Reactive Pt(II) center as part of redox-active quinoline-based heterocyclic scaffolds toward new anticancer leads

[Display omitted] New cisplatin analogs in which the diamminedichloro-Pt(II) unit is conjugated to dihydroquinoline- or tetrahydroquinoline frameworks were synthesized and subjected to biological evaluation in order to understand their effects on cellular redox homeostasis and cell viability. They e...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2020-11, Vol.30 (22), p.127594-127594, Article 127594
Main Authors: Kumbhakonam, Sateeshkumar, Saroj, Soumya, Venkatesan, Nalini, Devarajan, Karunagaran, Manheri, Muraleedharan K.
Format: Article
Language:English
Subjects:
Anticancer leads
Cisplatin analogs
Dihydroquinoline
Redox chemotherapy
Tetrahydroquinoline
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Summary:[Display omitted] New cisplatin analogs in which the diamminedichloro-Pt(II) unit is conjugated to dihydroquinoline- or tetrahydroquinoline frameworks were synthesized and subjected to biological evaluation in order to understand their effects on cellular redox homeostasis and cell viability. They exhibited better selectivity towards cancer cells (A549) compared to mice fibroblast NIH3T3 cells, with cytotoxicity in the same range as that of cisplatin. There was structure-dependent variation in the levels of ROS and were also able to induce cell death, as evidenced by accumulation of cells in sub-G1 phase.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2020.127594