A5043674524- Microtubule and mitosis dynamics
- Cancer-related Molecular Pathways
- Quinazolinone synthesis and applications
- Microbial Natural Products and Biosynthesis
- Ubiquitin and proteasome pathways
- Protein Kinase Regulation and GTPase Signaling
- Melanoma and MAPK Pathways
- Protein Tyrosine Phosphatases
- Cell Adhesion Molecules Research
- PI3K/AKT/mTOR signaling in cancer
- Autophagy in Disease and Therapy
- Cancer Mechanisms and Therapy
- Photosynthetic Processes and Mechanisms
- Sirtuins and Resveratrol in Medicine
- Monoclonal and Polyclonal Antibodies Research
- Glycosylation and Glycoproteins Research
- Biochemical and Molecular Research
- Synthesis and biological activity
Guangzhou Institutes of Biomedicine and Health
2014-2019
Chinese Academy of Sciences
2014-2019
A series of 2-amino-2,3-dihydro-1H-indene-5-carboxamides were designed and synthesized as new selective discoidin domain receptor 1 (DDR1) inhibitors. One the representative compounds, 7f, bound with DDR1 a Kd value 5.9 nM suppressed kinase activity an half-maximal (50%) inhibitory concentration 14.9 nM. 7f potently inhibited collagen-induced signaling epithelial–mesenchymal transition, dose-dependently colony formation pancreatic cancer cells, exhibited promising in vivo therapeutic...
A series of N-(3-((1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl)benzenesulfonamides were designed as the first class highly selective ZAK inhibitors. The representative compound 3h strongly inhibits kinase activity with an IC50 3.3 nM and dose-dependently suppresses activation downstream signals in vitro vivo, while it is significantly less potent for majority 403 nonmutated kinases evaluated. Compound also exhibits orally therapeutic effects on cardiac hypertrophy a spontaneous hypertensive rat model.
Inhibition of nicotinamide phosphoribosyltransferase (NAMPT) has the potential to directly limit NAD production in cancer cells and is an effective strategy for treatment. Using a structure-based strategy, we have designed new class potent small-molecule inhibitors NAMPT. Several compounds showed promising antiproliferative activities vitro. (E)-N-(5-((4-(((2-(1H-Indol-3-yl)ethyl)(isopropyl)amino)methyl)phenyl)amino)pentyl)-3-(pyridin-3-yl)acrylamide, 30, bearing indole moiety, IC50 25.3 nM...