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

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

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

Cited by 70 publications

(31 citation statements)

References 14 publications

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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%

“…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. Among them, three compounds ( 46, 47 and 48 ) were capable of activating the mosquito ( Aedes aegypti L.) EcR at µ M concentrations in mammalian cell‐based assays 39…”

Section: Resultsmentioning

confidence: 99%

“…THQ compounds have been shown to activate the dipteran mosquito and fly EcRs 8, 39. Of the eight THQs tested, only 48 is active as agonist at a concentration of 100 µ M .…”

Section: Resultsmentioning

confidence: 99%

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Assessment of species specificity of moulting accelerating compounds in Lepidoptera: comparison of activity between Bombyx mori and Spodoptera littoralis by in vitro reporter and in vivo toxicity assays

et al. 2010

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Section: Discussionmentioning

confidence: 92%

Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

“…THQ compounds have been shown to activate the dipteran mosquito and fly EcRs 8, 39. Of the eight THQs tested, only 48 is active as agonist at a concentration of 100 µ M .…”

Section: Resultsmentioning

confidence: 99%

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Assessment of species specificity of moulting accelerating compounds in Lepidoptera: comparison of activity between Bombyx mori and Spodoptera littoralis by in vitro reporter and in vivo toxicity assays

et al. 2010

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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%

Insect cell culture and applications to research and pest management

Smagghe

Goodman

Stanley

2009

In Vitro Cell.Dev.Biol.-Animal

104

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Building on earlier research, insect cell culture began with the successful establishment of one cell line from pupal ovarian tissue. The field has grown to the extent that now over 500 insect cell lines have been established from many insect species representing numerous insect orders and from several different tissue sources. These cell lines are used as research tools in virology, in studies of signaling mechanisms to study insect immunity, hemocyte migration, and to test hypotheses about gene expression, and in screening programs designed to discover new insecticide chemistries. Virology research is revealing fundamentally new information on virus/host cell interactions. Studies in gene expression are uncovering signal transduction pathways that are new to insect science. Research is leading to the development of high-speed screening technologies that are essential in the search for new insect pest management tools. A few insect cell lines are, in routine industrial processes, designed to produce proteins of biomedical significance. Both primary cell cultures and established lines are used in basic biological studies to reveal how insect cells work. This review is designed to briefly cover the history of insect cell culture, recount some recent advances in the field, and offer a vision of the future of insect cell culture.

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m-Trifluoromethylbenzoyl Chloride

Dunlap

2005

Encyclopedia of Reagents for Organic Synthesis

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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

Cited by 70 publications

References 14 publications

Assessment of species specificity of moulting accelerating compounds in Lepidoptera: comparison of activity between Bombyx mori and Spodoptera littoralis by in vitro reporter and in vivo toxicity assays

Assessment of species specificity of moulting accelerating compounds in Lepidoptera: comparison of activity between Bombyx mori and Spodoptera littoralis by in vitro reporter and in vivo toxicity assays

Insect cell culture and applications to research and pest management

m-Trifluoromethylbenzoyl Chloride

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