brocklehurst K, Brown H, Clarke D, Easter A, et al.
J Med Chem
. 2014 Oct;
57(21):8984-98.
PMID: 25286150
Agonism of GPR119 is viewed as a potential therapeutic approach for the treatment of type II diabetes and other elements of metabolic syndrome. During progression of a previously disclosed candidate...
6.
Scott J, Brocklehurst K, Brown H, Clarke D, Coe H, Groombridge S, et al.
Bioorg Med Chem Lett
. 2013 May;
23(11):3175-9.
PMID: 23628336
A series of conformationally restricted GPR119 agonists were prepared based around a 3,8-diazabicyclo[3.2.1]octane scaffold. Examples were found to have markedly different pharmacology in mouse and human despite similar levels of...
7.
Crawford J, Kenny P, Bowyer J, Cook C, Finlayson J, Heyes C, et al.
J Med Chem
. 2012 Sep;
55(20):8827-37.
PMID: 22984809
Rational structure-based design has yielded highly potent inhibitors of cathepsin K (Cat K) with excellent physical properties, selectivity profiles, and pharmacokinetics. Compounds with a 3,4-(CH₃O)₂Ph motif, such as 31, were...
8.
Dossetter A, Bowyer J, Cook C, Crawford J, Finlayson J, Heron N, et al.
Bioorg Med Chem Lett
. 2012 Aug;
22(17):5563-8.
PMID: 22858142
The discovery of nitrile compound 4, a potent inhibitor of Cathepsin K (Cat K) with good bioavailability in dog is described. The compound was used to demonstrate target engagement and...
9.
Dossetter A, Beeley H, Bowyer J, Cook C, Crawford J, Finlayson J, et al.
J Med Chem
. 2012 Jun;
55(14):6363-74.
PMID: 22742641
Directed screening of nitrile compounds revealed 3 as a highly potent cathepsin K inhibitor but with cathepsin S activity and very poor stability to microsomes. Synthesis of compounds with reduced...
10.
Scott J, Birch A, Brocklehurst K, Broo A, Brown H, Butlin R, et al.
J Med Chem
. 2012 May;
55(11):5361-79.
PMID: 22545772
G protein coupled receptor 119 (GPR119) is viewed as an attractive target for the treatment of type 2 diabetes and other elements of the metabolic syndrome. During a program toward...