Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 53, Issue 6, Pages 2622-2635Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm901868z
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Funding
- MIUR
- Cofinanziamento di Ateneo Universita di Pisa
- Compagnia di SanPaolo
- AIRC
- Minister della Salute
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Activated leukocyte cell adhesion molecule (ALCAM) plays a relevant role in tumor biology and progression. Our previous studies showed that ALCAM is expressed at the surface of epithelial ovarian cancer (EOC) cells and is released in a soluble form by ADAM-17-mediated shedding. This process is relevant to EOC cell motility and invasiveness, which is reduced by nonspecific inhibitors of ADAM-17. For this reason. ADAM-17 may represent a new useful target in anticancer therapy. Herein, we report the synthesis and biological evaluation of new ADAM-17 inhibitors containing an arylsulfonamidic scaffold. Among the new potential inhibitors, two very promising compounds 17 and 18 were discovered, with a nanomolar activity for ADAM-17 isolated enzyme. These compounds proved to be also the most potent in inhibiting soluble ALCAM release in cancer cells, showing a nanomolar activity on A2774 and SKOV3 cell lines.
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