Articles Accepted

In-silico and in vitro assessment of synthesized quinoline-thiazole hybrid bearing diazenyl sulfonamides as apoptosis inducers and radical scavengers

ABSTRACT A series of eight quinoline-thiazole hybrid bearing diazenyl sulfonamides, 4a-4h were synthesized and characterized by UV-Vis, FT/IR, 1H NMR and LC-MS. These compounds were formed when two prepared intermediate precursors of schiff-base compounds, (E)-N-((2-chloroquinolin-3-yl)methylene)-4-phenylthiazol-2-amine (3a) and (E)-N-((2-chloroquinolin-3-yl)methylene)-4-chlorophenylthiazol-2-amine (3b) have converted to the corresponding diazenyl compounds 4a-4h by treating and coupling with the individual diazonium salt of sulfa-drugs. The results of in vitro cytotoxic activity of the synthesized compounds in two cancer cell lines MCF 7 (human breast cancer cell line) and K562 (myelogenousleukemia cell line) have shown the IC50 values as given: 4b against MCF 7 19.52 and against K562 20.55µM; 4d against MCF 7 15.96 and against K562 13.05µM. Moreover, the compound 4-(((Z)-(2-chloroquinolin-3-yl)(4-phenylthiazol-2-ylimino)methyl)diazenyl)benzenesulfonic acid (4d) have induced maximum percentage of apoptosis. Furthermore, the in vitro antioxidant activity study revealed that among all the synthesized compounds, the compound 4d have an excellent radical scavenging effect. Additionally, molecular docking was performed to investigate the binding affinity of H-bonding interaction of synthesized compounds with a targeted enzyme and to compare it with the anticancer drugs, Dasatinib, Bosutinib and Dacarbazine.

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