Article ID Journal Published Year Pages File Type
2079883 Drug Discovery Today 2016 18 Pages PDF
Abstract

•Cyclooxygenase-2 participates in carcinogenesis.•Cyclooxygenase-2 inhibitors can be used in breast cancer prophylaxis or therapy.•Trans-stilbene derivatives are a novel class of cyclooxygenase inhibitors.•In silico techniques are auxiliary means in the discovery of new drugs.

Cyclooxygenase-2 (COX-2) inhibitors are common anti-inflammatory drugs with pleiotropic, endogenous actions that could be useful in the management of breast cancer. Here, we provide a complete understanding of the biochemistry of COX-2 and discuss the various molecular mechanisms behind its increased expression in breast cancer. We also analyze the possible mechanisms responsible for the anticancer effect of COX-2 inhibitors and provide an overview of the available preclinical and clinical data on the use of COX-2 inhibitors in breast cancer. Finally, we describe a mathematical model of the relation between the structure and biological potency of promising new COX-2 inhibitors (trans-stilbenes) using a 2D quantitative structure–activity relationship (QSAR) technique.

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