Distamycin Analogues Synthesis And Mass Spectrometry Law

Many research efforts have been aimed at targeting specific sequences in DNA reorganization with the idea of designing drugs for antiviral, antitumor and antibacterial activities by people. Some of these molecules form noncovalent complexes with DNA. While others DNA-binding compounds cause cleavages in the DNA backbone(such as distamycin derivatives). Some research testified that mustargen is effective in antitumor activities in modern pharmacody and clinical application. But nitrogen mustard drugs have very much damaging effect in normal cells. Now we must improve the selectivity of mustargen to get the application in clinical. Some people also find that the combination of the mustargen and other drugs matrix or carrier reduce the cytotoxic and improve the selectivity. So the combination of nitrogen mustard and other drugs is a new way in finding antitumor compounds. We want to design these compounds to get less cytotoxic drugs.In this article we design some compounds which consist of polyamide and amino acid methyl esters, mustargen-polyamide and amino acid methyl esters. We use N-methyl pyrrole as monomer to get the combination compounds, In this way we have synthesised twenty new compounds in total. Because both distamycin derivatives and nitrogen mustard have antitumor activities, the combination of them may produce activity compounds.In the process of synthesis, there are DCC/HOBt coupling reaction, Chloroform reaction, hydrogenation reaction used Pd-C as catalysts. The reaction condition is mild, the reaction time is short and the yield of many compounds is good. Some analysis tools and methods are very necessary in characterization of synthetic products, such as ¹H NMR, ¹³C NMR, Infrared spectroscopy, Electrospray ionization mass spectrometer (ESI-MS) and two-dimensional nuclear magnetic resonance spectra. Some conclusions can be get from a lot of data, they can be used as references to other analogues. For example, based on these conclusions it is very convenient to estimate how many N-methylpyrrole residues in one compound through ¹HNMR. Order of residues connection can be identified from fracture paths of compounds in electrospray ionization mass spectrometer.