Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 63, Issue 14, Pages 7817-7826Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.0c00596
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Funding
- 2017 AACR-Bayer Innovation and Discovery grant [17-80-44-GRAY]
- DF/HCC GI SPORE Developmental Research Project Award [P50CA127003]
- Hale Center for Pancreatic Research
- American Cancer Society [132205-RSG-18-039-01-DMC]
- Welch Foundation [I1829]
- NIH [5U01CA207160]
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Doublecortin-like kinase 1 (DCLK1) is a serine/threonine kinase that is overexpressed in gastrointestinal cancers, including esophageal, gastric, colorectal, and pancreatic cancers. DCLK1 is also used as a marker of tuft cells, which regulate type II immunity in the gut. However, the substrates and functions of DCLK1 are understudied. We recently described the first selective DCLK1/2 inhibitor, DCLK1-IN-1, developed to aid the functional characterization of this important kinase. Here we describe the synthesis and structure-activity relationships of 5,11-dihydro-6H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6-one DCLK1 inhibitors, resulting in the identification of DCLK1-IN-1.
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