Edward S Tasber
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Explore the profile of Edward S Tasber including associated specialties, affiliations and a list of published articles.
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8
Citations
56
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Recent Articles
1.
Li C, Lu B, Garbaccio R, Tasber E, Fraley M, Hartman G, et al.
Biochem Pharmacol
. 2010 Jan;
79(10):1526-33.
PMID: 20109439
Compound A, 1-{(3R,3aR)-3-[3-(4-acetylpiperazin-1-yl)propyl]-7-fluoro-3-phenyl-3a,4-dihydro-3H-pyrazolo[5,1-c][1,4]benzoxazin-2-yl}ethanone, is a novel and potent inhibitor of the mitotic kinesin spindle protein. Metabolism studies with human hepatocytes showed that Compound A underwent significant ketone reduction to its...
2.
Rickert K, Schaber M, Torrent M, Neilson L, Tasber E, Garbaccio R, et al.
Arch Biochem Biophys
. 2007 Nov;
469(2):220-31.
PMID: 17999913
The kinesin spindle protein (KSP, also known as Eg5) is essential for the proper separation of spindle poles during mitosis, and inhibition results in mitotic arrest and the formation of...
3.
Garbaccio R, Huang S, Tasber E, Fraley M, Yan Y, Munshi S, et al.
Bioorg Med Chem Lett
. 2007 Sep;
17(22):6280-5.
PMID: 17900896
From HTS lead 1, a novel benzoisoquinolinone class of ATP-competitive Chk1 inhibitors was devised and synthesized via a photochemical route. Using X-ray crystallography as a guide, potency was rapidly enhanced...
4.
Garbaccio R, Tasber E, Neilson L, Coleman P, Fraley M, Olson C, et al.
Bioorg Med Chem Lett
. 2007 Sep;
17(20):5671-6.
PMID: 17804233
Observations from two structurally related series of KSP inhibitors led to the proposal and discovery of dihydropyrazolobenzoxazines that possess ideal properties for cancer drug development. The synthesis and characterization of...
5.
Brnardic E, Garbaccio R, Fraley M, Tasber E, Steen J, Arrington K, et al.
Bioorg Med Chem Lett
. 2007 Sep;
17(21):5989-94.
PMID: 17804227
The development of 2,5-dihydro-4H-pyrazolo[4,3-c]quinolin-4-ones as inhibitors of Chk1 kinase is described. Introduction of a fused ring at the C7/C8 positions of the pyrazoloquinolinone provided an increase in potency while guidance...
6.
Fraley M, Garbaccio R, Arrington K, Hoffman W, Tasber E, Coleman P, et al.
Bioorg Med Chem Lett
. 2006 Jan;
16(7):1775-9.
PMID: 16439123
The evolution of 2,4-diaryl-2,5-dihydropyrroles as inhibitors of KSP is described. Introduction of basic amide and urea moieties to the dihydropyrrole nucleus enhanced potency and aqueous solubility, simultaneously, and provided compounds...
7.
Garbaccio R, Fraley M, Tasber E, Olson C, Hoffman W, Arrington K, et al.
Bioorg Med Chem Lett
. 2006 Jan;
16(7):1780-3.
PMID: 16439122
2,4-Diaryl-2,5-dihydropyrroles have been discovered to be novel, potent and water-soluble inhibitors of KSP, an emerging therapeutic target for the treatment of cancer. A potential concern for these basic KSP inhibitors...
8.
Wu Z, Fraley M, Bilodeau M, Kaufman M, Tasber E, Balitza A, et al.
Bioorg Med Chem Lett
. 2004 Mar;
14(4):909-12.
PMID: 15012992
3,7-Diarylsubstituted imidazopyridines were designed and developed as a new class of KDR kinase inhibitors. A variety of imidazopyridines were synthesized and potent inhibitors of KDR kinase activity were identified with...