Preprint Article Version 1 This version not peer reviewed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.

Subject Areas

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

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