Jeremy I Levin
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Explore the profile of Jeremy I Levin including associated specialties, affiliations and a list of published articles.
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30
Citations
187
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Recent Articles
1.
Horan J, Kuzmich D, Liu P, Disalvo D, Lord J, Mao C, et al.
Bioorg Med Chem Lett
. 2015 Dec;
26(2):466-471.
PMID: 26687487
Poor solubility and cationic amphiphilic drug-likeness were liabilities identified for a lead series of S1P3-sparing, S1P1 agonists originally developed from a high-throughput screening campaign. This work describes the subsequent optimization...
2.
Zapf C, Bloom J, Li Z, Dushin R, Nittoli T, Otteng M, et al.
Bioorg Med Chem Lett
. 2011 Jul;
21(15):4602-7.
PMID: 21715165
An extension of our previously reported series of macrocyclic ortho-aminobenzamide Hsp90 inhibitors is reported. Addition of a second methyl group to the tether provided analogs that show increased potency in...
3.
Zapf C, Bloom J, McBean J, Dushin R, Golas J, Liu H, et al.
Bioorg Med Chem Lett
. 2011 May;
21(12):3627-31.
PMID: 21605975
A novel series of macrocyclic ortho-aminobenzamide Hsp90 inhibitors is reported. In continuation of our research, heterocycle-containing tethers were explored with the intent to further improve potency and minimize hERG liabilities....
4.
Zapf C, Bloom J, McBean J, Dushin R, Nittoli T, Otteng M, et al.
Bioorg Med Chem Lett
. 2011 Apr;
21(11):3411-6.
PMID: 21515049
A novel series of macrocyclic ortho-aminobenzamide Hsp90 inhibitors is reported. In continuation of our research in this area, macrocyclic amides and lactams were explored to reduce the risk of hERG...
5.
Zapf C, Bloom J, McBean J, Dushin R, Nittoli T, Ingalls C, et al.
Bioorg Med Chem Lett
. 2011 Mar;
21(8):2278-82.
PMID: 21420297
A novel series of macrocyclic ortho-aminobenzamide Hsp90 inhibitors is reported. A basic nitrogen within the tether linking the aniline nitrogen atom to a tetrahydroindolone moiety allowed access to compounds with...
6.
Wang X, Berger D, Salaski E, Torres N, Dutia M, Hanna C, et al.
J Med Chem
. 2010 Oct;
53(21):7874-8.
PMID: 20961062
Novel indazolylpyrazolo[1,5-a]pyrimidine analogues have been prepared and found to be extremely potent type I B-Raf inhibitors. The lead compound shows good selectivity against a panel of 60 kinases, possesses a...
7.
Di Grandi M, Berger D, Hopper D, Zhang C, Dutia M, Dunnick A, et al.
Bioorg Med Chem Lett
. 2009 Oct;
19(24):6957-61.
PMID: 19875283
A novel series of pyrazolo[1,5-a]pyrimidines bearing a 3-hydroxyphenyl group at C(3) and substituted tropanes at C(7) have been identified as potent B-Raf inhibitors. Exploration of alternative functional groups as a...
8.
Berger D, Torres N, Dutia M, Powell D, Ciszewski G, Gopalsamy A, et al.
Bioorg Med Chem Lett
. 2009 Oct;
19(23):6519-23.
PMID: 19864136
As part of our research effort to discover B-Raf kinase inhibitors, we prepared a series of C-3 substituted N-(3-(pyrazolo[1,5-a]pyrimidin-7-yl)phenyl)-3-(trifluoromethyl)benzamides. X-ray crystallography studies revealed that one of the more potent inhibitors...
9.
Wang X, Berger D, Salaski E, Torres N, Hu Y, Levin J, et al.
Bioorg Med Chem Lett
. 2009 Oct;
19(23):6571-4.
PMID: 19854649
A series of pyrazolo[1,5-alpha]pyrimidine analogs has been prepared and found to be potent and selective B-Raf inhibitors. Molecular modeling suggests they bind to the active conformation of the enzyme.
10.
Li W, Hu Y, Li J, Thomason J, DeVincentis D, Du X, et al.
Bioorg Med Chem Lett
. 2009 Jul;
19(16):4546-50.
PMID: 19625186
Potent 3,4-disubstituted benzofuran P1' MMP-13 inhibitors have been prepared. Selectivity over MMP-2 was achieved through a substituent at the C4 position of the benzofuran P1' moiety of the molecule. By...