Pyridazinopsoralens of wide chemotherapeutic interest

Bioorganic & Medicinal Chemistry
2010.0

Abstract

The synthesis of new 6,10-dimethylpyridazino[4,5-h]psoralens, carrying no (4), one (5), or two (6-9) dialkylaminoalkylcarboxamide side chains on the pyridazine ring is reported. All compounds exert a significant photoantiproliferative activity. Moreover, the derivatives characterised by the protonable side chains show a notable cytotoxicity in the dark. The investigation on the mechanism of action demonstrated the capacity to intercalate into DNA base pairs and to inhibit the relaxation activity of topoisomerase II.

Knowledge Graph

Similar Paper

Pyridazinopsoralens of wide chemotherapeutic interest
Bioorganic & Medicinal Chemistry 2010.0
Antitumor Agents. 5. Synthesis, Structure−Activity Relationships, and Biological Evaluation of Dimethyl-5H-pyridophenoxazin-5-ones, Tetrahydro-5H-benzopyridophenoxazin-5-ones, and 5H-Benzopyridophenoxazin-5-ones with Potent Antiproliferative Activity
Journal of Medicinal Chemistry 2006.0
Benzothiopyranoindole-Based Antiproliferative Agents: Synthesis, Cytotoxicity, Nucleic Acids Interaction, and Topoisomerases Inhibition Properties
Journal of Medicinal Chemistry 2009.0
Synthesis and biological evaluation of N-substituted benzo[c]phenanthrolines and benzo[c]phenanthrolinones as antiproliferative agents
European Journal of Medicinal Chemistry 2011.0
Synthesis and evaluation of new 6-amino- substituted benzo[c]phenanthridine derivatives
Journal of Medicinal Chemistry 1993.0
Synthesis and antiproliferative activity of new cytotoxic azanaphthoquinone pyrrolo-annelated derivatives: Part II
Bioorganic & Medicinal Chemistry Letters 2011.0
Novel pyrazolo[3,4-d]pyrimidine with 4-(1H-benzimidazol-2-yl)-phenylamine as broad spectrum anticancer agents: Synthesis, cell based assay, topoisomerase inhibition, DNA intercalation and bovine serum albumin studies
European Journal of Medicinal Chemistry 2017.0
Structure−Activity Relationships for Pyrido-, Imidazo-, Pyrazolo-, Pyrazino-, and Pyrrolophenazinecarboxamides as Topoisomerase-Targeted Anticancer Agents
Journal of Medicinal Chemistry 2002.0
Novel imidazo[1,2-a]naphthyridinic systems (part 1): Synthesis, antiproliferative and DNA-intercalating activities
European Journal of Medicinal Chemistry 2008.0
Pyrroloquinolinone-based dual topoisomerase I/II inhibitor
European Journal of Medicinal Chemistry 2014.0