Synthesis and Antimetastatic Activity of 6-Trichloroacetamido and 6-Guanidino Analogues of Siastatin B.

Abstract

Current studies1 ~5) have provided considerable evidence of increase of /?-glucuronidase activity in human tumors and suggested that /?-glucuronidase plays a key role in degradation of basement membranes during metastasis of the tumor cells, and showed that pglucuronidase inhibitors inhibit tumor-cell metastasis. In the course of our studies6~16) of new drugs for tumor metastasis based on siastatin B (1),17) we showed that synthetic (35' ,45' , 5^,6^)-6-(trifluoroacetamido)-4,5dihydroxypiperidine-3-carboxylic acid (2) and (3R,4R,