CFTR activation in human bronchial epithelial cells by novel benzoflavone and benzimidazolone compounds

1 Laboratorio di Genetica Molecolare, Istituto Giannina Gaslini, 16148 Genova, Italy; 2 Departments of Medicine and Physiology, University of California, San Francisco 94143; and 3 Department of Chemistry, University of California, Davis, California 95616 Submitted 21 October 2002 ; accepted in final form 12 March 2003 Activators of the CFTR Cl - channel may be useful for therapy of cystic fibrosis. Short-circuit current ( I sc ) measurements were done on human bronchial epithelial cells to characterize the best flavone and benzimidazolone CFTR activators identified by lead-based combinatorial synthesis and high-throughput screening. The 7,8-benzoflavone UC CF -029 was a potent activator of Cl - transport, with activating potency (5 to