PUBLICATION

NaSH in the construction of thiophene ring fused with N-heterocycles: A rapid and inexpensive synthesis of novel small molecules as potential inducers of apoptosis

Authors
Kolli, S.K., Nakhi, A., Medishetti, R., Yellanki, S., Kulkarni, P., Ramesh Raju, R., Pal, M.
ID
ZDB-PUB-140830-8
Date
2014
Source
Bioorganic & medicinal chemistry letters   24(18): 4460-5 (Journal)
Registered Authors
Kulkarni, Pushkar
Keywords
Apoptosis, Pyrazine, Quinoxaline, Thiophene
MeSH Terms
  • Animals
  • Apoptosis/drug effects*
  • Crystallography, X-Ray
  • Dose-Response Relationship, Drug
  • Heterocyclic Compounds/chemistry*
  • Models, Molecular
  • Molecular Structure
  • Small Molecule Libraries/chemical synthesis
  • Small Molecule Libraries/chemistry
  • Small Molecule Libraries/pharmacology*
  • Structure-Activity Relationship
  • Sulfides/chemistry*
  • Thiophenes/chemical synthesis
  • Thiophenes/chemistry
  • Thiophenes/pharmacology*
  • Zebrafish/embryology
PubMed
25168747 Full text @ Bioorg. Med. Chem. Lett.
Abstract
A facile construction of a thiophene ring fused with N-heterocycles has been achieved via the reaction of NaSH with 2-chloro-3-alkynyl quinoxalines/pyrazines leading to novel 2-substituted thieno[2,3-b]pyrazine/quinoxaline derivatives as potential inducers of apoptosis. Some of them showed encouraging pharmacological properties when tested in zebrafish.
Genes / Markers
Figures
Expression
Phenotype
Mutations / Transgenics
Human Disease / Model
Sequence Targeting Reagents
Fish
Antibodies
Orthology
Engineered Foreign Genes
Mapping