2. Academic Validation
  3. Discovery and structure-activity relationships of (2-(arylthio)benzylideneamino)guanidines as a novel series of potent apoptosis inducers

Discovery and structure-activity relationships of (2-(arylthio)benzylideneamino)guanidines as a novel series of potent apoptosis inducers

  • Bioorg Med Chem. 2009 Apr 1;17(7):2852-8. doi: 10.1016/j.bmc.2009.02.029.
Han-Zhong Zhang 1,  Candace Crogan-Grundy,  Chris May,  John Drewe,  Ben Tseng,  Sui Xiong Cai
Affiliations

Affiliation

  • 1 EpiCept Corporation, 6650 Nancy Ridge Drive, San Diego, CA 92121, USA.
PMID: 19282188 DOI: 10.1016/j.bmc.2009.02.029
Abstract

1-(2-(2,5-Dimethoxyphenylthio)benzylidene)semicarbazide (2a) was discovered as a potent Apoptosis Inducer through our cell based HTS assay. SAR study led to the discovery of a more aqueous soluble analog (2-(2,5-dimethoxyphenylthio)-6-methoxybenzylideneamino)guanidine (5e) with EC(50) value of 60 nM in the Caspase activation assay and GI(50) value of 62 nM in the growth inhibition assay in T47D cells. Compound 5e was found to be an inhibitor of tubulin polymerization and efficacious in a MX-1 breast tumor model.

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