| Literature DB >> 27234893 |
Nagwa M Abdel Gawad1, Noha H Amin2, Mohammed T Elsaadi3, Fatma M M Mohamed3, Andrea Angeli4, Viviana De Luca5, Clemente Capasso5, Claudiu T Supuran6.
Abstract
A series of 4-(thiazol-2-ylamino)-benzenesulfonamides was synthesized and screened for their carbonic anhydrase (CA, EC 4.2.1.1) inhibitory and cytotoxic activity on human breast cancer cell line MCF-7. Human (h) CA isoforms I, II and IX were included in the study. The new sulfonamides showed excellent inhibition of all three isoforms, with KIs in the range of 0.84-702nM against hCA I, of 0.41-288nM against hCA II and of 5.6-29.2 against the tumor-associated hCA IX, a validated anti-tumor target, with a sulfonamide (SLC-0111) in Phase I clinical trials for the treatment of hypoxic, metastatic solid tumors overexpressing CA IX. The new compounds showed micromolar inhibition of growth efficacy against breast cancer MCF-7 cell lines.Entities:
Keywords: Antitumor; Carbonic anhydrase; Cytotoxic agent; Inhibitor; Sulfonamide
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Year: 2016 PMID： 27234893 DOI： 10.1016/j.bmc.2016.05.016
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641