Triazole-substituted N-hydroxyindol-2-carboxylates as inhibitors of isoform 5 of human lactate dehydrogenase (hLDH5)

Carlotta Granchi; Sarabindu Roy; Claudia Del Fiandra; Tiziano Tuccinardi; Mario Lanza; Laura Betti; Gino Giannaccini; Antonio Lucacchini; Adriano Martinelli; Marco Macchia; Filippo Minutolo

doi:10.1039/C1MD00071C

Triazole-substituted N-hydroxyindol-2-carboxylates as inhibitors of isoform 5 of human lactate dehydrogenase (hLDH5)†

Carlotta Granchi,^a Sarabindu Roy,^a Claudia Del Fiandra,^a Tiziano Tuccinardi,^a Mario Lanza,^b Laura Betti,^a Gino Giannaccini,^b Antonio Lucacchini,^b Adriano Martinelli,^a Marco Macchia^a and Filippo Minutolo*^a

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^a Dipartimento di Scienze Farmaceutiche, Università di Pisa, Via Bonanno 6, Pisa, Italy
E-mail: filippo.minutolo@farm.unipi.it
Fax: +39 050 2219605
Tel: +39 050 2219557

^b Dipartimento di Psichiatria, Neurobiologia, Farmacologia e Biotecnologie, Università di Pisa, Via Bonanno 6, Pisa, Italy

Abstract

hLDH5 plays a key role in the glycolytic metabolic switch found in invasive tumours and is now considered as a promising therapeutic target in cancer. Here we report a series of new hLDH5-inhibitors based on triazole-containing N-hydroxyindol-2-carboxylates, whose synthesis includes the highly reliable and simple “click chemistry” reaction.

MedChemComm

Triazole-substituted N-hydroxyindol-2-carboxylates as inhibitors of isoform 5 of human lactate dehydrogenase (hLDH5)†

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Triazole-substituted N-hydroxyindol-2-carboxylates as inhibitors of isoform 5 of human lactate dehydrogenase (hLDH5)

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