Benzoheterocyclic distamycin derivatives, process for preparing them, and their use as antitumor agents
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United States of America Patent
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Oct 1, 2002
Grant Date -
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 benzoheterocyclic distamycin derivatives of formula (I), wherein n is 2, 3 or 4; A is a heteroatom selected from O and S or is a group NR, wherein R is hydrogen or C.sub.1 -C.sub.4 alkyl; B is CH or N; R.sub.1 is hydrogen or C.sub.1 -C.sub.4 alkyl; G is selected from the group consisting of (a, b, c, d, e, f, g, h, i, j), and --C.ident.N; wherein R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10, R.sub.11 and R.sub.12 are, independently from each other, hydrogen or C.sub.1 -C.sub.4 alkyl; T is a group of formula (II) or (III) as defined above, wherein p is 0 or 1; R.sub.2 and R.sub.3 are, independently from each other, hydrogen, C.sub.1 -C.sub.4 alkyl optionally substituted by one or more fluorine atoms, or C.sub.1 -C.sub.4 alkoxy; R.sub.4 is C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.3 haloalkyl; X.sub.1 and X.sub.2 are halogen atoms or pharmaceutically acceptable salts thereof; provided that at least one of R.sub.5, R.sub.6 and R.sub.7 is alkyl; are useful as antitumor agents. ##STR1## ##STR2##
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