Bazı Rutenyum (II) Komplekslerinin Sentezi, Sitostatik ve Antiviral Aktiviteleri

Subhas S. KARKI,Ravikumar TK,Arpit KHATIYAR,Sreekanth THOTA,Sujeet KUMAR,Sureshbabu A RAMAREDDY,Erik De CLERCQ,Jan BALZARINI

Abstract

(where L=2,2’-bipyridine (bpy)/ 1,10-phenanthroline (phenyl)/ dimethylsulfoxide (DMSO)) with ligands L1= HBT, FCl-HBT, IINH, NO2-MPC, OCH3-MPC, N(CH3)2-MPC, Cl-MPC (where HBT=2-hydrazinyl- 1,3-benzothiazole, FCl-HBT =5-chloro-6-fluoro-2-hydrazinyl-1,3-benzothiazole, IINH=N-2-oxo-1,2- dihydro-3H-indol-3-ylidene]pyridine-4-carbo-hydrazide, NO2-MPC=N(4-nitrophenyl)-methylidenepyridine-4-carbohydrazide,OCH3-MPC=N(4-methoxyphenyl)methylidene-pyridine-4-carbohydrazide, N(CH3)2-MPC=N(4-dimethylaminophenyl)methylidene-pyridine-4-carbo-hydrazide, Cl-MPC=N(4- chlorophenyl)methylidene-pyridine-4-carbohydrazide. The title complexes were subjected to in vitro cytostatic activity testing against the human cervix carcinoma HeLa and T-lymphocyte CEM cell lines, and the murine leukemia tumor cell line L1210. The most active ruthenium complex TKA-9 [Ru(phen)2(N(CH3)2-MPC)] revealed a cytostatic activity of 16 µM against CEM, 20 µM against L1210 and 5.5 µM against HeLa tumor cells. All complexes were also tested for antiviral activity against a wide variety of DNA and RNA viruses, but found not to display selective activity at subtoxic concentrations.

Özet

Ru(L)2Cl2'in (L=2,2'-bipiridin (bpy)/ 1,10-fenantrolin (fenil)/dimetilsülfoksit), L1= HBT, FCl-HBT, IINH, NO2-MPC, OCH3-MPC, N(CH)2-MPC, Cl-MPC (HBT=2-hidrazinil-1,3-benzotiyazol, FCl- HBT=5-kloro-6-floro-2-hidrazinil-1,3-benzotiyazole, ilidene]piridine-4-karbohidrazit, NO2-MPC= N(4-nitrofenil)-metiyliden-piridin-4-karbohidrazit, OCH3- MPC=N(4-metoksifenil)metiliden-piridin-4-karbohidrazit, dimetilaminofenil)metiliden-piridin-4-karbohidrazit, karbohidrazit ligantları ile reaksiyonuyla 11 adet rutenyum kompleksi hazırlanmıştır. Elde edilen kompleksler insan serviks karsinoma HeLa ve T-lemfosit CEM hücreleri ile fare lösemi tümör L1210 hücrelerinde sitostatik aktivitileri açısından değerlendirilmiştir. En aktif rutenyum kompleksi olan TKA-9 [Ru(fen)2(N(CH3)2-MPC)] CEM hücrelerinde, 16 µM, L1210 hücrelerinde 20 µM ve HeLa hücrelerinde 5.5 µM sitostatik aktivite göstermiştir. Ayrıca bütün bileşikler antiviral aktiviteleri açısından da değerlendirilmiş ancak subtoksik konsantrasyonlarda selektif aktivite göstermedikleri saptanmıştır