Abstract
Several novel isoquino[4,5-bc]acridine derivatives have been designed and synthesized. Their DNA-binding, anti-tumor and DNA-photo-damaging properties were investigated. A4 exhibited the highest anti-tumor activities against both A 549 (human lung cancer cell) and P388 (murine leukemia cells). All these compounds were found to be more cytotoxic against P388 than against A549. Under 365-nm light irradiation, A3 damaged plasmid DNA pBR322 at <2 μM and cleaved DNA from form I to 100% form II by 50 μM. The mechanism studies revealed that A3 damaged DNA by electron transfer mechanism and singlet oxygen species.
| Original language | English |
|---|---|
| Pages (from-to) | 221-226 |
| Number of pages | 6 |
| Journal | Journal of Photochemistry and Photobiology B: Biology |
| Volume | 84 |
| Issue number | 3 |
| DOIs | |
| State | Published - 1 Sep 2006 |
| Externally published | Yes |
Keywords
- Acridine
- Anti-tumor activity
- DNA binding
- DNA photo-cleavage