Details

Autor(en) / Beteiligte

• Abdel Gawad, Nagwa M.
• Amin, Noha H.
• Elsaadi, Mohammed T.
• Mohamed, Fatma M.M.
• Angeli, Andrea
• De Luca, Viviana
• Capasso, Clemente
• Supuran, Claudiu T.

Titel

Synthesis of 4-(thiazol-2-ylamino)-benzenesulfonamides with carbonic anhydrase I, II and IX inhibitory activity and cytotoxic effects against breast cancer cell lines

Ist Teil von

• Bioorganic & medicinal chemistry, 2016-07, Vol.24 (13), p.3043-3051

Ort / Verlag

England: Elsevier Ltd

Erscheinungsjahr

2016

Quelle

MEDLINE

Beschreibungen/Notizen

• [Display omitted] 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.