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Antitumor and acute toxicity studies of 4-(pyridin-4-yl)-6-(thiop | 57661
Journal of Clinical Trials

Journal of Clinical Trials
Open Access

ISSN: 2167-0870

+44 7868 792050

Antitumor and acute toxicity studies of 4-(pyridin-4-yl)-6-(thiophen-2-yl)pyrimidin-2(1H)-one against Ehrlich ascites carcinoma and sarcoma-180


Joint Event on Global Pharmacovigilance and Advanced Pharmacy

July 16-17, 2018 Sydney, Australia

Dinesh Kumar

Sri Sai College of Pharmacy, India

Posters & Accepted Abstracts: J Clin Trials

Abstract :

In an effort to discover an effective and selective anti-tumor agent, 4,6-diarylpyrimidones as constrained chalcone analogues have been synthesized were evaluated against a panel of human cancer cell lines. Striking selectivity was displayed by the compounds against MiaPaca-2 (breast) cell lines while PC-3 (prostate) and A-549 (lung) cell lines were almost resistant to the exposure of the test compounds. Compound SK-25 exhibited remarkable cytotoxicity against MiaPaca-2 cell line with an IC50 value of 1.95 ?¼M and was found to induce apoptosis evidenced through phase contrast microscopy, DAPI staining, mitochondrial membrane potential loss. The cell phase distribution studies indicated that the apoptotic population increased from 1.79% in control sample to 30.33% in sample treated with 20 ?¼M compound SK-25. The anti-tumor efficacy of SK-25 was investigated on Ehrlich ascites tumor (solid), sarcoma 180 (solid) tumors and Ehrlich ascites carcinoma. The compound was found to inhibit tumor development by 94.71% in Ehrlich Ascites Carcinoma (EAC), 59.06% in Ehrlich Tumor (ET, solid) and 45.68% in Sarcoma-180 (solid) at 30 mg/kg dose. Additionally, SK-25 was established to be non-toxic at a maximum tolerated dose of 1000 mg/kg in acute oral toxicity in Swiss-albino mice. The current study provides insight for further investigation of the anti-tumor potential of the molecule.

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