Synthesis and antitumor activity of several new analogues of penclomedine and its metabolites

A Tiwari, JM Riordan, WR Waud…

Index: Tiwari, Anita; Riordan, James M.; Waud, William R.; Struck, Robert F. Journal of Medicinal Chemistry, 2002 , vol. 45, # 5 p. 1079 - 1085

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Citation Number: 4

Abstract

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 ...