918335-87-2Relevant articles and documents
Synthesis of Novel Thymine-β-lactam Hybrids and Evaluation of Their Antitumor Activity
Piens, Nicola,De Vreese, Rob,De Neve, Nympha,Van Hecke, Kristof,Balzarini, Jan,De Kimpe, Norbert,D'Hooghe, Matthias
, p. 2436 - 2444 (2014)
Trimethylene-tethered thymine-β-lactam and thymine-bis-β-lactam chimeras were prepared as novel classes of hybrid systems through selective mono- or bis-N-alkylation of thymine with cis-1-(3-bromopropyl)-β-lactams. In addition, acidic methanolysis of the β-lactam nucleus in these systems provided an entry into the class of thymine-β-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.
A systematic study of nitrated indenoisoquinolines reveals a potent topoisomerase I inhibitor
Morrell, Andrew,Antony, Smitha,Kohlhagen, Glenda,Pommier, Yves,Cushman, Mark
, p. 7740 - 7753 (2006)
The biological activity of indenoisoquinoline topoisomerase I inhibitors is significantly enhanced by nitration of the isoquinoline ring. In the present study, nitrated analogues were synthesized with the indenone ring substituted with methoxy groups to f