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Expansion of the 4-(Diethylamino)benzaldehyde Scaffold to Explore the Impact on Aldehyde Dehydrogenase Activity and Antiproliferative Activity in Prostate Cancer

Ali I. M. Ibrahim, Elisabet Batlle, S Sneha, Rafael Jiménez, Raquel Pequerul, Xavier Parés, Till Rüngeler, Vibhu Jha, Tiziano Tuccinardi, Maria Sadiq, Fiona M. Frame, Norman J. Maitland, Jaume Farrés, Klaus Pors

2022Journal of Medicinal Chemistry24 citationsDOIOpen Access PDF

Abstract

were more potent than DEAB against patient-derived primary prostate tumor epithelial cells, as single agents or in combination treatment with docetaxel. In conclusion, our study supports the use of DEAB as an ALDH inhibitor but also reveals closely related analogues with increased selectivity and potency.

Topics & Concepts

Aldehyde dehydrogenaseChemistryProstate cancerBenzaldehydeProstateAldehydeCytotoxicitySelectivityIC50CancerCancer researchGene isoformPotencyCancer cellBiochemistryPharmacologyStereochemistryIn vitroEnzymeInternal medicineCatalysisGeneMedicineProstate Cancer Treatment and ResearchMass Spectrometry Techniques and ApplicationsBerberine and alkaloids research
Expansion of the 4-(Diethylamino)benzaldehyde Scaffold to Explore the Impact on Aldehyde Dehydrogenase Activity and Antiproliferative Activity in Prostate Cancer | Litcius