Acryloyl derivatives analogous to distamycin, process for preparing them, and their use as antitumor agents
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United States of America Patent
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Jun 22, 2004
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N/A
app pub date -
Sep 19, 2000
filing date -
Mar 27, 1998
priority date (Note) -
Expired
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Abstract
Compounds which are acryloyl substituted distamycin derivatives of formula (I) wherein: n is 2, 3 or 4; m is 1 or 2; X and Y are the same or different and are selected, independently for each heterocyclic ring of the polyetherocyclic chain, from N and CH; R.sub.1 and R.sub.2, which are the same or different, are selected from hydrogen, halogen, and C.sub.1 -C.sub.4 alkyl; R.sub.3 is hydrogen or halogen; B is selected from (a), (b), (c), (d), (e), (f), (g) and --C.ident.N; wherein R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.10, R.sub.11, and R.sub.12 are, independently from each other, hydrogen or C.sub.1 -C.sub.4 alkyl; and R.sub.9 is hydrogen or hydroxy, or pharmaceutically acceptable salt thereof; provided that a) at least one of R.sub.4, R.sub.5 and R.sub.6 is alkyl b) at least one of the heterocyclic rings within the polyheterocyclic chain is other than pyrole; and c) X and Y are not both N for the same heterocyclic ring; are useful as antitumor agents.
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