Methyltransferase inhibitors for treating cancer

摘要

Compounds having methyltransferase inhibitory activity are disclosed. The compounds have the structure;
and are useful in the treatment of cancer and similar diseases associated with inappropriate methyltransferase activity.

主权项

1. A compound of formula I or II wherein: X1 is N or CH; Q is NH or 0; A is chosen from direct bond, (C1-C20)hydrocarbon, (C1-C20)oxaalkyl and (C1-C20)azaalkyl; R1 is chosen from —C(═NH)NH2, —C(═NH)NH(C1-C10)hydrocarbon, fluoro(C1-C6)hydrocarbon, and —CH(NH2)COOH, with the provisos that,
(1) when A is a direct bond, R1 cannot be H;(2) when QR3 is OH, R1 cannot be fluoro(C2-C6)hydrocarbon; or the combination R1A is chosen from ethyl, propyl, isopropyl, butyl, s-butyl, t-butyl, cyclic hydrocarbon groups of from 3 to 8 carbon atoms, benzyl, phenethyl, cyclohexylmethyl, adamantyl, camphoryl and naphthylethyl; R2 is chosen from hydrogen, —C(═NH)NH2, —C(═NH)NH(C1-C10)hydrocarbon and —CH(NH2)COOH; R3 is chosen from H and (C1-C20) hydrocarbon; and n is 1 or 2.