Insilico Design and Synthesis, Evaluation of Anti-Colon Cancer Activity of Novel Stilbene Hybrids

Abstract

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.