Twelve Mannich base derivatives of 2'-hydroxychalcone were synthesized through Mannich reaction, and the regioselectivity of the reaction occurred preferentially at C-3' position of B ring of chalcone backbone. All the target compounds have been identified by ¹H NMR, IR spectra and elemental analyses, and further confirmed by X-ray analysis. The characteristic of this reaction was simple process, mild condi-tion, easy purification and middle to good yields (49%～72%). Some compounds showed potent CDK1/cyclin B inhibitory activities and most of compounds displayed a significant growth inhibitory action against various cancer cell lines.

Key words: Mannich reaction, growth inhibitory activity, Mannich base, CDK1/cyclin B inhibitory activity, 2'-hydroxychalcone