Discovering simple phenylboronic acid and benzoxaborole derivatives for experimental oncology - phase cycle-specific inducers of apoptosis in A2780 ovarian cancer cells

Investigational New Drugs
Mateusz PsurskiAndrzej Sporzyński

Abstract

Objective The aim of the study was to evaluate the antiproliferative potential of simple phenylboronic acid and benzoxaborole derivatives as well as to provide preliminary insight into their mode of action in cancer cells in vitro. Methods The antiproliferative activity was assessed in five diverse cancer cell lines via the SRB method (sulforhodamine B) or MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) method after 72 h of treatment. Further studies of the mechanism of action consisted of the influence of the compounds on cell cycle progression and apoptosis induction, which was assessed by flow cytometry, caspase-3 enzymatic activity, fluorescence microscopy and western blot analysis. Results A clear structure-activity relationship was observed for both groups of compounds with several representatives evaluated as highly active antiproliferative agents with low micromolar [Formula: see text] values. 2-Fluoro-6-formylphenylboronic acid (18) and 3-morpholino-5-fluorobenzoxaborole (27) exhibited strong cell cycle arrest induction in G2/M associated with caspase-3 activation in an A2780 ovarian cancer cell line. These events were accompanied by a mitotic catastrophe cell morphology and an increased percentage o...Continue Reading

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Citations

Sep 25, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Mariana Pereira SilvaMaria Emília Sousa
Aug 25, 2019·Bioorganic Chemistry·Krzysztof M BorysAgnieszka Adamczyk-Woźniak

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Methods Mentioned

BETA
fluorescence microscopy
GTPases

Software Mentioned

Cheburator
ImageJ
Prolab
GraphPad Prism
Flowing

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