Site specific alkylating agents
AssigneeFarmitalia Carlo Erba S.p.A.
InventorsEttore Lazzari, Federico Arcamone, Sergio Penco, Maria A. Verini, Nicola Mongelli
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Abstract
The invention relates to distamycin A analogs of the following formula ##STR1## wherein n is 2, 3 or 4; A is an optionally substituted divalent radical chosen from ##STR2## and --Het-- wherein Het is a pentatomic or hexatomic heteromonocyclic ring, except pyrrole; and wherein either one of R.sub.1 and R.sub.2 is hydrogen and the other is an acylating moiety or R.sub.1 and R.sub.2 are both hydrogen or both alkyl groups optionally substituted, including the pharmaceutically acceptable salts of the said compounds. The compounds of the invention can be useful antitumor and antiviral agents.
Claims6
A compound of formula (I) ##STR19## wherein n is 2, 3, or 4;
- A is a divalent carbocyclic radical selected from the group consisting of ##STR20## wherein the radical is unsubstituted or substituted by one or more substituents selected from the group consisting of C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, cyano, and trifluoromethyl;
- and either one of R.sub.1 and R.sub.2 is a hydrogen and the other is
- a) a group ##STR21## in which R.sub.3 is a C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by halogen atoms;
- phenyl;
- or cyclohexyl;
- or
- b) a group --CO--(CH.sub.2).sub.m --R.sub.4 in which m is zero, 1, 2, or 3 and R.sub.4 is hydrogen, halogen. hydroxy, aziridinyl, or oxiranyl;
- or R.sub.1 and R.sub.2 are the same and they are both hydrogen or both a C.sub.1 -C.sub.6 alkyl group unsubstituted or substituted by halogen, hydroxy, or C.sub.1 -C.sub.6 alkoxy, provided however, that when R.sub.1 and R.sub.2 are both chloroethyl and A is ##STR22## then n is 2 or 4, and the pharmaceutically acceptable salts thereof.
A compound selected from the group consisting of:
- .beta.-[1-methyl-4-[1-methyl-4-[1-methyl-4-[4-(N'-methyl-N'-nitrosoureido-b enzene)-1-carboxamido]pyrrole-2-carboxamido]pyrrole-2-carboxamido]pyrrole-2 -carboxamido]propionamidine;
- .beta.-[1-methyl-4-[1-methyl-4-[1-methyl-4-[4-N'-(2-chloroethyl)-N'-nitros oureido-benzene)-1-carboxamido]pyrrole-2-carboxamido]pyrrole-2-carboxamido] pyrrole-2-carboxamido]propionamidine;
- and
- .beta.-[1-methyl-4-[1-methyl-4-[1-methyl-4-[3-N,N-bis(2-chloroethyl)amino-b enzene-1-carboxamido]pyrrole-2-carboxamido]pyrrole-2-carboxamido]pyrrole-2- carboxamido]propionamidine, as hydrochloric acid salt.
Dependencies are inferred from the claim text.