Carboranylanilinoquinazoline EGFR-inhibitors: toward ‘lead-to-candidate’ stage in the drug-development pipeline

Marcos Couto, Catalina Alamón, Carina Sánchez, Belén Dávila, Marcelo Fernández, Nicole Lecot, Pablo Cabral, Francesc Teixidor, Clara Viñas & Hugo Cerecetto. FUTURE MEDICINAL CHEMISTRY. Vol. 11, No. 17.

Background: Carboranylanilinoquinazoline-hybrids, developed for boron neutron capture therapy, have demonstrated cytotoxicity against murine-glioma cells with EGFR-inhibition ability. In addition, their adequate aqueous/metabolic stabilities and ability to cross blood–brain barrier make them good leads as to become antiglioma drugs. 

Aim: Analyze drug-like properties of representative carboranylanilinoquinazolines. 

Materials & methods: To expand carboranylanilinoquinazolines therapeutic spectrum, we studied their ability to act against glioma-mammal cells, U-87 MG and other tyrosine kinase-overexpress cells, HT-29. Additionally, we predicted theoretically and studied experimentally drug-like properties, in other words, organization for economic cooperation and development-recommended toxicity-studies and, due to some aqueous-solubility problems, and vehicularization for oral and intravenous administrations. 

Conclusion: We have identified a promising drug-candidate with broad activity spectrum, appropriate drug-like properties, adequate toxicological behavior and able ability to be loaded in suitable vehicles.

Carboranylanilinoquinazoline EGFR-inhibitors: toward ‘lead-to-candidate’ stage in the drug-development pipeline

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