.1. Tyrosine Protein Kinase Inhibitor Design And Synthesis. Are Butylphthalide The Analogues And Rearrangement Reactions

Tyrosine Protein Kinases (TPK) constitute a family of enzymes that catalyze the transfer of phosphate from ATP to the hydroxyl group of tyrosine residue on many key proteins. Spesific inhibitor of tyrosine protein kinases may be not only useful in investigating the mechanism of carcinogenesis, cell proliferation and differentiation, but also effective in prevention and chemotherapy of cancer. TPK inhibitors may act as a valuable research tool for elucidating the biological function of tyrosine kinases in cell. In this paper, we designed and synthesized five classes of compounds with the following structural characteristics: a conjugation system in the target molecule, hetero-atoms at the two ends and generally, 1-2 hydroxyl groups on a benzene ring. Some of the compounds were evaluated with part of them having evident inhibiting activity. The structure-activity relationship was also disscussed. This study will be of value for the further design of TPK inhibitors.Another project was also carried out. Several analogues of 3-butyl phthalide were synthesized. In our attempts to introduce an ethyl group in the C-6 position of 3-butyl phthalide by means of Friedel-Crafts reaction, no desired product was found but an unexpected rearrangement compound was obtained instead. Its structure was established by MS, ¹HNMR, ¹³CNMR and elemental analysis. The possible...