Synthesis and anti-tumor evaluation of new trisulfide derivatives
- Bioorg Med Chem Lett. 2006 Sep 15;16(18):4826-9. doi: 10.1016/j.bmcl.2006.06.070.
Affiliations
- 1. ACEA Biosciences, Inc., 11585 Sorrento Valley Road, Suite 103, San Diego, CA 92121, USA. [email protected]
PMID: 16828553
DOI: 10.1016/j.bmcl.2006.06.070
Abstract
New bis-aromatic and heterocyclic trisulfide derivatives 5, 7-10 were synthesized by optimizing lead dibenzyl trisulfide natural product (4) to evaluate their anti-tumor activities. Five compounds 5-7, 9, and 10 exhibited potent anti-tumor activities against eight different tumor cell lines with low cytotoxicity against HepG2. Initial SAR was discussed, and MOA of these anti-microtubule agents was suggested based on cell kinetic response patterns observed on RT-CES system.