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‐bicyclo2,2,1] heptane (ene)‐3‐arylamide‐2‐acid of the general formula Ph₄SbO₂CCHCHCH₂CH₂CH(O)HCONHAr (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 Ph₄SbO₂CCHCHCH₂CH₂CH(O)HCONHC₆­H₄CH₃·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. Copyright © 2001 John Wiley & Sons, Ltd.