AI Article Synopsis
- A series of thirteen cyclic sulfonyl guanidines were developed and tested for their effectiveness against tumor-associated hCA IX and hCA XII isoforms, with minimal activity against off-target isoforms hCA I and hCA II.
- All tested compounds showed moderate inhibition of the target isoforms, with K values ranging from 0.57 to 8.4 µM for hCA IX and 0.34 to 9.7 µM for hCA XII.
- Due to their selectivity towards the target isoforms, these compounds hold potential as starting points for creating more effective antitumor treatments.
Article Abstract
A series of thirteen cyclic sulfonyl guanidines were prepared and evaluated against tumor-associated human (h) carbonic anhydrase (CA, EC 4.2.1.1) isoforms hCA IX and hCA XII, as well as against off-target cytosolic isoforms hCA I and hCA II. The compounds reported here were generally inactive against both off-target isoforms (K>100 μM), while all of them moderately inhibited both target isoforms hCA IX and XII in the submicromolar to micromolar ranges in which K values spanned from 0.57 to 8.4 μM against hCA IX and from 0.34 to 9.7 against hCA XII. Due to the notable selectivity of the title compounds toward isoforms hCA IX and XII, they can be considered as useful scaffolds for further chemical optimization to develop new highly selective antitumor agents.
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| http://dx.doi.org/10.1002/cmdc.202400197 | DOI Listing |
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