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
نویسندگان
چکیده
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 keywords: antitumour; cancer; chalcone; DMPK; in silico; in vivo Preprints (www.preprints.org) | NOT PEER-REVIEWED | Posted: 23 January 2018 doi:10.20944/preprints201801.0214.v1
منابع مشابه
Synthesis and cytotoxicity evaluation of some novel thiazoles, thiadiazoles, and pyrido[2,3-d][1,2,4]triazolo[4,3-a]pyrimidin-5(1H)-ones incorporating triazole moiety.
Reactions of hydrazonoyl halides and each of methyl 2-(1-(5-methyl-1-phenyl-1H-1,2,3-triazol-4-yl)ethylidene)hydrazine-1-carbodithioate and 2-(1-(5-methyl-1-phenyl-1H-1,2,3-triazol-4-yl)ethylidene)hydrazine-1-carbothioamide afforded 2-(1-(5-methyl-1-phenyl-1H-1,2,3-triazol-4-yl)ethylidene)hydrazono)-3-phenyl-5-substituted-2,3-dihydro-1,3,4-thiadiazoles and 5-(4-substituted)diazenyl)-2-(2-(1-(5-...
متن کاملInhibition of ascites tumor growth by 4-aminopyrazolo-(3,4-d)pyrimidine in combination with azaserine, 6-mercaptopurine, and thioguanine.
The effects of 4-aminopyrazolo(3,4-d)pyrimidine (APP), alone or in combination with azaserine, thioguanine, and 6-mercaptopurine, have been tested in Ehrlich ascites carcinoma, Sarcoma 180 ascites, 6C3HED ascites lymphosarcoma, Mecca ascites lymphosarcoma, and TAS ascites carcinoma. The Ehrlich ascites carcinoma is the only tumor of this series which responds to APP. Several combinations of APP...
متن کاملSynthesis and biological evaluation of some novel pyrazolopyrimidines incorporating a benzothiazole ring system.
In the present study, a series of benzothiazol derivatives 3a-l containing pyrazolo[3,4-d]pyrimidine moiety at the second position were synthesized and characterized by analytical and spectral data. The compounds were tested for their in vitro antimicrobial activity. Compounds 1-(1,3-benzothiazol-2- yl)-3-methyl-4-phenyl-1H-pyrazolo[3,4-d]pyrimidine (3a), 1- (1,3-benzothiazol-2-yl)-4-(4-chlorop...
متن کاملA major mechanism of action of nonsteroidal anti-inflammatory drugs (NSAIDs) is the lowering of prostaglandin (PG) production through inhibition of the cyclooxygenase
Accepted September 28, 2012 In the present study, a series of benzothiazol derivatives 3a-l containing pyrazolo[3,4-d]pyrimidine moiety at the second position were synthesized and characterized by analytical and spectral data. The compounds were tested for their in vitro antimicrobial activity. Compounds 1-(1,3-benzothiazol-2yl)-3-methyl-4-phenyl-1H-pyrazolo[3,4-d]pyrimidine (3a), 1(1,3-benzoth...
متن کاملSynthesis, Characterization and Anti-Breast Cancer Activity of New 4-Aminoantipyrine-Based Heterocycles
4-Aminoantipyrine was utilized as key intermediate for the synthesis of pyrazolone derivatives bearing biologically active moieties. The newly synthesized compounds were characterized by IR, 1H- and 13C-NMR spectral and microanalytical studies. The compounds were screened as anticancer agents against a human tumor breast cancer cell line MCF7, and the results showed that (Z)-4-((3-amino-5-imino...
متن کامل