Novel Antitumor Precursor Of Color Derivatives Aiming Of DNA: Design, Synthesis And Evaluation Biological Activity

Several colors as 1,8-naphthalimide, porphyrin, and 1,8-dicyanonaphthalene created by our group which have excellent plane rigidity and plasticity, and are studied widely in biological field and conjugated π electron system has been chosen for our study. Some new DNA intercalators and antitumor precursors are synthesized by binding some biological active groups to the colors. Their spectral properties, DNA intercalative, DNA damaging abilities and the ability of the inducement of tumorous apoptosis are studied.21 naphthalimide or bisnaphthalimide compounds which are linked by isothiourea cations have been designed and synthesized. All the compounds are proved to have obvious injury to DNA and inducement of apoptosis by biological experiments. The fluorescent spectral of these compounds after intercalating to DNA are different from previous. The groups binding to the sulfur of isothiourea and the interchromophore chain make the difference of the intercalative activity, the DNA damaging ability and the ability of the inducement of tumorous apoptosis of these compounds. The former one take the major part in the two effects.The 5,10,15,20-tetrakis(4, -hydroxyphenyl)-porphyrin [T(4-OH P)P](THPP) has been synthesized by two steps. The compound whose purity has been higher than 97 percents is obtained at the scale of some decades compared to the milligram scale before. The efficiency has been improved by microwave heating. The abstraction and fluorescence of this compound turn out to be near to the infrared area and change in different solvents and different pH. The fluorescent spectral changes obviously after intercalate to DNA.Two compounds 3-3-nitro-acenaphthenequinone(3-NAD) and3-nitro-dicyanonaphthalene (3-NCN) has been synthesized and both of them are excellent photosensitive DNA cleaver.