Diversely substituted sulfamides for fragment-based drug discovery of carbonic anhydrase inhibitors: synthesis and inhibitory profile

A series of sulfamide fragments has been synthesised and investigated for human carbonic anhydrase inhibition. One of the fragments showing greater selectivity for cancer-related isoforms hCA IX and XII was co-crystalized with hCA II showing significant potential for fragment periphery evolution via...

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Detalles Bibliográficos
Autores principales: Sharonova, Tatiana, Zhmurov, Petr, Kalinin, Stanislav, Nocentini, Alessio, Angeli, Andrea, Ferraroni, Marta, Korsakov, Mikhail, Supuran, Claudiu T., Krasavin, Mikhail
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Taylor & Francis 2022
Materias:
Short Communication
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8933014/
https://www.ncbi.nlm.nih.gov/pubmed/35296197
http://dx.doi.org/10.1080/14756366.2022.2051023
Descripción
Sumario:A series of sulfamide fragments has been synthesised and investigated for human carbonic anhydrase inhibition. One of the fragments showing greater selectivity for cancer-related isoforms hCA IX and XII was co-crystalized with hCA II showing significant potential for fragment periphery evolution via fragment growth and linking. These opportunities will be identified in the future via the screening of this fragment structure for co-operative carbonic anhydrase binding with other structurally diverse fragments. [Figure: see text]

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