Aims:
To develop of anticancer active pharmaceutical intermediates.
Background: Acridone derivatives possesses wide range of pharmacological activities:1) intercalate DNA 2) form covalent
bond with DNA.
Objective:
To Screening of in vitro anticancer activity against Cdc25b and SHP1 of new acridone derivatives and preliminary study on structure-activity relationship.
Materials and Methods:
Synthesis of new acridone derivatives and in vitro evaluation of their anticancer activity on
Cdc25b and SHP1. 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:
Starting from 2-nitrobenzaldehyde derivatives and 1, 3-cyclohexanedione derivatives, twelve new
acridone derivatives were prepared and exhibited substantial anticancer activity against Cdc25b and SHP1 cells.
Conclusion:
Preliminary studies of 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 structure-activity relationship.
Indole-3-acetamides: As Potential Antihyperglycemic and Antioxidant Agents; Synthesis, In Vitro α-Amylase Inhibitory Activity, Structure–Activity Relationship, and In Silico Studies
