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• 487-49-0 1-(2,4-dihydroxyphenyl)-2-(4-methoxyphenyl)ethanone 
• 485-72-3 7-Hydroxy-3-(4-methoxy-phenyl)-chromen-4-on 
• 105-39-5 chloroacetic acid ethyl ester 
• 108-46-3 recorcinol 
• 104-47-2 p-methoxybenzylnitrile 
• 105-36-2 ethyl bromoacetate 

Relevant academic research and scientific papers

C-7 modified flavonoids as novel tyrosyl-tRNA synthetase inhibitors

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

Synthesis, characterization and biological evaluation of formononetin derivatives as novel EGFR inhibitors: Via inhibiting growth, migration and inducing apoptosis in breast cancer cell line

Over the past few decades, the human epidermal growth factor receptor (EGFR) has been established as an attractive target for non-small cell lung cancer (NSCLC) therapy. Nevertheless, the approved EGFR inhibitors, gefitinib or erlotinib have shown minimum clinical activity to breast cancer patients, who also highly expressed EGFR. In this study, we designed and synthesized a series of novel formononetin derivatives by reference to the binding mode of lapatinib to EGFR. In vitro EGFR and cell growth inhibition assay demonstrated that compound 4v exhibited the most potent anti-EGFR (IC50 = 14.5 nM) and anti-proliferation activity (IC50 = 5.44 ± 1.28 μM) against MDA-MB-231 cell line, which was comparable to that of lapatinib (EGFR, IC50 = 5.6 nM; MDA-MB-231, IC50 = 2.48 ± 1.04 μM). Further biological experiment results demonstrated that 4v could effectively induce apoptosis, inhibit proliferation and migration in MDA-MB-231 cells through targeting EGFR and then blocking the downstream signaling pathways, EGFR/PI3K/Akt/Bad, EGFR/ERK and EGFR/PI3K/Akt/β-catenin, respectively. However, it had no significant influence on cell cycle distribution and the related proteins (Cyclin A, Cyclin D1, CDK4) expression. In vivo anti-tumor results also preliminarily confirmed the effectiveness of 4v in tumor chemotherapy in mice and indicated its potential as a new EGFR inhibitor in the treatment of MDA-MB-231 malignant tumor.

Structural modification and antihypertensive activity study of formononetin derivatives

A series of formononetin derivatives with substituted benzyloxy groups on the 4′ position of isoflavone were designed and synthesized. Their vasodilative activities were evaluated by wire myograph system on isolated rat mesenteric arterial ring. The preli

Novel daidzein analogs and their in vitro anti-influenza activities

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

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.