Background: Searching for new cytotoxic agents with apoptosis induction may represent a viable strategy for cancer treatment to overcome the increased resistance to available anticancer agents. Objective: The purpose of the current study aimed at preparation and anticancer evaluation of two new series of 2Hquinolinone and halogenated 2H-quinolinone derivatives against two cancer cell lines. Methods: Two new series of 2Hquinolinone and halogenated 2H-quinolinone derivatives were prepared and screened for their cytotoxicity against breast MCF-7 and liver HepG-2 cancer cell lines as well as normal breast MCF-10a. Results: The tested molecules revealed good cytotoxicity and selectivity toward cancer cell line relative to normal cells. These compounds were analyzed by DNA flow cytometry on MCF-7 cells. They were found to cause G2/M phase arrest and induced apoptosis at pre-G1 phase. In addition, increased caspase 3/7 activity and decreased osteopontin expression verified the apoptotic activity. Conclusion: The potent compounds discovered in this study can be a hit for discovery of new cytotoxic agents and are worthy of further investigation.

Nowadays, quinoline scaffold is among the most vital construction compounds for the development of new drugs. The purpose of this research is to evaluate the anti-cancer activity of sodium salt of ethyl (E)-2-cyano-3-(7-hydroxy-4-methyl-2-oxoquinoline-1(2H)-yl)-3-(4-hydroxyphenyl) acrylate against Ehrlich ascites carcinoma (EAC) cells residing in female mice's peritoneal cavity. The docking study exhibited a favourable interaction between the compound and the receptors 1MOY and 3KJF of osteopontin and caspase 3, respectively. The compound's sodium salt showed potential antioxidant and anti-cancer effects against Ehrlich ascites carcinoma (EAC) cells in vivo.Herein, the results elucidated that treatment with the compound's sodium salt exerted significant chemopreventive and chemotherapeutic effects, which reduced both EAC cell volume and count. Our results revealed that treatment with the sodium salt of the compound demonstrated a remarkable in vivo apoptotic effect through elevation of the expression of caspase 3 and reduction of osteopontin levels. Histopathological examination confirmed that the compound's sodium salt improved liver and kidney tissues without any apparent adverse effects.