Studies On Synthesis,properties And Antitumor Activities In Vitro Of Photosensitive System Of Novel Porphyrin-Chrysin Derivatives

Objective: For obtaining more efficient,low toxicity,good targeting potential antitumor drugs,we synthesized a new type of porphyrinchrysin derivatives,and then tested the performance and initial activity of the target compound to explore its antitumor activity in vitro.Methods: The project first synthesizes three types of suitable porphyrin molecules,and then uses a method of forming ether bonds with different lengths of carbon chain among porphyrin molecules and chrysin molecules to form a new class of porphyrin-chrysin derivatives.The structure of the compounds are confirmed by nuclear magnetic resonance spectroscopy,MS and UV-visible spectroscopy.The wavelength of the characteristic absorption peak is obtained by the detection of the fluorescence spectroscopy and UV-visible spectroscopy.To determine the singlet state of the compounds through the fluorescence intensity of DPBF at a specific wavelength that captures singlet oxygen(1O2).On the other hand,standard MTT assays are used to preliminarily investigate theantitumor activity of compounds in vitro;cell cycle assays and apoptosis assay are used to detect the cell cycle inhibition of human cervical cancer Hela cells.Results: A total of 23 novel antitumor compounds were synthesized and confirmed by 1H NMR,MS,UV-Vis spectroscopy and so on.These compounds have a strong ability to produce 1O2 through singlet oxygen detection.Compounds 2 series and 4 series showed better antitumor cell proliferation in vitro under light conditions.The compound 4a can significantly inhibit the G1 phase of Hela cells and lead to apoptosis.Conclusions: A series of novel porphyrin-chrysin derivatives have been successfully synthesized in this study.Compound 4a shows further research value through a series of performance tests and preliminary evaluation of human gastric cancer MGC-803 cells and human cervical cancer Hela cells proliferation in vitro of compounds.This topic provides a new direction for the in-depth study of antitumor compounds.