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Carbonic anhydrase inhibitors based on sorafenib scaffold: Design, synthesis, crystallographic investigation and effects on primary breast cancer cells. | LitMetric

AI Article Synopsis

  • Carbonic anhydrase inhibitors (CAIs) from sulfonamide, sulfamate, and coumarin classes, similar to Sorafenib, a drug for liver cancer, were studied for their effects on various human carbonic anhydrase isoforms.
  • Several sulfonamide compounds were found to selectively inhibit the hCA IX isoform, demonstrating very low inhibition constants (K values of 0.7-30.2 nM).
  • The research also included X-ray crystallography to analyze how these compounds bind to hCA I and tested the anticancer effects of certain sulfamates on breast cancer cells.

Article Abstract

Carbonic anhydrase inhibitors (CAIs) of the sulfonamide, sulfamate and coumarin classes bearing the phenylureido tail found in the clinically used drug Sorafenib, a multikinase inhibitor actually used for the management of hepatocellular carcinomas, are reported. All compounds were assayed on human (h) CA isoforms I, II, VII and IX, involved in various pathologies. Among the sulfonamides, several compounds were selective for inhibiting hCA IX, with K values in the low nanomolar ranges (i.e. 0.7-30.2 nM). We explored the binding modes of such compounds by means of X-ray crystallographic studies on isoform hCA I in adduct with one sulfonamide and a sulfamate inhibitor. Antiproliferative properties of some sulfamates on breast tumor cell lines were also investigated.

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Source
http://dx.doi.org/10.1016/j.ejmech.2019.111600DOI Listing

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