Details

Autor(en) / Beteiligte

• Cao, Thai M.
• Durrant, David
• Tripathi, Ashutosh
• Liu, Jihua
• Tsai, Schickwann
• Kellogg, Glen E.
• Simoni, Daniele
• Lee, Ray M.

Titel

Stilbene derivatives that are colchicine site microtubule inhibitors have antileukemic activity and minimal systemic toxicity

Ist Teil von

• American journal of hematology, 2008-05, Vol.83 (5), p.390-397

Ort / Verlag

Hoboken: Wiley Subscription Services, Inc., A Wiley Company

Erscheinungsjahr

2008

Quelle

MEDLINE

Beschreibungen/Notizen

• Stilbenes are a group of natural compounds with many biological activities. Two highly potent stilbenes, cis‐3,4′,5‐trimethoxy‐3′‐aminostilbene (stilbene 5c) and cis‐3,4′,5‐trimethoxy‐3′‐hydroxystilbene (stilbene 6c) induce G2/M cell‐cycle arrest and leukemic cell death in nanomolarity range without affecting normal bone marrow progenitor cells. The mechanism of stilbenes is mediated by interfering with microtubule polymerization through the colchicine‐binding site. Docking of the stilbenes into tubulin structure confirms that stilbenes fit into the colchicine‐binding pocket. Animal studies show that stilbenes are well tolerated in mice and are capable of inducing more than 50% leukemic cell death by a single dose injection. A 5‐day treatment with low‐dose stilbenes suppresses tumor growth in mice with established tumor xenografts. No major organ damage was detected by histological section. Our results indicate that stilbene 5c is a microtubule‐interfering agent and can be potentially useful in leukemic therapy. Am. J. Hematol., 2008. © 2008 Wiley‐Liss, Inc.