What question did this study set out to answer?

The study aims to design and synthesize new inhibitors for monocarboxylate transporters, specifically MCT1.

February 28, 2026Журнал органической химии / Russian Journal of Organic Chemistry0 citations

Design, Synthesis, and Biological Evaluation of New Potential Inhibitors of Monocarboxylate Transporters MCT1 Based on 1,5-Diarylpyrazoles

Key Points

The study aims to design and synthesize new inhibitors for monocarboxylate transporters, specifically MCT1.
Synthesis of inhibitors through arylation of pyrazole using the Suzuki reaction.
Preparation of derivatives with aryl and heteroaryl groups at position 5 of the pyrazole ring.
Evaluation of the ability of synthesized compounds to block lactate transport into cells.
The compound derivative 3a showed significant inhibition of lactate transport.
At concentrations of 25 and 50 μM, derivative 3a exhibited activity comparable to the known MCT1 inhibitor BAY-8002.
Multiple target derivatives were successfully synthesized and evaluated.

Abstract

The article describes the synthesis of potential inhibitors of lactic acid transport proteins (MCT proteins). The key stage of the synthesis is the arylation of pyrazole by the Suzuki reaction. According to the synthetic scheme proposed in the work, a number of target derivatives containing aryl and heteroaryl substituents at position 5 of the pyrazole ring were obtained. The ability to block lactate transport into the cell was assessed for all the derivatives obtained. It was shown that the most promising compound is derivative 3a, containing a chloropyridine fragment at position 5 of pyrazole. Its activity at concentrations of 25 and 50 μM was comparable to the activity of the confirmed MCT1 inhibitor BAY-8002, which was used as a reference compound.

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