Various biologically important Stilbene analogues were competently synthesized using inexpensive, non-toxic, and readily available amino acids and Stilbene; the systematic study was carried out to characterize parameters such as TLC, melting point, IR, 1H NMR and mass spectral studies. The synthesized compounds were screened for anticancer activities. The molecular docking studies have been performed by using software Autodock 4.2, Autodock vina. The targeted proteins are P450a2 & Estrogen. The reaction of phenylacetic acid substituted Benzaldehyde, and triethylamine in acetic anhydride was irradiated in a microwave oven for 3 minutes at 700W afforded (2E)-3-(substituted phenyl)-2-phenylacrylic acid. The above compound, after irradiating with hydrazine provided (2E)-3-(substituted phenyl)-2-phenyl acrylic acid hydrazide. Anti-Cancer activity for synthesized compounds was evaluated using the MTT assay technique against colon cancer. The results were obtained as a percentage in cell lysis data. The IC50 value of the compounds was between 0.037-0.0257 µM/lt. Among all the compounds, tyrosine derivatives exhibited the more potent activity. Insilico studies PCB-arg having more binding affinity with the receptor Cytochrome P450 A2 and PCB-try having more binding affinity with the receptor estrogen beta when compared to other derivatives.
A simple, rapid, precise, sensitive, and reproducible reverse-phase high-performance liquid chromatography (RPHPLC) LCMS/MS method has been developed for the bioanalytical method for Selinexor with D6-Selinexor as Internal Standard in the pharmaceutical dosage form. Chromatographic separation of Selinexor was achieved on Waters Alliance-e2695, by using X-Bridge phenyl, 150x4.6mm, 3.5μm column, and the mobile phase containing 0.1% Formic acid & Acetonitrile in the ratio of 80:20% v/v. The flow rate was 1.0 ml/min; detection was carried out by absorption at 225nm using a photodiode array detector at ambient temperature. The method was validated to fulfill International Conference on Harmonization (ICH) requirements and this validation included specificity, selectivity, matrix effect, linearity, the limit of detection (LOD), limit of quantification (LOQ), precision, and accuracy. The proposed method was Bio-analytical validated according to USFDA guidelines. This method was found to be a very simple, economical, suitable, precise, accurate, and stable method for pharmacokinetic analysis of Selinexor and study of its stability. The calibration curve was linear over the concentration range from 0 to 40 ng/ml, and the lower limit of detection of 12.5 ng/ml. The accuracy and precision of the method were within the acceptable limit of ±20% at the lower limit of quantitation and ±15% at other concentrations. Selinexor was unstable at room temperature it showed more than 25% loss after 24 h. While, Selinexor is very stable at refrigerator 40C auto-sampler, freeze/thaw cycles, and 30 days storage in a freezer at 35 ± 20C. All results were acceptable and this confirmed that the method is suitable for its intended use in routine quality control and an assay of drugs.
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