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Abstract

A compound which is a benzo[a]phenazine-11-carboxamide derivative of formula (I) wherein each of R.sup.1 to R.sup.4, which are the same or different, is selected from hydrogen, halogen, hydroxyl, C.sub.1-C.sub.6 alkoxy which is unsubstituted or substituted, heteroaryloxy, C.sub.1-C.sub.6 alkyl which is unsubstituted or substituted, nitro, cyano, azido, amidoxime, CO.sub.2R.sup.10, CON(R.sup.12).sub.2, OCON(R.sup.12), SR.sup.10, SOR.sup.11, SO.sub.2(R.sup.11), SO.sub.2N(R.sup.12).sub.2, N(R.sup.12).sub.2, NR.sup.10SO.sub.2R.sup.11, N(SO.sub.2R.sup.11).sub.2NR.sup.10(CH.sub.2).sub.nCN, NR.sup.10COR.sup.11, OCOR.sup.11 or COR.sup.10; each of R.sup.5 to R.sup.7, which are the same or different, is selected from hydrogen, halogen, hydroxy, C.sub.1-C.sub.6 alkoxy, C.sub.1-C.sub.6 alkyl, SR.sup.10 and N(R.sup.12).sub.2; Q is C.sub.1-C.sub.6 alkylene which is unsubstituted or substituted by (i) C.sub.1-C.sub.6 alkyl which is unsubstituted or substituted, (ii) hydroxy, provided that the hydroxy group is not, to either of the N atoms adjacent to Q in formula (I), (iii) CO.sub.2R.sup.10, or (iv) CON(R.sup.12); R.sup.1 and R.sup.9, which are the same or different, are each hydrogen or C.sub.1-C.sub.6 alkyl, or R.sup.8 and R.sup.9 together with the nitrogen atom to which they are attached form a saturated 5- or 6-membered N-containing heterocyclic ring which may include one additional heteroatom selected from O, N and S, or one of R.sup.8 and R.sup.9 is an alkylene chain optionally interrupted by O, N or S, which is attached to a carbon atom on the alkylene chain represented by Q to complete a saturated 5- or 6-membered N-containing heterocyclic ring as defined above; or a pharmaceutically acceptable salt thereof; with the proviso that at least one R.sup.1 to R.sup.4 is other than hydrogen. These compounds are inhibitors of topoisomerase I and/or topoisomerase II and can be used to treat tumours, including tumours which express MDR.

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First Claim