2494. Combretastatins
Description and references
A group of compounds isolated from the bark and stem wood of the South African bushwillow tree, Combretum caffrum, which inhibit tubulin polmerization. The most active are combretastatins A-2 and A-4. Used in folk medicine, extracts have shown antileukemic properties. Isoln: G. R. Pettit et al., Can. J. Chem. 60, 1374 (1982); of A-2: G. R. Pettit, S. B. Singh, ibid. 65, 2390 (1987); of A-4: idem et al., Experientia 45, 209 (1989). Enantioselective synthesis: A. Ramacciotti et al., Tetrahedron: Asymmetry 7, 1101 (1996). Mechanism of action study: C. M. Lin et al., Biochemistry 28, 6984 (1989). Antineoplastic activity of A-4: A. A. E. El-Zayat et al., Anti-Cancer Drugs 4, 19 (1993); inhibition of tumor vascularization: G. G. Dark et al., Cancer Res. 57, 1829 (1997). Review of structure-activity of combretastatins, podophyllotoxin, q.v. and steganacin: D. L. Sackett, Pharmacol. Ther. 59, 163-228 (1993).
