In vivo Anti-Tumour Activity of Novel 2, 3, 7 Trisubstituted Quinazoline Derivatives

OBJECTIVE: The 2, 3, 7-trisubstituted quinazoline derivatives (Compound HP1, HP2, HP3 and HP4) in two different concentrations were evaluated for antitumor activity against Ehrlich ascites carcinoma (EAC) and Dalton’s lymphoma ascites (DLA) bearing Swiss albino mice.
METHODS: The in vivo antitumor potency of quinazoline bases was measured in EAC model by assessing the increase in mean survival time of the treated drug over untreated control mice and treated standard (Gefitinib) mice. Their toxicity was assessed in vivo in normal, standard and EAC bearing mice by measuring the drug-induced changes in haematological parameters. The in vivo antitumor potency of quinazoline bases was assessed in DLA model by measuring solid tumor volume, solid tumor weight and % inhibition of the tumor weight of the treated drug over untreated control mice and treated standard (Gefitinib) mice.
RESULTS: Among the four quinazoline bases studied, HP1, HP3 and HP4 at a dose of 10mg/kg and 20 mg/kg, optimally inhibited the growth of EAC and DLA cells in vivo. Besides, the treatment with HP1 and HP3 (20 mg/kg) significantly restored the deviated haematological parameters in EAC challenged mice. In vivo result authenticates that compound HP3 at a dose of 20mg/kg was most effective. The apoptotic studies shows that, both HP1 and HP3, at 10 and 20 mg/kg body weight showed induction of apoptosis as they significantly restored the deviated haematological parameters in EAC challenged mice. CONCLUSIONS: Further studies are required to explore the mechanism of action of this novel molecule which might bring gifted outcomes in cancer chemotherapy.

Author(s): Pallavi K.J, Jeevani C.V, Mayur P, Manjula S.N, Satyanarayana S.V, Thippeswamy B.S and Noolvi M.N

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