Synthesis and in vitro antitumor activity of some tetraphenylantimony derivatives of exo-7-oxa-bicyclo[2,2,1]heptane(ene)-3-arylamide-2-acid

A series of novel tetraphenylantimony derivatives of exo-7-oxa-bicyclo[2,2,1] heptane (ene)-3 -arylamide-2-acid of the general formula Ph₄SbO₂CCHCHCH₂CH₂CH(O)CHCONHAr (Ar = Ph,4-ClC₆H₄, 4-BrC₆H₄, 3-BrC₆H₄, 4-F-3-ClC₆H₃ and 4-MeC₆H₄) have been synthesized and characterized by elemental analysis, IR, ¹H NMR and mass spectra. The crystal structure of Ph₄SbO₂CCHCHCH₂CH₂ CH(O)CHCONHC₆H₄CH₃·CHCl₃ was determined by X-ray diffraction. Five human neoplastic cell lines (HL-60, KB, Bel-7402, BGC-823 and HCT-8) were used to screen these compounds. The results indicate that these compounds at 10 μM show certain in vitro antitumor activities.