2003
DOI: 10.1016/s0960-894x(03)00317-2
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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

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Cited by 69 publications
(31 citation statements)
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“…Of the eight analogues tested, one ( 48 ) showed agonist activity. THQ analogues were identified as ecdysone agonists in other reporter assays employing mammalian cells overexpressing the mosquito receptor as well as Drosophila S2 cells containing endogenous EcR/USP 8, 38, 39. Here it was shown that this class of analogues is not specific to the Diptera with respect to activation of the EcR/USP complex.…”
Section: Discussionmentioning
confidence: 92%
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“…Of the eight analogues tested, one ( 48 ) showed agonist activity. THQ analogues were identified as ecdysone agonists in other reporter assays employing mammalian cells overexpressing the mosquito receptor as well as Drosophila S2 cells containing endogenous EcR/USP 8, 38, 39. Here it was shown that this class of analogues is not specific to the Diptera with respect to activation of the EcR/USP complex.…”
Section: Discussionmentioning
confidence: 92%
“…The THQ [1‐aroyl‐4‐(arylamino)‐1,2,3,4‐tetrahydroquinoline] ligand class of ecdysone agonists was identified recently by the FMC Corporation using mammalian cell‐based assays expressing insect EcRs 39, 40. The authors also synthesised eight THQ analogues, including one related piperidinamine analogue ( 42 to 49 in Table 3), and submitted them to ecdysone‐dependent reporter assays.…”
Section: Resultsmentioning
confidence: 99%
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“…These in silico models helped to provide better fundamental insights in new ligand-receptor interactions allowing predictions for enhanced activities and new lead molecules. Three good examples from the recent years are: 3,5-di-tert-butyl-4hydroxy-N-iso-butyl-4-hydroxybenzamide (DTBHIB) (Mikitani 1996), tetrahydroquinoline [1-aryl-4-(arylamino)-1,2,3,4-tetrahydroquinoline], and α-acylaminoketone (Smith et al 2003;Tice et al 2003).…”
Section: Insect Cell Cultures In Screening For Novel Insecticide Actimentioning
confidence: 99%