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- W4313479935 abstract "In cancer cells, Pol η allows DNA replication and cell proliferation even in the presence of chemotherapeutic drug-induced damages, like in the case of platinum-containing drugs. Inhibition of Pol η thus represents a promising strategy to overcome drug resistance and preserve the effectiveness of chemotherapeutic drugs. Here, we report the discovery of a novel class of Pol ƞ inhibitors, with 35 active close analogs. Compound 21 (ARN24964) stands out as the best inhibitor, with an IC50 value of 14.7 μM against Pol η and a good antiproliferative activity when used in combination with cisplatin - with a synergistic effect in three different cancer cell lines (A375, A549, OVCAR3). Moreover, it is characterized by a favorable drug-like profile in terms of its aqueous kinetic solubility, plasma and metabolic stability. Thus, ARN24964 is a promising compound for further structure-based drug design efforts toward developing drugs to solve or limit the issue of drug resistance to platinum-containing drugs in cancer patients." @default.
- W4313479935 created "2023-01-06" @default.
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- W4313479935 date "2023-02-01" @default.
- W4313479935 modified "2023-10-14" @default.
- W4313479935 title "Computer-aided identification, synthesis, and biological evaluation of DNA polymerase η inhibitors for the treatment of cancer" @default.
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- W4313479935 doi "https://doi.org/10.1016/j.ejmech.2022.115044" @default.
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