Derek Norris
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Explore the profile of Derek Norris including associated specialties, affiliations and a list of published articles.
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21
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1210
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Recent Articles
1.
Qiao J, Williams D, Gill P, Li L, Norris D, Tokarski J, et al.
J Med Chem
. 2024 Oct;
67(21):19736-19754.
PMID: 39437163
We describe the design, synthesis, and structure-activity relationship (SAR) of heterobifunctional RET ligand-directed degraders (LDDs) derived from three different second-generation RET inhibitors. These LDDs are composed of a target binding...
2.
Hill M, Fang H, Norris D, Delucca G, Huang H, DeBenedetto M, et al.
ACS Med Chem Lett
. 2022 Jul;
13(7):1165-1171.
PMID: 35859878
We describe the synthesis of triazole-containing carboline derivatives and their utility as bromodomain and extra-terminal (BET) inhibitors. A convergent synthetic route permitted the detailed investigation of deuteration and fluorination strategies...
3.
Gavai A, Norris D, Delucca G, Tortolani D, Tokarski J, Dodd D, et al.
J Med Chem
. 2021 Sep;
64(19):14247-14265.
PMID: 34543572
Inhibition of the bromodomain and extra-terminal (BET) family of adaptor proteins is an attractive strategy for targeting transcriptional regulation of key oncogenes, such as c-MYC. Starting with the screening hit...
4.
Gavai A, Quesnelle C, Norris D, Han W, Gill P, Shan W, et al.
ACS Med Chem Lett
. 2015 May;
6(5):523-7.
PMID: 26005526
Structure-activity relationships in a series of (2-oxo-1,4-benzodiazepin-3-yl)-succinamides identified highly potent inhibitors of γ-secretase mediated signaling of Notch1/2/3/4 receptors. On the basis of its robust in vivo efficacy at tolerated doses...
5.
Shan W, Balog A, Quesnelle C, Gill P, Han W, Norris D, et al.
Bioorg Med Chem Lett
. 2015 Apr;
25(9):1905-9.
PMID: 25857941
This Letter describes synthesis, SAR, and biological activity of (2-oxo-1,4-benzodiazepin-3-yl)-succinamides as inhibitors of γ-secretase mediated signaling of Notch receptors. Optimization of this series led to the identification of BMS-871 (compound...
6.
Wong T, Lee F, Emanuel S, Fairchild C, Fargnoli J, Fink B, et al.
Clin Cancer Res
. 2011 May;
17(12):4031-41.
PMID: 21531814
Purpose: The extensive involvement of the HER kinases in epithelial cancer suggests that kinase inhibitors targeting this receptor family have the potential for broad spectrum antitumor activity. BMS-690514 potently inhibits...
7.
Fink B, Norris D, Mastalerz H, Chen P, Goyal B, Zhao Y, et al.
Bioorg Med Chem Lett
. 2010 Dec;
21(2):781-5.
PMID: 21177105
A novel series of 5-((4-aminopiperidin-1-yl)methyl)-pyrrolo[2,1-f][1,2,4]triazin-4-amines with small aniline substituents at the C4 position were optimized for dual EGFR and HER2 protein tyrosine kinase inhibition. Compound 8l exhibited promising oral efficacy...
8.
Gavai A, Fink B, Fairfax D, Martin G, Rossiter L, Holst C, et al.
J Med Chem
. 2009 Oct;
52(21):6527-30.
PMID: 19821562
Structure-activity relationships in a series of 4-[1H-indazol-5-ylamino]pyrrolo[2,1-f][1,2,4]triazine-6-carbamates identified dual human epidermal growth factor receptor (HER)1/HER2 kinase inhibitors with excellent biochemical potency and kinase selectivity. On the basis of its favorable...
9.
Mastalerz H, Chang M, Chen P, Fink B, Gavai A, Han W, et al.
Bioorg Med Chem Lett
. 2007 Jul;
17(17):4947-54.
PMID: 17606372
Pyrrolotriazine dual EGFR/HER2 kinase inhibitors with a 5-((4-aminopiperidin-1-yl)methyl) solubilizing group were found to be superior to analogs with previously reported C-5 solubilizing groups. New synthetic methodology was developed for the...
10.
Das J, Chen P, Norris D, Padmanabha R, Lin J, Moquin R, et al.
J Med Chem
. 2006 Dec;
49(23):6819-32.
PMID: 17154512
2-aminothiazole (1) was discovered as a novel Src family kinase inhibitor template through screening of our internal compound collection. Optimization through successive structure-activity relationship iterations identified analogs 2 (Dasatinib, BMS-354825)...