Synthesis and Evaluation of Some Alkoxy-, Chloro-, and Acyloxy-Conjugated Styryl Ketones Against P-388 Lymphocytic Leukemia and an Examination of the Metabolism and Toxicological Effects of l-(m-Ethoxymethyloxyphenyl)-l-nonen-3-one in Rats

Dimmock, Jonathan R.; Kirkpatrick, David; Webb, N.G.; Cross, B.

doi:10.1002/jps.2600710912

Cited by 5 publications

(1 citation statement)

References 29 publications

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“…In addition, there have been a number of studies that deal with the cytotoxic activities of α,β-unsaturated ketones which are being designed as thiol-alkylators [10][11][12]. In one study, for example, acyclic α,β-unsaturated ketones were found to be nearly bereft of cytotoxic activity following their tests against P388 lymphocytic leukemia in mice [13][14][15]. Later studies dealt with the cytotoxic activity of 2,6-bis(phenylmethylene)-cyclohexanone against murine P388/MRI leukemic cells where the IC 50 value disclosed to be 36.5 nM [16].…”

Section: Introductionmentioning

confidence: 99%

Functionalized N-Pyridinylmethyl Engrafted Bisarylmethylidenepyridinones as Anticancer Agents

Al‐thamili¹,

Almansour²,

Arumugam³

et al. 2020

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Structurally interesting N-pyridinylmethyl engrafted bisarylmethylidenepyridinones with high functionality have been constructed in good yield. The structural interpretation of these compounds has been done with the aid of spectroscopic analysis and further established by single crystal X-ray diffraction studies. Following physical characterization, the synthesized compounds were tested for their in vitro anticancer activity against HepG2 cancer cells and it was found that all of the compounds exhibited some level of activity. We observed a significant level of cell viability losses to the cancer cells, while only smaller losses to the non-cancer cells were observed. Besides, the mechanistic investigation of toxicology revealed that the cancer cells were undergoing apoptotic pathway, induced by the generation of oxidative stress and the involvement of caspases. The analysis provides preliminary evidence for the successful control of cancer cells with a minimal effect on healthy normal cells because of the high IC50 levels and cell death mechanisms.

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Section: Introductionmentioning

confidence: 99%