Synthesis and structure–affinity relationship of chlorinated pyrrolidinone-bearing benzenesulfonamides as human carbonic anhydrase inhibitors

[Display omitted] •Pyrrolidinone-bearing benzenesulfonamides with chlorine at position 3 were synthesized.•Compounds 12 and 15 exhibited low nanomolar dissociation constants for cancer-related isozyme CA IX.•Disulfonamide 3 was the most selective compound for CA II and exhibited 5 nM binding affinit...

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Veröffentlicht in:	Bioorganic chemistry 2020-04, Vol.97, p.103658-103658, Article 103658
Hauptverfasser:	Balandis, Benas, Ivanauskaitė, Guostė, Smirnovienė, Joana, Kantminienė, Kristina, Matulis, Daumantas, Mickevičius, Vytautas, Zubrienė, Asta
Format:	Artikel
Sprache:	eng
Schlagworte:	5-Oxopyrrolidine Antigens, Neoplasm - metabolism Benzenesulfonamide Benzenesulfonamides Biochemistry & Molecular Biology Carbonic anhydrase Carbonic Anhydrase Inhibitors - chemistry Carbonic Anhydrase Inhibitors - pharmacology Carbonic Anhydrase IX - antagonists & inhibitors Carbonic Anhydrase IX - metabolism Chemistry Chemistry, Organic Fluorescent thermal shift assay Halogenation Humans Life Sciences & Biomedicine Physical Sciences Pyrrolidinones - chemistry Pyrrolidinones - pharmacology Science & Technology Structure-Activity Relationship Structure-affinity relationship Sulfonamides - chemistry Sulfonamides - pharmacology
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