Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1994-12-01
1997-04-22
Daus, Donald G.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
546 43, 546108, 546 75, 546 14, A61K 3147
Patent
active
056229585
ABSTRACT:
A quinone imine enediyne possessing cytotoxic activity towards cancer cells having the general structure: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are independently the same or different and are H, Br, Cl, F, NH.sub.2, CO.sub.2 H, or OH or a linear or branched alkyl, etc.; wherein R.sub.4 is H, OH or a linear or branched alkoxy, linear or branched alkoxycarbonyl, etc.; wherein R.sub.5 is H, Br, Cl, F, O.dbd., OH or S--SR, or a linear or branched alkyl, etc.; wherein R.sub.6 is H, Br, Cl, F, CO.sub.2 H, OH or S--SR', or a linear or branched alkyl, etc; wherein R.sub.7 is H, OH or S--SR", or a linear or branched alkyl, linear or branched alkoxycarbonyl, linear or branched alkoxy or linear or branched hydroxyalkyl group; and wherein R, R' and R" are independently the same or different and are a linear or branched alkyl, linear or branched acyl or linear or branched alkoxyalkyl group. Also provided are conjugates of the compound with cleavable peptides and carbohydrates, monoclonal antibodies immunoreactive with cancer cells, compositions comprising the analogues and conjugates, methods of treating tumors and a method of preparing the analogues.
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Chou T.-C.
Danishefsky Samuel J.
Shair Matthew D.
Yoon Taeyoung
Daus Donald G.
Sloan-Kettering Institute for Cancer Research
White John P.
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