As shown in Table 1, most of thiourea a-aminophosphonate
derivatives 4e5 displayed much higher inhibitory activity than
DHA against the NCI-H460, A549, HepG2 and SKOV3 cell lines,
indicating the introduction of thiourea a-aminophosphonate on
DHA should markedly improve the antitumor activity. Moreover,
the substituents in benzene of compound 4 have important influence
on the cytotoxic inhibition and the introduction of electron
donor substituents and halogen groups may result in the
decrease of cytotoxic inhibition, while substituent groups in
benzene of compound 5 also have important effect on the cytotoxic
inhibition and the introduction of electron donor substituents
and halogen groups may lead to the enhancement of
cytotoxic inhibition.