In Vitro Anticancer Evaluation of Some Synthesized 2H-Quinolinone and Halogenated 2H-Quinolinone Derivatives as Therapeutic Agents

Abstract

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.

In vivo biological evaluation of sodium salt of ethyl (E)‐2‐cyano‐3‐(7‐hydroxy‐4‐methyl‐2‐oxoquinoline‐1(2H)‐yl)‐3‐(4‐hydroxyphenyl) acrylate as anticancer agent

“…Our results agree with those of our previous in vitro measurement of apoptotic markers, 11 and this proves that treatment with ethyl (E)-2-cyano-3-(7-hydroxy-4-methyl-2-oxoquinoline-1(2H)yl)-3-(4-hydroxyphenyl) acrylate induces expressions of caspase 3…”

“…In addition, different quinoline derivatives have displayed impressive anti-cancer activity via DNA intercalation and interference with the replication process. 9,10 As a continuation of our previous study, 11 quinoline derivatives were assessed in vitro for their antiproliferative ability against two cancer cell lines. Most compounds have proven to be effective.…”

Snail Mucus from Achatina fulica as a Biomaterial Exhibits Pro-Survival Effects on Human Chondrocytes

“…Since 6-gingerol is the only phenolic compound detected during the LC–MS/MS analysis, and the total phenols estimated in the SMu by the Folin–Ciocalteu method was 66 μg/mL, therefore, 6-gingerol may be the phenolic compound in the polyphenols detected and gastropod mucus so far, but its specific role in SMu needs to be further explored. Furthermore, quinolinone has been reported for its anticancer activity. , The presence of this substance in SMu may positively impact the anticancer properties of SMu. For example, Ellijimi et al reported the antitumorigenic effects of H.…”

A Review of the Recent Developments of Molecular Hybrids Targeting Tubulin Polymerization

“…Heterocycle-fused quinolinone is another privileged structure used as a building block in drug discovery. The quinolinone hybrids have shown biological activities, including antimicrobial [ 75 ], anti-inflammatory [ 76 ], anticancer [ 77 ], anti-Alzheimer [ 78 ], and anti-leishmanial [ 79 ] effects. Interestingly, quinolinone derivatives can successfully inhibit IDH1 mutants R132H, R132C, R132G, and R132L and display good selectivity vs. the wild-type IDH protein [ 80 ].…”