PUBLICATION

Synthesis and evaluation of 3-amino/guanidine substituted phenyl oxazoles as a novel class of LSD1 inhibitors with anti-proliferative properties

Authors
Dulla, B., Kirla, K.T., Rathore, V., Deora, G.S., Kavela, S., Maddika, S., Chatti, K., Reiser, O., Iqbal, J., and Pal, M.
ID
ZDB-PUB-130418-17
Date
2013
Source
Organic & biomolecular chemistry   11(19): 3103-7 (Journal)
Registered Authors
Chatti, Kiranam, Kirla, Krishna Tulasi
Keywords
none
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
PubMed
23575971 Full text @ Org. Biomol. Chem.
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.

Genes / Markers
Figures
Expression
Phenotype
Mutations / Transgenics
Human Disease / Model
Sequence Targeting Reagents
Fish
Antibodies
Orthology
Engineered Foreign Genes
Mapping