Abstract: Novel indolyl-2-phenyl bisamidines are described which are DNA methyltransferase inhibiting agents, and pharmaceutical compositions containing them are used as antiproliferative agents for treating a disease, especially a neoplastic disease, characterized by abnormally rapid proliferation of tissue involved in said disease; said indolyl-2-phenyl bisamidines comprising a and a pharmaceutically acceptable salt thereof, wherein: R1 is hydrogen or (C1-C3)alkyl; R3, R4, R5, R8, R9, and R10 are hydrogen or (C1-C3)alkyl, or R3 and R4 may be taken together, or R8 and R9 may be taken together with the nitrogen atoms to which they are attached, to form an imidazolinyl group; R14 is —H; —NHC(═O)(CH2)mR20; —(CH2)mR20; —CH(CH3)R20; —(CH2)m(C6H3)—R17; —(CH2)m(C6H3)—R20; —(CH2)m(heterocyclyl)—R17; —(CH2)m(heterocyclyl)—R20; —CH2CH═CHR20; —(CH2)mC(═O)NH—CHR20R21; or —(CH2)mC(═O)NH—CH2&m

Abstract: Known bisamidine compounds are newly discovered to possess DNA methyltransferase inhibiting properties, making them useful for preparing pharmaceutical compositions useful as antiproliferative agents for treating a neoplastic or a non-neoplastic disease characterized by abnormally rapid proliferation of tissue involved in said disease; wherein said bisamidines comprise a compound of Formula (5.0.0): and a pharmaceutically acceptable salt thereof, wherein: —X is —C(R34)—; or —N—; —R23, R24, R28 and R29 are each independently —H; or —CH2— where R23 and R24 and R28 and R29 are taken together with the nitrogen atoms to which they are attached, to form an imidazolinyl group; and —R34 is —H; or —CH3. A preferred species of Formula (5.0.0) is the following: 2-(4-Carbamimidoyl-phenyl)-1H-indole-6-carboxamidine.