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Updated: Jul 7, 2026

Optimizing Tubulin Yield from Porcine Brain Tissue
Published on: October 11, 2024
Combretastatin dinitrogen-substituted stilbene analogues as tubulin-binding and vascular-disrupting agents
Rogelio Siles1, J Freeland Ackley, Mallinath B Hadimani
1Department of Chemistry and Biochemistry, Baylor University, Waco, TX 76798-7348, USA.
Abstract:
Several stilbenoid compounds having structural similarity to the combretastatin group of natural products and characterized by the incorporation of two nitrogen-bearing groups (amine, nitro, serinamide) have been prepared by chemical synthesis and evaluated in terms of biochemical and biological activity. The 2',3'-diamino B-ring analogue 17 demonstrated remarkable cytotoxicity against selected human cancer cell lines in vitro (average GI 50 = 13.9 nM) and also showed good activity in regard to inhibition of tubulin assembly (IC 50 = 2.8 microM). In addition, a single dose (10 mg/kg) of compound 17 caused a 40% tumor-selective blood flow shutdown in tumor-bearing SCID mice at 24 h, thus suggesting the potential value of this compound and its corresponding salt formulations as new vascular-disrupting agents.
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