| Autor: |
Miguel F. Braña, M. Moran, J. M. Castellano, Emling F, N. Walker, Schlick E, Gerhard Klebe, M. Kluge |
| Rok vydání: |
2010 |
| Předmět: |
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| Zdroj: |
ChemInform. 27 |
| ISSN: |
0931-7597 |
| DOI: |
10.1002/chin.199615170 |
| Popis: |
New benz[d,e]isoquinoline-1,3-diones related to mitonafide (CAS 54824-17-8) and amonafide (CAS 69408-81-7) with double substitution on the chromophore and branched side chains have been synthesized and their biological activity determined. Molecular modeling studies of 3a based on X-ray crystallographic data of mitonafide have shown that the aromatic system intercalates between GC steps of DNA. The in vitro cytotoxic test data using CX-1 and LX-1 cells showed higher cytotoxic activities in disubstituted derivatives compared to both lead compounds. Some of the compounds have been selected for in vivo test using L1210 tumor cells and CX-1 cells. Two of them (3b and 3j) have shown promising activity as good candidates for clinical development. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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