Synthesis, Crystal Structure and in vitro Antitumor Activity of Benzyloxyurea and Benzyloxyhydantoin Derivatives

A series of benzyloxyurea and benzyloxyhydantoin derivatives were synthesized by substituting different benzyl groups on O-position and glucosamine, amino acid ester on N3-position of hydroxyurea. Their structures were elucidated by using spectrometry along with X-ray crystal structures analysis and in vitro antitumor activity against the human leukemia cell line K562 and murine leukemia cell line L1210 was evaluated by MTT assay. The L-phenylalanine ester substituent at N3-position was allowed with markedly increasing the activity against the tumor cells. The most promising compounds were 7e and 7b.