Synthesis And Conditions Studies Of Galaxamide Analogues

For nearly 30 years,from the ocean bacteria,sea squirts,seaweed and other Marine creatures have been isolated many of the Marine cyclic peptide compounds,most of these cyclic peptide is of unique chemical structure and biological activity.The research from the Xisha islands in the south China sea Galaxaura Filamentosa algae have been isolated by the Galaxamide is a three leucine and two N-a new type of methyl leucine ring five peptides.The structure is simple but is unique,and to a wide variety of tumor cells present good physiological activity characteristic.This paper using classical "3 + 2" methods,to improve discusses D,L configuration to the influence of the Galaxamide physiological activity.To leucine as the starting material,design and synthesis of the two new Galaxamide analogues C-1,C-2,a total of 18 compounds synthesized.This paper also produced in has not seen the reports in the literature of the nine new compounds in cytotoxic activity screening.The selected tumor cell lines A549 cells for lung cancer,cervical cancer Hela cells,breast cancer MCF-7 cells and HepG2 liver cancer.The results show that these compounds have certain physiological activity,especially contains D configuration of small molecules can show good cytotoxic activity.Synthetic matrix for the next Galaxamide coordination study to prepare,and statistics and summary of synthetic route reaction conditions on the influence of the Galaxamide synthesis,optimize the synthetic route improve production rate.Try to use the Galaxamide small fragments on the research coordination intermediates,so as to obtain the ocean coordination compounds.