Stephen Stokes
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Explore the profile of Stephen Stokes including associated specialties, affiliations and a list of published articles.
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Articles
13
Citations
137
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Recent Articles
1.
Shields J, Baker D, Balazs A, Bommakanti G, Casella R, Cao S, et al.
J Med Chem
. 2025 Feb;
68(4):4582-4595.
PMID: 39928839
Hematopoietic progenitor kinase 1 (HPK1) is a negative regulator of the T cell receptor signaling pathway and is therefore a target of interest for immunooncology. Nonselective HPK1 inhibitors may affect...
2.
McCoull W, Thomson C, Braybrooke E, Chan C, Colclough N, Cortes Gonzalez M, et al.
J Med Chem
. 2025 Jan;
68(3):3700-3748.
PMID: 39869768
Despite recent advances in the inhibition of EGFR (epidermal growth factor receptor), there remains a clinical need for new EGFR Exon20 insertion (Ex20Ins) inhibitors that spare EGFR WT. Herein, we...
3.
Scott J, Stead D, Barlaam B, Breed J, Carbajo R, Chiarparin E, et al.
J Med Chem
. 2023 Feb;
66(4):2918-2945.
PMID: 36727211
Herein, we report the optimization of a meta-substituted series of selective estrogen receptor degrader (SERD) antagonists for the treatment of ER+ breast cancer. Structure-based design together with the use of...
4.
Scott J, Moss T, Barlaam B, Davey P, Fairley G, Gangl E, et al.
ACS Med Chem Lett
. 2020 Dec;
11(12):2519-2525.
PMID: 33335676
Herein we describe our efforts using a late stage functionalization together with more traditional synthetic approaches to generate fluorinated analogues of the clinical candidate AZD9833. The effects of the addition...
5.
Scott J, Moss T, Balazs A, Barlaam B, Breed J, Carbajo R, et al.
J Med Chem
. 2020 Sep;
63(23):14530-14559.
PMID: 32910656
Herein we report the optimization of a series of tricyclic indazoles as selective estrogen receptor degraders (SERD) and antagonists for the treatment of ER breast cancer. Structure based design together...
6.
Degorce S, Anjum R, Dillman K, Drew L, Groombridge S, Halsall C, et al.
Bioorg Med Chem
. 2018 Feb;
26(4):913-924.
PMID: 29398441
We have developed a series of orally efficacious IRAK4 inhibitors, based on a scaffold hopping strategy and using rational structure based design. Efforts to tackle low permeability and high efflux...
7.
Alanine T, Stokes S, Roberts C, Scott J
Org Biomol Chem
. 2017 Dec;
16(1):53-56.
PMID: 29226938
A palladium mediated C-H aziridination reaction of 3,3,5,5-substituted-piperazin-2-ones has been developed using phenyliodonium diacetate (PIDA) and succinic acid to give synthetically useful bicyclic aziridines, in moderate to good yields. Succinic...
8.
Brough P, Baker L, Bedford S, Brown K, Chavda S, Chell V, et al.
J Med Chem
. 2017 Feb;
60(6):2271-2286.
PMID: 28199108
Libraries of nonpurified resorcinol amide derivatives were screened by surface plasmon resonance (SPR) to determine the binding dissociation constant (off-rate, k) for compounds binding to the pyruvate dehydrogenase kinase (PDHK)...
9.
Bradbury R, Callis R, Carr G, Chen H, Clark E, Feron L, et al.
J Med Chem
. 2016 Aug;
59(17):7801-17.
PMID: 27528113
Here we report the discovery and optimization of a series of bivalent bromodomain and extraterminal inhibitors. Starting with the observation of BRD4 activity of compounds from a previous program, the...
10.
Massey A, Stokes S, Browne H, Foloppe N, Fiumana A, Scrace S, et al.
Oncotarget
. 2015 Oct;
6(34):35797-812.
PMID: 26437226
Chk1 kinase is a critical component of the DNA damage response checkpoint especially in cancer cells and targeting Chk1 is a potential therapeutic opportunity for potentiating the anti-tumor activity of...