Synthesis and anti-tumor evaluation of new trisulfide derivatives

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...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2006-09, Vol.16 (18), p.4826-4829
Hauptverfasser: An, Haoyun, Zhu, Jenny, Wang, Xiaobo, Xu, Xiao
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Sprache:eng
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Zusammenfassung: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. 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2006.06.070