Alkyl camptothecin compounds as potent inhibitors of human colorectal cancer
AssigneeResearch Triangle Institute
InventorsMonroe E. Wall, Mansukh C. Wani, Allan W. Nicholas, Govindarajan Manikumar
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Abstract
A method for synthesizing camptothecin and camptothecin analogs using a novel hydroxyl-containing tricyclic intermediate and the camptothecin analogs produced by the process. The camptothecin analogs are effective inhibitors of topoisomerase. I and show antileukemic and anti-tumor activity.
Claims11
An alkyl camptothecin having the structure shown below ##STR10## wherein R.sup.1 is hydroxy, nitro, amino, chloro, bromo, iodo, fluoro, C.sub.1-8 alkyl, C.sub.1-8 alkoxy, trifluoromethyl, aminomethyl, amido, hydrazino, azido, formyl, cyano or an amino acid bonded to the aromatic ring through the amino-nitrogen atom of said amino acid;
- and
- R.sup.2 is C.sub.1-8 alkyl.
Dependencies are inferred from the claim text.