Analogues of penclomedine (PEN, 3, 5-dichloro-4, 6-dimethoxy-2-(trichloromethyl) pyridine) and its metabolites have been synthesized and evaluated as potential antitumor agents. PEN and 4-DMPEN (3, 5-dichloro-4-hydroxy-6-methoxy2-(trichloromethyl) pyridine (3a)), the major plasma metabolite in patients, were modified at 4-and 6-positions with different alkyl, aryl, and ester groups. All of the analogues and many of the intermediates were evaluated ...
