Michael A Galella
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Explore the profile of Michael A Galella including associated specialties, affiliations and a list of published articles.
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Citations
154
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Recent Articles
11.
Watterson S, De Lucca G, Shi Q, Langevine C, Liu Q, Batt D, et al.
J Med Chem
. 2016 Sep;
59(19):9173-9200.
PMID: 27583770
Bruton's tyrosine kinase (BTK), a nonreceptor tyrosine kinase, is a member of the Tec family of kinases. BTK plays an essential role in B cell receptor (BCR)-mediated signaling as well...
12.
Gilmore J, Sheppeck 2nd J, Watterson S, Haque L, Mukhopadhyay P, Tebben A, et al.
J Med Chem
. 2016 Jun;
59(13):6248-64.
PMID: 27309907
Sphingosine-1-phosphate (S1P) is a bioactive sphingolipid metabolite that regulates a multitude of physiological processes such as lymphocyte trafficking, cardiac function, vascular development, and inflammation. Because of the ability of S1P1...
13.
Brown G, Shi Q, Delucca G, Batt D, Galella M, Cvijic M, et al.
Bioorg Med Chem Lett
. 2015 Dec;
26(2):662-666.
PMID: 26631321
A novel cyclohexenyl series of CCR2 antagonists has been discovered. This series of small, rigid compounds exhibits submicromolar binding affinity for CCR2. Modification of the substituents on the cyclohexene ring...
14.
Yang M, Murali Dhar T, Xiao Z, Xiao H, Duan J, Jiang B, et al.
J Med Chem
. 2015 Apr;
58(10):4278-90.
PMID: 25905990
An empirical approach to improve the microsomal stability and CYP inhibition profile of lead compounds 1a and 1b led to the identification of 5 (BMS-341) as a dissociated glucocorticoid receptor...
15.
Liu C, Lin J, Everlof G, Gesenberg C, Zhang H, Marathe P, et al.
Bioorg Med Chem Lett
. 2013 Apr;
23(10):3028-33.
PMID: 23578688
A series of carbamoylmethylene linked prodrugs of 1 (BMS-582949), a clinical p38α inhibitor, were synthesized and evaluated. Though the phosphoryloxymethylene carbamates (3, 4, and 5) and α-aminoacyloxymethylene carbamates (22, 23,...
16.
Diphenylpyridylethanamine (DPPE) derivatives as cholesteryl ester transfer protein (CETP) inhibitors
Harikrishnan L, Finlay H, Qiao J, Kamau M, Jiang J, Wang T, et al.
J Med Chem
. 2012 Jun;
55(13):6162-75.
PMID: 22650305
A series of diphenylpyridylethanamine (DPPE) derivatives was identified exhibiting potent CETP inhibition. Replacing the labile ester functionality in the initial lead 7 generated a series of amides and ureas. Further...
17.
Watterson S, Langevine C, Van Kirk K, Kempson J, Guo J, Spergel S, et al.
Bioorg Med Chem Lett
. 2011 Oct;
21(23):7006-12.
PMID: 22018461
The synthesis, structure-activity relationships (SAR), and biological results of pyridyl-substituted azaindole based tricyclic inhibitors of IKK2 are described. Compound 4m demonstrated potent in vitro potency, acceptable pharmacokinetic and physicochemical properties,...
18.
Salvati M, Balog A, Shan W, Rampulla R, Giese S, Mitt T, et al.
Bioorg Med Chem Lett
. 2008 Feb;
18(6):1910-5.
PMID: 18291644
A novel series of [2.2.1]-oxabicyclo imide-based compounds were identified as potent antagonists of the androgen receptor. Molecular modeling and iterative drug design were applied to optimize this series. The lead...
19.
Discovery of potent and muscle selective androgen receptor modulators through scaffold modifications
Li J, Sutton J, Nirschl A, Zou Y, Wang H, Sun C, et al.
J Med Chem
. 2007 Jun;
50(13):3015-25.
PMID: 17552509
A novel series of imidazolin-2-ones were designed and synthesized as highly potent, orally active and muscle selective androgen receptor modulators (SARMs), with most of the compounds exhibiting low nM in...
20.
Shi Y, Zhang J, Grazier N, Stein P, Atwal K, Traeger S, et al.
J Org Chem
. 2004 Jan;
69(1):188-91.
PMID: 14703396
N,N'-Disubstituted ketene aminals are bioisosteres of thioureas and are useful building blocks in many synthetic operations. A convenient one-pot synthesis of N,N'-disubstituted ketene aminals from activated methylene compounds and isothiocyanates...