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Synthesis and SAR of cis-1-Benzoyl-1,2,3,4-tetrahydroquinoline ligands for control of gene expression in ecdysone responsive systems

2003; Elsevier BV; Volume: 13; Issue: 11 Linguagem: Inglês

10.1016/s0960-894x(03)00317-2

1464-3405

Howard C. Smith, Caitlin K. Cavanaugh, Jennifer L. Friz, Christine S. Thompson, Jessica A. Saggers, Enrique L. Michelotti, Javier Garcia, Colin M. Tice,

bioluminescence and chemiluminescence research

A library of 35 cis-1-benzoyl-2-methyl-4-(phenylamino)-1,2,3,4-tetrahydroquinolines was prepared. The compounds bore various substitutuents on the benzoyl ring, at the 4-position of the phenylamino ring and at the 6-position of the tetrahydroquinoline ring. The compounds were assayed for their ability to cause expression of a reporter gene downstream of an ecdysone response element in a mammalian cell line engineered to express the ecdysone receptor from Aedes aegypti. In general, compounds with small lipophilic substituents at the meta and para-positions of the benzoyl ring and hydrogen or fluorine at the 4-position of the phenylamino ring and the 6-position of the tetrahydroquinoline ring were the most potent.