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Régis Millet Jean-François Goossens Karine Bertrand-Caumont Philippe Chavatte Raymond Houssin Jean-Pierre Hénichart 《Letters in Peptide Science》1999,6(4):221-233
Chemical modifications on the NK1 competitive antagonist L-732,138, with a view to creating a dual NK1/NK2 ligand, led to the tryptophan derivative 1 possessing the protected Gly-Leu sequence of the C-terminus of substance P and neurokinin A. Modifications in the nature of the carbamate function increased the selectivity for the NK1 receptor, whereas the inclusion of the indole moiety in -carboline or carbazole rings decreased the affinity for both receptors. Free indolylmethyl and Cbz carbamate groups were shown to be essential for NK2 affinity. 相似文献
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Millet Régis Goossens Jean-François Bertrand-Caumont Karine Chavatte Philippe Houssin Raymond Hénichart Jean-Pierre 《International journal of peptide research and therapeutics》1999,6(4):221-233
Summary Chemical modifications on the NK1 competitive antagonist L-732,138, with a view to creating a dual NK1/NK2 ligand, led to the tryptophan derivative 1 possessing the protected Gly-Leu sequence of the C-terminus of substance P and
neurokinin A. Modifications in the nature of the carbamate function increased the selectivity for the NK1 receptor, whereas the inclusion of the indole moiety in β-carboline or carbazole rings decreased the affinity for both receptors.
Free indolylmethyl and Cbz carbamate groups were shown to be essential for NK2 affinity. 相似文献
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《Journal of enzyme inhibition and medicinal chemistry》2013,28(2):308-315
AbstractThe present study reported the synthesis of tetrahydrocarbazoles hybridized with dithioate derivatives. Three series were synthesized namely alkyl dithiocarbonates (4a–d), heterocyclic dithiocarbamates (6a–g) and dialkyl dithiocarbamate (7). The synthesized compounds were tested in vitro on human breast adenocarcinoma cell line (MCF7) and the human colon tumor cell line (HCT116). Most of the synthesized compounds exploited potent antitumor activity, especially compound 6f [4-chlorophenylpiperazine derivative], which showed cytotoxic activity against MCF7 superior to doxorubicin with IC50 value of 7.24?nM/mL. 相似文献
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