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Morpholine substituted quinazoline derivatives as anticancer agents against MCF-7, A549 and SHSY-5Y cancer cell lines and mechanistic studies.

ABSTRACT: A series of morpholine substituted quinazoline derivatives have been synthesized and evaluated for cytotoxic potential against A549, MCF-7 and SHSY-5Y cancer cell lines. These compounds were found to be non-toxic against HEK293 cells at 25 μM and hence display anticancer potential. In these series compounds, AK-3 and AK-10 displayed significant cytotoxic activity against all the three cell lines. AK-3 displayed IC₅₀ values of 10.38 ± 0.27 μM, 6.44 ± 0.29 μM and 9.54 ± 0.15 μM against A549, MCF-7 and SHSY-5Y cancer cell lines. Similarly, AK-10 showed IC₅₀ values of 8.55 ± 0.67 μM, 3.15 ± 0.23 μM and 3.36 ± 0.29 μM against A549, MCF-7 and SHSY-5Y, respectively. In the mechanistic studies, it was found that AK-3 and AK-10 inhibit the cell proliferation in the G1 phase of the cell cycle and the primary cause of death of the cells was found to be through apoptosis. Thus, morpholine based quinazoline derivatives have the potential to be developed as potent anticancer drug molecules.

SUBMITTER: Dwivedi AR

PROVIDER: S-EPMC9132193 | biostudies-literature | 2022 May

REPOSITORIES: biostudies-literature

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Morpholine substituted quinazoline derivatives as anticancer agents against MCF-7, A549 and SHSY-5Y cancer cell lines and mechanistic studies.

Dwivedi Ashish Ranjan AR Kumar Vijay V Prashar Vikash V Verma Akash A Kumar Naveen N Parkash Jyoti J Kumar Vinod V

RSC medicinal chemistry 20220405 5

A series of morpholine substituted quinazoline derivatives have been synthesized and evaluated for cytotoxic potential against A549, MCF-7 and SHSY-5Y cancer cell lines. These compounds were found to be non-toxic against HEK293 cells at 25 μM and hence display anticancer potential. In these series compounds, AK-3 and AK-10 displayed significant cytotoxic activity against all the three cell lines. AK-3 displayed IC50 values of 10.38 ± 0.27 μM, 6.44 ± 0.29 μM and 9. ...[more]

PMID: 35694693

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Project description:The modulation of the brain's electrical activity for therapeutic purposes has recently gained attention, supported by the promising results obtained through the non-invasive application of transcranial direct current stimulation (tDCS) in the treatment of neurodegenerative and neurological diseases. To optimize therapeutic efficacy, it is crucial to investigate the cellular and molecular effects of tDCS. This will help to identify important biomarkers, predict patient's response and develop personalized treatments. In this study, we applied direct current stimulation (DCS) to a neural cell line, using mild currents over short periods of time (0.5 mA, 20 min), with 24-h intervals. We observed that DCS induced changes in the cellular lipidome, with transient effects observed after a single stimulation (lasting 24 h) and more significant, long-lasting effects (up to 72 h) after repeated stimulation cycles. In neural cells, multiple DCS treatment modulated structural membrane lipids (PE, PS, PI), downregulated glycerol lipids with ether-linked fatty acids and pro-inflammatory lipids (ceramides and lyso-glycerophospholipids) (p ≤ 0.005). Multiple DCS sessions altered transcriptional activity by decreasing the expression of inflammatory cytokines (TNF-α, p ≤ 0.05; IL-1β, p ≤ 0.01), while increasing the expression of neuroprotective factors such as heme oxygenase-1 (p ≤ 0.0001) and brain-derived neurotrophic factor (p ≤ 0.05), as well as proteins involved in vesicular transport (SNARE, sorting nexins and seipin and α-synuclein; p ≤ 0.05). In addition, DCS enhanced the release of extracellular vesicles, with repeated stimulations significantly increasing the release of exosomes threefold. In conclusion, while a single electrical stimulation induces transient metabolic changes with limited phenotypic effects, repeated applications induce a broader and deeper modulation of lipid species. This may lead to a neuroprotective and neuroplasticity-focussed transcriptional profile, potentially supporting the therapeutic effects of tDCS at the cellular and molecular level in patients..

Dataset Information

Morpholine substituted quinazoline derivatives as anticancer agents against MCF-7, A549 and SHSY-5Y cancer cell lines and mechanistic studies.

Publications

Morpholine substituted quinazoline derivatives as anticancer agents against MCF-7, A549 and SHSY-5Y cancer cell lines and mechanistic studies.

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