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conferenceseries.com
Volume 8 Journal of Clinical Trials Pharmacy and Pharmacovigilance 2018
July 16-17, 2018
July 16-17, 2018 Sydney, Australia
Joint Event on
Global Pharmacovigilance and
Advanced Pharmacy
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
Dinesh Kumar
Sri Sai College of Pharmacy, India
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 μM 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 μM 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.
J Clin Trials 2018, Volume 8
DOI: 10.4172/2167-0870-C2-026