Effective synthesis of benzodiazepine sulfonamide-based MGAT2 inhibitors and evaluation of their antitumor activity†

This study synthesized benzodiazepine sulfonamide-based MGAT2 inhibitors to combat cancer recurrence and resistance. Despite modest effects, compounds 13 and 16 showed enhanced antitumor activity. The six-step synthesis method using amino acids is industrially viable, offering a basis for future drug development.