The invention relates to the use of novel chiral N-(1,2,3-triazolmethyl)-3-hydroxy-3-aryloxindoles and N-(1,2,3-triazolmethyl)-isatin derivatives with cytotoxic and antitumor activity.The chiral N-(1,2,3-triazolmethyl)-3-hydroxy-3-aryloxindoles compounds of formula (I) are obtained in an enantiomerically enriched or pure state from precursors of formula (II) via an efficient arylation process using aryl boron reagents and derivatives and a chiral transition-metal based catalyst under mild reaction conditions.The present application describes the application of compounds of formula (I) and (II) as potent inhibitors of certain tumor cell lines.