abstract |
The invention provides helquat derivatives of general formula I, wherein substituents R 1 and R 2 are independently selected from a group comprising H and C 1 to C 4 alkyl, up to three of S 1,2 , S 1',2' , S 3,4 and S 3',4' are present, each of S 1,2 , S 1',2' , S 3,4 and S 3',4' independently represents a linker consisting of a bivalent hydrocarbon chain having 3-6 carbon atoms, preferably hydrocarbon chain having 4 carbon atoms, more preferably hydrocarbon chain having 4 carbon atoms and two double bonds, and one to four atoms selected from the carbon atoms with the descriptor 2, 4, 2', and 4' are substituted with a substituent R 3 of general formula II, wherein R 4 is substituted or unsubstituted heteroaryl, T 1 and T 2 are independent linkers that bridge atoms N 5 with C 8 and N 5´ with C 8´ , wherein T 1 and T 2 independently represent a bivalent hydrocarbon chain having 2-5 carbon atoms, preferably 2 or 3 carbon atoms; and anions (X 1 ) - and (X 2 ) - independently represent anions of pharmaceutically acceptable salts. The helquat derivatives are useful as medicaments in the treatment of diseases related to increased cellular proliferation, such as oncologic diseases and in the treatment, requiring affecting of G-quadruplex, preferably at telomeres or in gene promoters. ˙ |