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One-Pot Green Synthesis of Acridine Alkaloid Derivatives and Screening of in vitro Anti-Cancer Activity Against Cdc25b and SHP1

Author(s):

Hao Li, Buer Song, Mamtimin Mahmut* and Mukhtar Imerhasan*   Pages 1 - 7 ( 7 )

Abstract:


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.

Keywords:

One-pot synthesis, in vitro anti-cancer activity, natural product analogs, Acridone, Alkaloid derivatives, Cdc25b, SHP1

Affiliation:

Key Laboratory of Energy Materials Chemistry, Ministry of Education; Key Laboratory of Advanced Functional Materials, Autonomous Region; Institute of Applied Chemistry, Urumqi Key Laboratory of Green Catalysis and Synthesis Technology, College of Chemistry, Xinjiang University, Urumqi, 830046, Xinjiang, Key Laboratory of Plant Resources and Chemistry in Arid Regions, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Science, Urumqi, 830011, Xinjiang, Key Laboratory of Energy Materials Chemistry, Ministry of Education; Key Laboratory of Advanced Functional Materials, Autonomous Region; Institute of Applied Chemistry, Urumqi Key Laboratory of Green Catalysis and Synthesis Technology, College of Chemistry, Xinjiang University, Urumqi, 830046, Xinjiang, Key Laboratory of Energy Materials Chemistry, Ministry of Education; Key Laboratory of Advanced Functional Materials, Autonomous Region; Institute of Applied Chemistry, Urumqi Key Laboratory of Green Catalysis and Synthesis Technology, College of Chemistry, Xinjiang University, Urumqi, 830046, Xinjiang



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