Thomas R Caferro
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Explore the profile of Thomas R Caferro including associated specialties, affiliations and a list of published articles.
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7
Citations
75
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Recent Articles
1.
Waterson A, Petrov K, Hornberger K, Hubbard R, Sammond D, Smith S, et al.
Bioorg Med Chem Lett
. 2009 Feb;
19(5):1332-6.
PMID: 19208477
Aniline 'headgroups' were synthesized and incorporated into an alkynyl thienopyrimidine series of EGFR and ErbB-2 inhibitors. Potent inhibition of enzyme activity and cellular proliferation was observed. In certain instances, protein...
2.
Rheault T, Caferro T, Dickerson S, Donaldson K, Gaul M, Goetz A, et al.
Bioorg Med Chem Lett
. 2008 Dec;
19(3):817-20.
PMID: 19111461
Two new series of potent and selective dual EGFR/ErbB-2 kinase inhibitors derived from novel thienopyrimidine cores have been identified. Isomeric thienopyrimidine cores were evaluated as isosteres for a 4-anilinoquinazoline core...
3.
Stevens K, Alligood K, Alberti J, Caferro T, Chamberlain S, Dickerson S, et al.
Bioorg Med Chem Lett
. 2008 Nov;
19(1):21-6.
PMID: 19028424
A novel class of pyrrolidinyl-acetyleneic thieno[3,2-d]pyrimidines has been identified which potently inhibit the EGFR and ErbB-2 receptor tyrosine kinases. Synthetic modifications of the pyrrolidine carbamate moiety result in a range...
4.
Long Y, Higuchi R, Caferro T, Lau T, Wu M, Cummings M, et al.
Bioorg Med Chem Lett
. 2008 Apr;
18(9):2967-71.
PMID: 18400499
Modification on a lead series of [1,4]oxazino[3,2-g]quinolin-7-ones at the 2-position led to selective androgen receptor modulators with improved in vivo activity. The most potent analog (-)-33a exhibited full maintenance of...
5.
Wood E, Shewchuk L, Ellis B, Brignola P, Brashear R, Caferro T, et al.
Proc Natl Acad Sci U S A
. 2008 Feb;
105(8):2773-8.
PMID: 18287036
Analysis of the x-ray crystal structure of mono-substituted acetylenic thienopyrimidine 6 complexed with the ErbB family enzyme ErbB-4 revealed a covalent bond between the terminal carbon of the acetylene moiety...
6.
Higuchi R, Thompson A, Chen J, Caferro T, Cummings M, Deckhut C, et al.
Bioorg Med Chem Lett
. 2007 Aug;
17(19):5442-6.
PMID: 17703938
A series of androgen receptor modulators based on 8H-[1,4]oxazino[2,3-f]quinolin-8-ones was synthesized and evaluated in an androgen receptor transcriptional activation assay. The most potent analogues from the series exhibited single-digit nanomolar...
7.
Higuchi R, Arienti K, Lopez F, Mani N, Mais D, Caferro T, et al.
J Med Chem
. 2007 Apr;
50(10):2486-96.
PMID: 17439112
Recent interest in orally available androgens has fueled the search for new androgens for use in hormone replacement therapy and as anabolic agents. In pursuit of this, we have discovered...