| abstract |
Indole compounds of the formula:n nwherein L 1 is CO; L 2 is a bond; R 1 is aryl ornheteroaryl; R 2 is H, aryl, heteroaryl, halogen, nitro, nitroso,ncyano, azide, isothionitro, OR, OC(O)R, OC(O)OR, OC(O)NRR', SO 2 R,nSO 3 R, SO 2 NRR', SR, NRR', NRSO 2 NR'R'',nNRSO 2 R', NRSO 3 R', NRC(O)R', NRC(O)NR'R'', NRC(C)OR',nNRC(N)NR'R'', C(O)OR, C(O)NRR', an amino acid moiety, a polypeptidenmoiety, a carbohydrate moiety, or a PEG moiety; each of R a ,nR b , R c , and R d , independently, is R, halogen,nnitro, nitroso, cyano, azide, isothionitro, OR, OC(O)R, OC(O)OR,nOC(O)NRR', SO 2 R, SO 3 R, SO 2 NRR', SR, NRR',nNRSO 2 NR'R'', NRSO 2 R', NRSO 3 R', NRC(O)R',nNRC(O)NR'R'', NRC(O)OR', NRC(N)NR'R'', C(O)R, C(O)OR, C(O)NRR',nOP(O)(OR)(OR'), O(CH 2 ) n OP(O)(OR)(OR'), ornO(CH 2 ) n -PEG, or R b and R c ,nR a and R b , or R c and R d takenntogether are O(CH 2 ) n O; and R e is H, alkyl,nalkenyl, alkynyl, cyclyl, heterocyclyl, halogen, nitro, nitroso, cyano,nazide, isothionitro, OR, OC(O)R, OC(O)OR, OC(O)NRR', SO 2 R,nSO 3 R, SO 2 NRR', SR, NRR', NRSO 2 NR'R'',nNRSO 2 R', NRSO 3 R', NRC(O)R', NRC(O)NR'R'', NRC(O)OR',nNRC(N)NR'R'', C(O)R, C(O)OR, or C(O)NRR'; in which each of R, R', andnR'', independently, is H, alkyl, alkenyl, alkynyl, aryl, heteroaryl,ncyclyl, or heterocyclyl; and n is 1, 2, 3, 4, or 5, as inhibitors ofntubulin polymerisation useful in the treatment of angiogenesis-relatedndisorders such as cancer. |