Abstract
A series of functionalized phenyl oxazole derivatives was designed, synthesized and screened in vitro for their activities against LSD1 and for effects on viability of cervical and breast cancer cells, and in vivo for effects using zebrafish embryos. These compounds are likely to act via multiple epigenetic mechanisms specific to cancer cells including LSD1 inhibition.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Animals
-
Antineoplastic Agents / chemical synthesis
-
Antineoplastic Agents / chemistry
-
Antineoplastic Agents / pharmacology*
-
Apoptosis / drug effects
-
Cell Line, Tumor
-
Cell Proliferation / drug effects
-
Cell Survival / drug effects
-
Dose-Response Relationship, Drug
-
Drug Screening Assays, Antitumor
-
Enzyme Inhibitors / chemical synthesis
-
Enzyme Inhibitors / chemistry
-
Enzyme Inhibitors / pharmacology*
-
Guanidine / chemistry*
-
Histone Demethylases / antagonists & inhibitors*
-
Histone Demethylases / metabolism
-
Humans
-
Molecular Dynamics Simulation
-
Molecular Structure
-
Oxazoles / chemical synthesis
-
Oxazoles / chemistry
-
Oxazoles / pharmacology*
-
Structure-Activity Relationship
-
Zebrafish
Substances
-
Antineoplastic Agents
-
Enzyme Inhibitors
-
Oxazoles
-
Histone Demethylases
-
KDM1A protein, human
-
Guanidine