| abstract |
THE PRESENT INVENTION RELATES TO WATER SOLUBLE, CAMPTOTHECIN DERIVATIVES OF FORMILA (I).WHEREIN A REPRESENTS A MOIETY OF THE FORMULA (IIA), (IIB) OR (IICX IS SELECTED FROM THE GROUP CONSISTING OF ALKYL, ARYL, (CH2)MOR1, (CH2)MSR1 AND (CH2)MNR1R2 WHEREIN M IS AN INTEGER OF 0 TO 6, AND R1 AND R2 ARE HYDROGEN, LOWER ALKYL, ARYL OR TOGETHER WITH THE NITROGEN FORM A 5-7 MEMBERED RING; Q IS AN INTEGER OF 0 TO 2; N REPRESENTS THE INTEGER 1 OR 2; P IS AN INTEGER OF 1 TO 6; Y AND W ARE SELECTED FROM THE GROUP CONSISTING OF ALKYL, ARYL, ALKOXY, ARYLOXY AND AMINO, Q IS OXYGEN OR SULFUR; P IS PHOSPHORUS; J REPRESENTS THE ATOMS NECESSARY TO COMPLETE A 5 OR 6 MEMBERED AROMATIC RING; AND THE PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF; THEIR USE AS TOPOISOMERASE INHIBITORS, THEIR PREPARATION; AND THEIR USE IN THE TREATMENT OF CANCER. |