Substituted spirooxindoles

US9822128B1 · kind B1 · utility

Inventors

• Assem Barakat · Riyadh, SA
• Mohammad Shahidul Islam · Riyadh, SA
• Abdullah Mohammed Al Majid · Riyadh, SA
• Hussain Mansur Ghawas · Riyadh, SA
• Fardous F. El-Senduny · Riyadh, SA
• Farid A. Badria · Riyadh, SA
• Yaseen Ali Mosa Mohamed Elshaier · Riyadh, SA
• Hazem Ahmed Ghabbour · Riyadh, SA

Key dates

• Filing date: Jun 1, 2017
• Grant date: Nov 21, 2017
• Expiry date: Jun 1, 2037

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D513/20
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The substituted spirooxindoles are MDM2-p53 inhibitors bearing a benzylidine (styryl) arm and have a complex fused ring system ideally suited for binding to the MDM2 protein, thereby interrupting its protein-protein interaction (PPI). Sixteen compounds, designated 4a-4p, were synthesized in a simple smooth method using an asymmetric 1,3-dipolar reaction as the key step. Testing showed that the compounds exhibit anti-cancer activity against various forms of cancer cells affecting humans.