Drug intelligence / Profile preview

CarbZDNaph

Development stage
Preclinical
Lead developer
University of Lodz
Modality
Small Molecules
01

Overview

CarbZDNaph is a carborane-based small molecule analog of the 5-lipoxygenase (5-LOX) inhibitor Rev-5901. It was investigated for its potential antineoplastic activity against colorectal carcinoma. In vitro studies using the CT26CL25 mouse colorectal carcinoma cell line demonstrated that CarbZDNaph reduces cell viability with an IC50 of 25 μM by inducing caspase-dependent apoptosis and cytoprotective autophagy. Despite its in vitro activity, CarbZDNaph failed to show efficacy in attenuating tumor growth in in vivo BALB/c mouse models, unlike its related compound CarbZDChin. The molecule targets the inflammatory pathway by inhibiting the conversion of polyunsaturated fatty acids into leukotrienes.

02

Targets

ALOX5 (Arachidonate 5-lipoxygenase)

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