Preprint Article Version 1 Preserved in Portico This version is not peer-reviewed

Antitumour and Acute Toxicity Studies of 4-(pyridin-4-yl)-6-(thiophen-2-yl)pyrimidin-2(1H)-one Against Ehrlich Ascites Carcinoma and Sarcoma-180

Version 1 : Received: 23 January 2018 / Approved: 23 January 2018 / Online: 23 January 2018 (09:46:42 CET)

How to cite: Kumar, D.; Sharma, P.; Nepali, K.; Mahajan, G.; Mintoo, M.J.; Singh, A.; Mondhe, D.M.; Singh, G.; Jain, S.K.; Gupta, G.K.; Ntie-Kang, F. Antitumour and Acute Toxicity Studies of 4-(pyridin-4-yl)-6-(thiophen-2-yl)pyrimidin-2(1H)-one Against Ehrlich Ascites Carcinoma and Sarcoma-180. Preprints 2018, 2018010214 (doi: 10.20944/preprints201801.0214.v1). Kumar, D.; Sharma, P.; Nepali, K.; Mahajan, G.; Mintoo, M.J.; Singh, A.; Mondhe, D.M.; Singh, G.; Jain, S.K.; Gupta, G.K.; Ntie-Kang, F. Antitumour and Acute Toxicity Studies of 4-(pyridin-4-yl)-6-(thiophen-2-yl)pyrimidin-2(1H)-one Against Ehrlich Ascites Carcinoma and Sarcoma-180. Preprints 2018, 2018010214 (doi: 10.20944/preprints201801.0214.v1).

Abstract

In an effort to discover an effective and selective antitumour agent, synthesis and anti-cancer potential of 4-(pyridin-4-yl)-6-(thiophen-2-yl)pyrimidin-2(1H)-one (SK-25), which has been reported earlier by us with significant cytotoxicity towards MiaPaCa-2 malignant cells, with an IC50 value of 1.95 μM and was found to instigate apoptosis. In the present study, the antitumour efficacy of SK-25 was investigated on Ehrlich ascites tumour (solid), Sarcoma 180 (solid) tumour and Ehrlich ascites carcinoma. The compound was found to inhibit tumour development by 94.71% in Ehrlich ascites carcinoma (EAC), 59.06% in Ehrlich tumour (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. Computer-based predictions also show that the compounds could have an interesting DMPK profile. The current study provides insight for further investigation of the antitumour potential of the molecule.

Keywords

antitumour; cancer; chalcone; DMPK; in silico; in vivo

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