13586-10-2Relevant academic research and scientific papers
NO donor compounds, compositions, preparation method and application thereof
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, (2019/11/13)
The object of the present invention is to provide NO donor compounds, compositions, a preparation method and application thereof. The compounds and the compositions show high anticancer activity in in-vitro anticancer activity tests, and have inhibitory a
C-7 modified flavonoids as novel tyrosyl-tRNA synthetase inhibitors
Xiao, Zhu-Ping,Wei, Wei,Liu, Qi,Wang, Peng-Fei,Luo, Xing,Chen, Fang-Yuan,Cao, Yang,Huang, Hong-Xia,Liu, Mi-Mi,Zhu, Hai-Liang
, p. 6193 - 6201 (2017/02/05)
Twenty C-7 modified flavonoids were designed and synthesized. Biological evaluation in vitro indicated that compounds generated by SYBYL-X with high scores also showed good inhibitory activities against TyrRS. Compounds containing the nargenin core exhibi
Novel daidzein analogs and their in vitro anti-influenza activities
Chung, Shu-Ting,Huang, Yi-Ting,Hsiung, Hsin-Yi,Huang, Wen-Hsin,Yao, Chen-Wen,Lee, An-Rong
, p. 685 - 696 (2015/04/27)
A series of novel isoflavonoids were synthesized based on structural modifications of daidzein, an active ingredient of traditional Chinese medicine (TCM) and evaluated for their anti-influenza activity, in vitro, against H1N1 Tamiflu-resistant (H1N1 TR) virus in the MDCK cell line. Among them, 4-oxo-4H-1-benzopyran-8-carbaldehydes 11a-11g were most promising, and they demonstrated better activities and selectivities comparable to those the reference ribarivin, a nucleoside antiviral agent. 3-(4-Bromophenyl)-7-hydroxy-4-oxo-4H-1-benzopyran-8-carboxaldehyde (11c) displayed the best inhibitory activity (EC50, 29.0 μM) and selectivity index (SI>10.3). Analysis of the structure£activity relationships (SAR) indicated that both the non-naturally-occurring Br-substituted B-ring and appropriate CHO and OH groups on the A-ring might be critical for the activity and selectivity against H1N1 TR influenza viruses.
Synthesis of haptens and conjugates for ELISAs of phytoestrogens. Development of the immunological tests
Bennetau-Pelissero, Catherine,Le Houerou, Cyril,Lamothe, Valerie,Le Menn, Francoise,Babin, Pierre,Bennetau, Bernard
, p. 305 - 311 (2007/10/03)
Seven carboxylic acid haptens of isoflavonoids were synthesized, with the spacer arm on the oxygen atom at the C7 position for one series, with formononetin, daidzein, equol, biochanin A, and genistein, and at the C8 position for a second series, with only formononetin and daidzein. The different haptens were coupled to bovine serum albumin (BSA) and to swine thyroglobulin (Thyr). Polyclonal antibodies were generated against the BSA conjugates. Enzyme-linked immunosorbent assays (ELISAs) were developed based on competition between free phytoestrogens and the Thyr-hapten conjugates for specific antibodies. IC50 values of the standard curves ranged between 0.8 and 20 ng/mL that is, 0.3 and 9.2 pmol/well. The antibodies obtained should be useful for assays in vegetable matter as well as in biological fluids after a separation step. These ELISAs should be valuable also in the food industry to control phytoestrogen concentrations prior to and after processing.
