摘要 |
A compound which is a benzo[a]phenazine-11-carboxamide derivative of formula (I) wherein each of R<SP>1</SP> to R<SP>4</SP>, which are the same or different, is selected from hydrogen, halogen, hydroxyl, C<SB>1</SB>-C<SB>6</SB> alkoxy which is unsubstituted or substituted, heteroaryloxy, C<SB>1</SB>-C<SB>6</SB> alkyl which is unsubstituted or substituted, nitro, cyano, azido, amidoxime, CO<SB>2</SB>R<SP>10</SP>, CON(R<SP>12</SP>)<SB>2</SB>, OCON(R<SP>12</SP>), SR<SP>10</SP>, SOR<SP>11</SP>, SO<SB>2</SB>(R<SB>11</SB>), SO<SB>2</SB>N(R<SP>12</SP>)<SB>2</SB>, N(R<SP>12</SP>)<SB>2</SB>, NR<SP>10</SP>SO<SB>2</SB>R<SP>11</SP>, N(SO<SB>2</SB>R<SP>11</SP>)<SB>2</SB>, NR<SP>10</SP>(CH<SB>2</SB>)<SB>n</SB>CN, NR<SP>10</SP>COR<SP>11</SP>, OCOR<SP>11</SP> or COR<SP>10</SP>; each of R<SP>5</SP> to R<SP>7</SP>, which are the same or different, is selected from hydrogen, halogen, hydroxy, C<SB>1</SB>-C<SB>6</SB> alkoxy, C<SB>1</SB>-C<SB>6</SB> alkyl, SR<SP>10</SP> and N(R<SP>12</SP>)<SB>2</SB>; Q is C<SB>1</SB>-C<SB>6</SB> alkylene which is unsubstituted or substituted by (i) C<SB>1</SB>-C<SB>6</SB> alkyl which is unsubstituted or substituted, (ii) hydroxy, provided that the hydroxy group is not a to either of the N atoms adjacent to Q in formula (I), (iii) CO<SB>2</SB>R<SP>10</SP>, or (iv) CON(R<SP>12</SP>); R<SP>8</SP> and R<SP>9</SP>, which are the same or different, are each hydrogen or C<SB>1</SB>-C<SB>6</SB> alkyl, or R<SP>8</SP> and R<SP>9</SP> 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<SP>8</SP> and R<SP>9</SP> 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<SP>1</SP> to R<SP>4</SP> 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. |