Small-molecule EGFR tyrosine kinase inhibitors for the treatment of cancer.

Introduction: EGFR has been implicated in various malignancies such as NSCLC, breast, head and neck, and pancreatic cancer. Numerous drugs have been developed in order to target the tyrosine domain of EGFR as an approach in cancer treatment.

Areas Covered: This article focuses on the different generations of EGFR tyrosine kinase inhibitors (TKIs).

Facile identification of dual FLT3-Aurora A inhibitors: a computer-guided drug design approach.

Computer-guided drug design is a powerful tool for drug discovery. Herein we disclose the use of this approach for the discovery of dual FMS-like receptor tyrosine kinase-3 (FLT3)-Aurora A inhibitors against cancer. An Aurora hit compound was selected as a starting point, from which 288 virtual molecules were screened.

3,5-Isoxazoles from alpha-bromo-pentafluorophenyl vinylsulfonates: synthesis of sulfonates and sulfonamides.

The regioselective 1,3-dipolar cycloaddition of alpha-bromo-pentafluorophenyl vinylsulfonate with nitrile oxides has been used to rapidly access a range of 3,5-isoxazoles which could be converted directly to their corresponding sulfonamides.