2. Academic Validation
  3. Synthesis, antitumor evaluation and DNA photocleaving activity of novel methylthiazonaphthalimides with aminoalkyl side chains

Synthesis, antitumor evaluation and DNA photocleaving activity of novel methylthiazonaphthalimides with aminoalkyl side chains

  • Bioorg Med Chem Lett. 2005 Jun 15;15(12):3143-6. doi: 10.1016/j.bmcl.2005.04.012.
Zhigang Li 1,  Qing Yang,  Xuhong Qian
Affiliations

Affiliation

  • 1 State Key Lab. of Fine Chemicals, Dalian University of Technology, PO Box 158, Zhongshan Road, Dalian 116012, China.
PMID: 15876532 DOI: 10.1016/j.bmcl.2005.04.012
Abstract

A series of methylthiazonaphthalimides was synthesized and quantitatively evaluated as efficient DNA intercalators, antitumor agents and DNA photocleavers. A(1) showed both efficient antitumor activities against cell lines of A549 and P388 with IC50 of 82.8 and 31 nM, respectively. A(3) was the strongest antitumor agent against A549 with the IC50 of 20.8 nM. A(2), the most efficient DNA intercalator, was found to be the strongest DNA photocleaver via superoxide anion. An explanation was given for the disaccord between antitumor and DNA photocleaving activities.

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