Synthesis of Novel Thymlne-p-Iaetam Hybrids and Evaluation of Their Anti-tumor Activity

摘要

Abstract: Trimethylene-tethered thymine-beta-lactam and thymine-bis-beta-lactam chimeras were prepared as novel classes of hybrid systems through selective mono- or bis-N-alkylation of thymine with cw-l-beta-bromopropyl)-beta-lactams. In addition, acidic methanolysis of the beta-lactam nucleus in these systems provided an entry into the class of thymine-P-amino ester hybrids. A selection of the newly synthesized hybrid compounds was assessed for their antiviral activity, cytotoxicity, and cytostatic activity, revealing a significant cytostatic effect of one of the derivatives against murine leukemia and human T-lymphocyte tumor cells.