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(1)-one (), which has been reported earlier by us with significant cytotoxicity towards MiaPaCa-2 malignant cells, with an IC value of 1.95 μM and was found to instigate apoptosis. In the present study, the antitumour efficacy of was investigated on Ehrlich ascites tumour (EAT, 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, 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 since all 51 computed physicochemical parameters fall within the recommended range for 95% of known drugs. The current study provides insight for further investigation of the antitumour potential of the molecule.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6039700 | PMC |
| http://dx.doi.org/10.1016/j.heliyon.2018.e00661 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Rhodium complex [RhLI]I: a novel anticancer agent inducing tumor inhibition and apoptosis.
Discov Oncol
December 2024
Department of Biochemistry and Molecular Biology, University of Rajshahi, Rajshahi, 6205, Bangladesh.
Numerous chemotherapeutic agents are currently employed in cancer treatment, but many are associated with significant side effects. This study aims to identify a novel anticancer drug that minimizes or eliminates these adverse effects. The anticancer activity of the Rhodium (III) complex cis-[RhLI]I was evaluated through both in vivo and in vitro functional assays.
View Article and Find Full Text PDFMolecular docking and / studies of a novel thiadiazole Schiff base as a hepatoprotective drug against angiogenesis induced by breast cancer.
RSC Adv
December 2024
Department of Pharmaceutics, Faculty of Pharmacy, Delta University for Science and Technology Gamasa Egypt.
Two new thiadiazole imidazolium salicylidene Schiff bases (TISSBs) were successfully synthesized, and their structures were analyzed comprehensively using spectroscopic techniques. The results of the MTT assay showed that TISSB2 was the safest and most effective anti-breast cancer agent. The anti-angiogenic activity of TISSB2 was evaluated using tests in Ehrlich ascites carcinoma (EAC)-bearing Swiss albino mice.
View Article and Find Full Text PDFRetraction Note: Hepatic ameliorative role of vitamin B17 against Ehrlich ascites carcinoma-induced liver toxicity.
Environ Sci Pollut Res Int
December 2024
Zoology Department, Faculty of Science, Tanta University, Tanta, Egypt.
Assessment of in vivo and in vitro anti-tumoral effects of Lycium barbarum extract on Ehrlich ascites tumor cells: histopathology, DNA damage and AgNOR.
Cell Mol Biol (Noisy-le-grand)
November 2024
Yozgat Bozok University, Faculty of Medicine, Department of Anatomy, Yozgat, Turkey.
Article Synopsis
- Natural product research has a rich history and has significantly impacted cancer treatment by targeting deregulated signaling pathways.
- Lycium barbarum shows promise due to its antioxidant and anti-cancer properties, as demonstrated through both in vivo and in vitro studies using Ehrlich ascites tumor (EAT) cells.
- The findings suggest that Lycium barbarum extracts reduce cancer cell adhesion and DNA damage, with the higher molecular weight extracts being more effective in promoting cancer cell death and potentially preventing cancer progression.
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!