Aim: To develop anti-cancer active pharmaceutical intermediates.
Background: Acridone derivatives possess a wide range of pharmacological activities: 1) they intercalate DNA
and 2) form a covalent bond with DNA.
Objective: To screen in vitro anti-cancer activity against Cdc25b and SHP1 of new acridone derivatives and preliminary
study on the structure-activity relationship.
Materials and Methods: The synthesis of new acridone derivatives and in vitro evaluation of their anti-cancer
activity on Cdc25b and SHP1 was achieved. Natural products that contain acridine structures, such as cystodytin
A and acronycine, are isolated from certain marine (tunicates & ascidians, sponges, sea anemones) and plant
(bark of Australian scrub ash tree) species. Herein, we report the efficient one-pot green synthesis of twelve novel
3,4-dihydro-1 (2H) acridone derivatives, using montmorillonite K10 as the catalyst and iron/citric acid in water.
Also, their inhibitory activity against Cdc25B and SHP1 is examined, in which specific derivatives show enhanced
inhibitory activity compared to others.
Results and Discussion: Twelve new acridone derivatives were prepared, starting from 2-nitrobenzaldehyde derivatives
and 1, 3-cyclohexanedione derivatives, which exhibited substantial anti-cancer activity against Cdc25b
and SHP1 cells.
Conclusion: Preliminary studies on the structure-activity relationship have shown the influence of the structural
parameters and, in particular, the nature of the substituent on aromatic ring structure and cyclohexanone.
Other: Further study on the structure-activity relationship is required.