Synthesis and antitumor activity of cis-dichloroplatinum(II) complexes of 1-(2-aminophenyl)-1,2,3,4-tetrahydroisoquinolines

Abstract: Fifteen cis-dichloroplatinum complexes (5a–5o) were synthesized by treatment of 1-(2-aminophenyl)-1,2,3,4-THIQs (4a–4o) with K2PtCl4. The antitumor activity of these compounds was examined against four different human tumor cell lines. Their structure–activity relationships for antitumor activity are reported. All of these compounds exhibited activity against MCF-7 cell line and showed good activity against WiDr cell line except 5c and 5f. On the other hand, compounds 5j and 5o are more active than the other compounds against Hepa59T/VGH cell line. The electron-donating group at the 6-position of isoquinoline ring seems to decrease the antitumor activity and the chloro substituent at the C-4 position of the aniline ring shown the highest potency. The “trans influence” dominates the control of the stability of [1-(2-aminophenyl)-1,2,3,4-THIQ]dichloroplatinums(II). [Copyright &y& Elsevier]