Mark T. Kershaw

Publications18
h-index8
Citations185
Highly Influential Citations0
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Aminoquinazolines as TRPV1 antagonists: modulation of drug-like properties through the exploration of 2-position substitution.
A focused SAR exploration of the lead 4-aminoquinazoline TRPV1 antagonist 2 led to the discovery of compound 18. In rats, compound 18 is readily absorbed following oral dosing and demonstrates… Expand
  • 15
Ethyl 2-chlorooxazole-4-carboxylate: a versatile intermediate for the synthesis of substituted oxazoles.
[reaction: see text] By using a sequence of regiocontrolled halogenation and palladium-catalyzed coupling reactions, the synthesis of variously substituted oxazoles from ethyl… Expand
  • 41
Synthesis of 2-aryl-oxazolo[4,5-c]quinoline-4(5H)-ones and 2-aryl-thiazolo[4,5-c]quinoline-4(5H)-ones.
[reaction: see text] Novel and highly efficient syntheses of oxazolo[4,5-c]quinoline-4(5H)-ones (1) and thiazolo[4,5-c]quinoline-4(5H)-ones (2) from ethyl 2-chlorooxazole-4-carboxylate (4) and ethyl… Expand
  • 50
FT-1101: A Structurally Distinct Pan-BET Bromodomain Inhibitor with Activity in Preclinical Models of Hematologic Malignancies
Members of the Bromodomain and Extra-Terminal (BET) family of bromodomain-containing proteins (BRD2, BRD3, BRD4, and BRDT) bind to acetylated lysine residues on histone tails and act as epigenetic… Expand
  • 11
1-Benzylbenzimidazoles: the discovery of a novel series of bradykinin B(1) receptor antagonists.
The design, synthesis, and structure-activity studies of a novel series of BK B(1) receptor antagonists based on a 1-benzylbenzimidazole chemotype are described. A number of compounds, for example,… Expand
  • 8
Aminopyrazine CB1 receptor inverse agonists.
A series of 5,6-diaryl-2-amino-pyrazines were prepared and found to have antagonist-like properties at the CB1 receptor. Subsequent SAR studies optimized both receptor potency and drug-like… Expand
  • 9
Regiocontrolled synthesis of substituted thiazoles.
The regiocontrolled synthesis of 2,5-disubstituted and 2,4,5-trisubstituted thiazoles from ethyl 2-bromo-5-chloro-4-thiazolecarboxylate 1 using sequential palladium-catalyzed coupling reactions is… Expand
  • 30
Structure-based design and identification of FT-2102 (olutasidenib), a potent mutant-selective IDH1 inhibitor.
Inhibition of mutant IDH1 is being evaluated clinically as a treatment option for oncology. Here we describe structure-based design and optimization of quinoline lead compounds to identify FT-2102, a… Expand
  • 8
Structure-Based Design and Identification of FT-2102 (Olutasidenib), a Potent Mutant-Selective IDH1 Inhibitor.
Inhibition of mutant IDH1 is being evaluated clinically as a treatment option for oncology. Here we describe the structure-based design and optimization of quinoline lead compounds to identify… Expand
  • 5
Advancing Parallel Solution Phase Library Synthesis through Efficient Purification, Quantitation, and Characterization Techniques
Historically, access to large numbers of quality compounds in a parallel solution phase library synthesis environment has been hindered by the inability to rapidly purify, quantitate, and… Expand
  • 3