Design, synthesis and biological evaluation of arylsulfonamides as ADAMTS7 inhibitors

Author:

Cuffaro Doretta1ORCID,Burkhard Tina2ORCID,Bernardoni Bianca Laura1ORCID,Di Leo Riccardo1ORCID,Zhang Xiaohan3,Galati Salvatore1ORCID,Tuccinardi Tiziano1,Macchia Marco1,Rossello Armando1,Santamaria Salvatore2ORCID,de Groot Rens3ORCID,Nuti Elisa1ORCID

Affiliation:

1. Department of Pharmacy, University of Pisa, Via Bonanno 6, 56126 Pisa, Italy

2. Department of Biochemical and Physiological Sciences, School of Biosciences, Faculty of Health and Medical Sciences, University of Surrey, Edward Jenner Building, Guildford GU2 7XH, UK

3. Institute of Cardiovascular Science, University College London, 51 Chenies Mews, London WC1E 6HX, UK

Abstract

Starting from the ADAMTS5/ADAMTS7 inhibitor EDV33, a structure-based optimization led to the lead compound 3a, with nanomolar activity against ADAMTS7 and good selectivity over ADAMTS5.

Funder

British Heart Foundation

Università di Pisa

Publisher

Royal Society of Chemistry (RSC)

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