Following surgical resection of malignant gastrointestinal and gynecological tumors, such as advanced pancreatic cancer and ovarian cancer, implantation of shed cancer cells into the peritoneal cavity can lead to peritoneal carcinomatosis, which has a low incidence of survival. We have previously disclosed a series of amide analogs of BAY 11-7085 [(E)-3-(4-tert-butylphenylsulfonyl)acrylonitrile], a tool compound which has been shown to induce apoptosis of colon and pancreatic cells during cell adhesion. Herein, we disclose additional analogs from the amide series as well as bioisosteric replacements and other derivatives aimed at achieving improved in vivo efficacy. Results from two in vivo metastatic models will be presented for which new analogs demonstrate reductions in local recurrence and distal metastases.

Synthesis and in vivo assessment of arylsulfonyl acrylonitriles for the inhibition of peritoneal carcinomatosis

248th National Meeting (2014)

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