Synthesis and anti-tumor evaluation of new trisulfide derivatives
Haoyun An1, Jenny Zhu, Xiaobo Wang
1ACEA Biosciences, Inc., 11585 Sorrento Valley Road, Suite 103, San Diego, CA 92121, USA. han@aceabio.com
Bioorganic & Medicinal Chemistry Letters
|July 11, 2006
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.


