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Synthesis and anticancer activity of tertiary amides of salinomycin and their C20-oxo analogs.

07:00 EST 8th November 2019 | BioPortfolio

Summary of "Synthesis and anticancer activity of tertiary amides of salinomycin and their C20-oxo analogs."

The polyether ionophore salinomycin (SAL) has captured much interest because of its potent activity against cancer cells and cancer stem cells. Our previous studies have indicated that C1/C20 double-modification of SAL is a useful strategy to generate diverse agents with promising biological activity profiles. Thus, in this paper, we describe the synthesis of a new class of SAL analogs that combine key modifications at the C1 and C20 positions. The activity of the obtained SAL derivatives was evaluated using primary acute lymphoblastic leukemia, human breast adenocarcinoma and normal mammary epithelial cells. One single- (5a) and two novel double-modified analogs (5b, 13b) were more potent towards the MDA-MB-231 cell line than SAL or its C20-oxo analog 2. When select analogs were tested against the NCI-60 human tumor cell line panel, 4a showed particular sensitivity to ovarian cancer cell line SK-OV-3. Additionally, both SAL and 2 were potent ex vivo against human ER/PR+, Her2- invasive mammary carcinoma, with 2 showing minimal toxicity towards normal epithelial cells. The present findings highlight the therapeutic potential of SAL derivatives for select targeting of different cancer types.

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This article was published in the following journal.

Name: ChemMedChem
ISSN: 1860-7187
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