In vivo anti-tumour activity of novel Quinazoline derivatives

V. Alapati, M.N. Noolvi, S.N. Manjula, K.J. Pallavi, H.M. Patel, B.S. Tippeswamy, S.V. Satyanarayana

Department of Pharmacology, JSS College of Pharmacy, Mysore, Karnataka, India. snm.manjula@gmail.com

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• Pharmacology

OBJECTIVE: The two scaffold Quinazoline analogues (Compound 21, NSC: 95112/753439 and Compound 12, NSC: D-104834/ 758270) in three different concentrations were evaluated for their anti-tumor activity against Ehrlich ascites carcinoma (EAC) and two different concentration were evaluated for their anti-tumor activity against Dalton’s ascites lymphoma (DLA) bearing Swiss albino mice.

MATERIALS AND METHODS: The in vivo anti-tumor potency of Quinazoline bases was assessed in EAC model by measuring the increase in mean survival time of the drug treated 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 anti-tumor 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 drug treated over untreated control mice and treated standard (Gefitinib) mice.

RESULTS AND CONCLUSIONS: Among the two quinazoline bases studied, 3-(2-chloro benzylideneamine)-2-(furan-2-yl) quinazoline-4(3h)-one (Compound 21) at an optimal dose of 20 mg/kg body weight was found to enhance the mean survival time of infected mice. Haematological parameters and mean survival time in tumor bearing mice were found to be significantly restored towards normal after treatment with Compound 21 at 20 mg/kg body weight of mice in EAC model. Tumor volume and tumor weight in tumor bearing mice were found to be significantly restored towards normal after treatment with Compound 12 at 20 mg/kg body weight of mice in DLA model. Compound 21 at a prime dose of 20 mg has shown promising anticancer activity in vivo against EAC and DLA models when compared to standard drug with minimum toxic effects.

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