Ustav Organicke Chemie a Biochemie Av Cr, V.v.i.

Ustav Organicke Chemie a Biochemie Akademie Ved Cr, V.v.i.

Vysoka Skola Chemicko-technologicka V Praze

Miroslav Hajek

Filip Teply

Vishwas Joshi

Erika Kuzmova

Jaroslav Kozak

Veronika Komarkova

Pavla Hubalkova

Paul Eduardo Reyes-Gutierrez

Michael Jirasek

Manoj R Sonawane

Lukas Severa

Jana Novotna

Monoj R Sonawane

Helquat derivatives of general formula I, in which substituents Rand Rare independently selected from a group comprising H and Cto Calkyl, up to three of S, S, Sand Sare present, each of S, S, Sand Sindependently represents a linker consisting of a bivalent hydrocarbon chain having 3-6 carbon atoms, preferably hydrocarbon chain having 4 carbon atoms, and one to four atoms selected from the carbon atoms with the descriptor 2, 4, 2', and 4&#x2032; are substituted with a substituent Rof general formula II, wherein Ris substituted or unsubstituted heteroaryl, Tand Tare independent linkers that bridge atoms Nwith Cand Nwith C, wherein Tand Tindependently represent a bivalent hydrocarbon chain having 2-5 carbon atoms, preferably 2 or 3 carbon atoms; and anions (X)and (X)independently represent anions of pharmaceutically acceptable salts.

Helquats with heteroaromatic substituents, preparation thereof, and use thereof as G-quadruplex stabilizers

The invention provides helquat derivatives of general formula I, wherein substituents Rand Rare independently selected from a group comprising H and Cto Calkyl; up to three of S, S, Sand Sare present, each of S, S, Sand Sindependently represents a linker consisting of a bivalent hydrocarbon chain having 3-6 carbon atoms; one or two atoms selected from the carbon atoms with the descriptor 2, 4, 2', and 4&#x2032; are substituted with a substituent Rof general formula II or general formula III wherein Ris substituted or unsubstituted aryl; Tand Tindependently represent a bivalent hydrocarbon chain having 2-5 carbon atoms; and anions (X)and (X)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. 

Helquat derivatives, preparation thereof, and use thereof as medicaments

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Praha, Czechia

Miroslav Hajek