Synthesis and antimetastatic activity of 6-trichloroacetamido and 6-guanidino analogues of siastatin B.
نویسندگان
چکیده
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,
منابع مشابه
Effect on spontaneous metastasis of mouse Lewis lung carcinoma by a trifluoroacetamide analogue of siastatin B.
As reported in our previous paperslf2), (3R,4R, 5#,6#)-6-(trifluoroacetamido)-3,4,5-trihydroxypiperidine-3-carboxylic acid (tentatively named SF 1 ) and (35,4S',5K,6^)-6-(trifluoroacetamido)-4, 5-dihydroxypiperidine-3-carboxylic acid (SF4) which were synthesized as trifluoroacetamide analogues of siastatin B3) (Fig. 1), were highly inhibitory against /?-glucuronidase (EC 3.2.1.31) from bovine l...
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عنوان ژورنال:
- The Journal of antibiotics
دوره 49 3 شماره
صفحات -
تاریخ انتشار 1996