81831-69-8Relevant articles and documents
Hederagenin compound H-X with anti-lung cancer effect and preparation method and application thereof
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Paragraph 0045; 0046; 0118; 0119, (2020/04/17)
The invention provides a hederagenin compound H-X with an anti-tumor effect and a preparation method and application thereof. The structural general formula 1 is shown in the specifications. Most of the derivatives provided by the invention have obvious inhibition effects on tumor cells A549, MCF-7 and HepG2, and the compound hederagenin-2, 6-dimethylpyrazine (H-08) shows good selectivity betweentumors and normal conditions, especially on lung cancer A549 cells. The IC50 of the compound to A549, MCF-7, HepG2, MDCK and H9c2 is 3.45+/-0.59 muM, 8.73+/-1.49 muM, 8.71+/-0.38 muM, 14.11+/-0.04 muM, and 16.69+/-0.12 muM, the inhibition effect on A549 cells is similar to that of a positive drug cis-platinum (IC50 is 3.85+/-0.63 muM), but the toxicity on MDCK and H9c2 is obviously lower than thatof cis-platinum.
Compound with dual antagonistic activity of histamine receptor and application
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Paragraph 0043-0047, (2019/01/16)
The invention relates to the field of pharmaceutical chemistry and in particular relates to a class of compounds (I) with dual antagonistic activity of histamine H1 and H4 receptors. Pharmacodynamic experiments prove that the compounds disclosed by the invention have dual antagonistic effects of the histamine H1 and H4 receptors. The compounds disclosed by the invention have obvious anti-allergicactivity, can further inhibit inflammatory factor release and achieve anti-inflammatory actions.
(2,6)- and (2,5)Pyrazinophanes: Synthesis and Molecular Structure
Eiermann, Uwe,Krieger, Claus,Neugebauer, Franz A.,Staab, Heinz A.
, p. 523 - 533 (2007/10/02)
The title compounds 1-3 and their methyl derivatives 4-7 were synthesized either by photolytic sulfur extrusion from the corresponding 2,11-dithiapyrazinophanes 24-26 or by Hofmann 1,6-elimination of the appropriate trimethylammonium hydroxides followed by dimerization of the generated 2,5-dihydro-2,5-dimethylene-pyrazines. α-Chlorination of the methylpyrazines 8-10 with N-chlorosuccinimide gave the required precursors 11, 12, 14, 17, and 18.The results of the X-ray structure determinations for 1-4 and 7 which indicate an unequivocal isomer assignment are discussed with regard to steric strain in these molecules.The electronic spectra of the pyrazinophanes 1-7 are reported and compared with those of the parent methylpyrazines.