Site specific alkylating agents

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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548518, A61K 3140, C07D40312

Patent

active

050495798

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.

REFERENCES:
patent: 4738980 (1988-04-01), Arcamone et al.
Arcamone, F., "On Distamycin and Related Compounds, Selective Antiviral Agents" Med. Chem. 1972, pp. 29-45.
Arcamone, F. et al., "Structure and Synthesis of Distamycin A" Nature, Sep. 5, 1964 vol. 203, pp. 1064-1065.
Arcamone, F. et al., Gazzetta Chimica Italiana, vol. 97, pp. 1097-1109. (1967).
Arcamone F. et al., Gazzetta Chimica Italiana, vol. XCIX 1969, pp. 632-640.
Bialer, M. et al., "Structure-Activity Relationship . . . " Jour. of Med. Chem., 1979, vol. 22, No. 11, pp. 1296-1301.
Chandra, P. et al., "Some Structural Requirements for the Antibiotic . . . " FEBS Letters, vol. 16, No. 4, Sep., 1971, pp. 249-252.

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