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Microtubules represent an attractive target for antitumor drug discovery.Combretastatin A-4 (CA-4),a natural cis-stilbene product, strongly inhibits the tubulin assembly and prevents tubulin polymerization.It also displayed potent cytotoxic activities against a variety of human cancer cell lines.These characters of CA-4 make this natural product an attractive lead compound in the development of new antiumor agents.A series of cis-restricted 3,4-diaryl-5-aminoisoxazoles and 4,5-diaryl-3-aminopyrazoles have been synthesized (Scheme l)and evaluated for their biological activities.