Cytotoxic macrolides and methods of use
AssigneeHarbor Branch Oceanographic Institution, Inc.
InventorsPaul A. Horton, Frank Koehn, Ross E. Longley, Oliver J. McConnell, Shirley A. Pomponi
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Abstract
A novel macrolide compound, lasonolide A, has been isolated from a marine sponge. This compound, derivatives of the compound, and compositions comprising the compound or its derivatives, are useful as antitumor agents and as biochemical tools.
Claims6
A substantially pure macrolide compound having the formula:
- ##STR11## wherein R.sub.1 =O, or H and OH, or H and OR, where
- R is H, acyl, alkyl, or phenyl;
- and
- R.sub.2 =alkyl, H, CH.sub.2 OH, CH.sub.2 OR, CHO, COOH, COOR', or COO.sup.- X.sup.+, where
- X=H, Na, K, amines, or other monovalent cationic molecule;
- R=acyl, alkyl, or phenyl;
- and R'=alkyl or phenyl.
A pharmaceutical composition for the inhibition of tumor cell growth comprising a compound having the formula:
- ##STR12## wherein R.sub.1 =O, or H and OH, or H and OR, where
- R is H, acyl, alkyl, or phenyl;
- and
- R.sub.2 =alkyl, H, CH.sub.2 OH, CH.sub.2 OR, CHO, COOH, COOR', or COO.sup.- X.sup.+, where
- X=H, Na, K, amines, or other monovalent carbonic molecule;
- R=acyl, alkyl, or phenyl;
- and R'=alkyl or phenyl;
- and a pharmaceutically acceptable carrier.
A process for treating a human or animal hosting tumor cells, said process comprising administering to said human or animal a tumor cell-inhibiting amount of a macrolide compound having the formula:
- ##STR13## wherein R.sub.1 =O, or H and OH, or H and OR, where
- R is H, acyl, alkyl, or phenyl;
- and
- R.sub.2 =alkyl, H, CH.sub.2 OH, CH.sub.2 OR, CHO, COOH, COOR', or COO.sup.- X.sup.+, where
- X=H, Na, K, amines, or other monovalent cationic molecule;
- R=acyl, alkyl, or phenyl;
- and R'=alkyl or phenyl.
Dependencies are inferred from the claim text.