2. Academic Validation
  3. Design, synthesis, and biological evaluation of novel coxsackievirus B3 inhibitors

Design, synthesis, and biological evaluation of novel coxsackievirus B3 inhibitors

  • Bioorg Med Chem. 2010 Jun 15;18(12):4374-84. doi: 10.1016/j.bmc.2010.04.081.
Michal Sála 1,  Armando M De Palma,  Hubert Hrebabecký,  Radim Nencka,  Martin Dracínský,  Pieter Leyssen,  Johan Neyts,  Antonín Holý
Affiliations

Affiliation

  • 1 Gilead Sciences & IOCB Research Centre, Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, Prague, Czech Republic.
PMID: 20576576 DOI: 10.1016/j.bmc.2010.04.081
Abstract

The synthesis and SAR study of a novel class of coxsackievirus B3 (CVB3) inhibitors are reported. These compounds could be considered as the 6-chloropurines substituted at position 9 with variously substituted bicyclic scaffolds (bicyclo[2.2.1]heptane/ene-norbornane or norbornene). The synthesis and biological evaluation of 31 target compounds are described. Several of the analogues inhibited CVB3 in the low micromolar range (0.66-2muM). Minimal or no cytotoxicity was observed.

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