Original scientific paper

https://doi.org/10.2478/v10007-009-0040-9

Sinteza, antitumorsko i citostatsko djelovanje derivata 6H-indolo[2,3-b]kinoksalina

SUBHAS S. KARKI ; Department of Pharmaceutical Chemistry, KLE College of Pharmacy, 2nd Block Rajajinagar, Bangalore-560 010, India
RAHUL HAZARE ; Department of Pharmaceutical Chemistry, KLE College of Pharmacy, 2nd Block Rajajinagar, Bangalore-560 010, India
SUJEET KUMAR ; Department of Pharmaceutical Chemistry, KLE College of Pharmacy, 2nd Block Rajajinagar, Bangalore-560 010, India
VIVEK S. BHADAURIA ; Department of Pharmaceutical Chemistry, KLE College of Pharmacy, 2nd Block Rajajinagar, Bangalore-560 010, India
JAN BALZARINI ; Rega Institute for Medical Research, Katholieke Universiteit Leuven, B-3000 Leuven Belgium
ERIK De CLERCQ ; Rega Institute for Medical Research, Katholieke Universiteit Leuven, B-3000 Leuven Belgium

Abstract

Reakcijom 1,5-disupstituiranih 2,3-diokso-2,3-dihidroindola s ortofenilen diaminom sintetizirani su različiti 6-aralkil-9-supstituirani-6H-indolo[2,3-b]kinoksalini. Spojevi 5b, 5d, 5g i 5l pokazali su značajno antitumorsko djelovanje na 59 humanih tumorskih stanica. Svi sintetizirani spojevi ispitani su na citostatsko djelovanje na stanične linije Molt 4/C8 i CEM T-limfocite, te na murin L1210 stanice leukemije. IC50 za spoj 5h je 71 μmol mL1 na staničnu liniju Molt 4/C8 i 117 μmol mL1 na CEM, dok su vrijednosti za melfalan 3,2, odnosno 2,5 μmol mL1. IC50 spoja 7i na stanice L1210 je 7,2 μmol mL1, dok je za melfalan 2,1 μmol mL1.

Keywords

indolo[2,3-b]kinoksalin; citostatsko djelovanje; antitumorsko djelovanje

Hrčak ID:

41024

URI

https://hrcak.srce.hr/41024

Publication date:

1.12.2009.

Article data in other languages: english

Visits: 1.859 *