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John F MacMaster

Explore the profile of John F MacMaster including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 5
Citations 269
Followers 0
Related Specialties
Biochemistry
Pharmacology
Chemistry
Top 10 Co-Authors
James R Burke
Kim W McIntyre
Kurt R Gregor
Mark A Pattoli
Yuping Qiu
F Christopher Zusi
Joann Strnad
Edwin J Iwanowicz
David J Shuster
Bang-Chi Chen
Published In
Bioorg Med Chem Lett
J Med Chem
J Pharmacol Exp Ther
J Biol Chem
Affiliations
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Recent Articles
1.
Synthesis and biological evaluation of 4-amino derivatives of benzimidazoquinoxaline, benzimidazoquinoline, and benzopyrazoloquinazoline as potent IKK inhibitors
Beaulieu F, Ouellet C, Ruediger E, Belema M, Qiu Y, Yang X, et al.
Bioorg Med Chem Lett . 2007 Jan; 17(5):1233-7. PMID: 17197177
We have recently identified BMS-345541 (1) as a highly selective and potent inhibitor of IKK-2 (IC50 = 0.30 microM), which however was considerably less potent against IKK-1 (IC50 = 4.0...
2.
Collagen and aggrecan degradation is blocked in interleukin-1-treated cartilage explants by an inhibitor of IkappaB kinase through suppression of metalloproteinase expression
Pattoli M, MacMaster J, Gregor K, Burke J
J Pharmacol Exp Ther . 2005 Jul; 315(1):382-8. PMID: 16009742
It has previously been shown that BMS-345541 [4(2'-aminoethyl)amino-1,8-dimethylimidazo(1,2-a)quinoxaline], a highly-selective inhibitor of IkappaB kinase (IKK), blocks both inflammation and joint destruction in murine collagen-induced arthritis. Although this agent has been...
3.
Reductively activated disulfide prodrugs of paclitaxel
Vrudhula V, MacMaster J, Li Z, Kerr D, Senter P
Bioorg Med Chem Lett . 2002 Nov; 12(24):3591-4. PMID: 12443783
A series of unsymmetrical polar disulfide prodrugs 2-5 of paclitaxel were designed and synthesized as reductively activated prodrugs. These compounds behaved as prodrugs in vitro on L2987 lung carcinoma cells....
4.
BMS-345541 is a highly selective inhibitor of I kappa B kinase that binds at an allosteric site of the enzyme and blocks NF-kappa B-dependent transcription in mice
Burke J, Pattoli M, Gregor K, Brassil P, MacMaster J, McIntyre K, et al.
J Biol Chem . 2002 Oct; 278(3):1450-6. PMID: 12403772
The signal-inducible phosphorylation of serines 32 and 36 of I kappa B alpha is critical in regulating the subsequent ubiquitination and proteolysis of I kappa B alpha, which then releases...
5.
Discovery of N-[2-[2-[[3-methoxy-4-(5-oxazolyl)phenyl]amino]-5-oxazolyl]phenyl]-N-methyl-4- morpholineacetamide as a novel and potent inhibitor of inosine monophosphate dehydrogenase with excellent in vivo activity
Murali Dhar T, Shen Z, Guo J, Liu C, Watterson S, Gu H, et al.
J Med Chem . 2002 May; 45(11):2127-30. PMID: 12014950
Inosine monophosphate dehydrogenase (IMPDH) is a key enzyme that is involved in the de novo synthesis of purine nucleotides. Novel 2-aminooxazoles were synthesized and tested for inhibition of IMPDH catalytic...