Scott H Dickerson
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Explore the profile of Scott H Dickerson including associated specialties, affiliations and a list of published articles.
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21
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773
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Recent Articles
1.
Rheault T, Stellwagen J, Adjabeng G, Hornberger K, Petrov K, Waterson A, et al.
ACS Med Chem Lett
. 2014 Jun;
4(3):358-62.
PMID: 24900673
Hyperactive signaling of the MAP kinase pathway resulting from the constitutively active B-Raf(V600E) mutated enzyme has been observed in a number of human tumors, including melanomas. Herein we report the...
2.
Tang J, Lackey K, Dickerson S
Bioorg Med Chem Lett
. 2012 Dec;
23(1):66-70.
PMID: 23218715
A series of novel, potent 4-aminothienopyridine B-Raf kinase inhibitors was designed and synthesized using knowledge-based design. Compounds 5f, and 6k exhibited not only excellent potency in both enzyme assay (IC(50)=5.1,...
3.
Greger J, Eastman S, Zhang V, Bleam M, Hughes A, Smitheman K, et al.
Mol Cancer Ther
. 2012 Mar;
11(4):909-20.
PMID: 22389471
Recent results from clinical trials with the BRAF inhibitors GSK2118436 (dabrafenib) and PLX4032 (vemurafenib) have shown encouraging response rates; however, the duration of response has been limited. To identify determinants...
4.
Stellwagen J, Adjabeng G, Arnone M, Dickerson S, Han C, Hornberger K, et al.
Bioorg Med Chem Lett
. 2011 Jul;
21(15):4436-40.
PMID: 21733693
A potent series of inhibitors against the B-Raf(V600E) kinase have been developed that show excellent activity in cellular assays and good oral bioavailability in rats. The key structural features of...
5.
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...
6.
Thomson S, Banker P, Bickett D, Boucheron J, Carter H, Clancy D, et al.
Bioorg Med Chem Lett
. 2009 Jan;
19(4):1177-82.
PMID: 19138846
Key binding interactions of the anthranilimide based glycogen phosphorylase a (GPa) inhibitor 2 from X-ray crystallography studies are described. This series of compounds bind to the AMP site of GP....
7.
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...
8.
Emmitte K, Wilson B, Baum E, Emerson H, Kuntz K, Nailor K, et al.
Bioorg Med Chem Lett
. 2008 Dec;
19(3):1004-8.
PMID: 19101143
The optimization of imidazo[1,2-a]pyridine inhibitors as potent and selective inhibitors of IGF-1R is presented. Further optimization of oral exposure in mice is also discussed. Detailed selectivity, in vitro activity, and...
9.
Sparks S, Banker P, Bickett D, Clancy D, Dickerson S, Garrido D, et al.
Bioorg Med Chem Lett
. 2008 Dec;
19(3):981-5.
PMID: 19095443
Optimization of the amino acid residue of a series of anthranilimide-based glycogen phosphorylase inhibitors is described leading to the identification of serine and threonine ether analogs. t-Butylthreonine analog 20 displayed...
10.
Sparks S, Banker P, Bickett D, Carter H, Clancy D, Dickerson S, et al.
Bioorg Med Chem Lett
. 2008 Dec;
19(3):976-80.
PMID: 19095442
Optimization of the amino acid residue within a series of anthranilimide-based glycogen phosphorylase inhibitors is described. These studies culminated in the identification of anthranilimides 16 and 22 which displayed potent...