Li Hao, Song Buer, Mahmut Mamtimin, Imerhasan Mukhtar
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, China.
Key Laboratory of Plant Resources and Chemistry in Arid Regions, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Science, Urumqi, 830011, Xinjiang, China.
Curr Org Synth. 2021;18(4):399-405. doi: 10.2174/1570179417666201228165500.
To develop anti-cancer active pharmaceutical intermediates.
Acridone derivatives possess a wide range of pharmacological activities: 1) they intercalate DNA and 2) form a covalent bond with DNA.
To screen in vitro anti-cancer activity against Cdc25b and SHP1 of new acridone derivatives and preliminary study on the structure-activity relationship.
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.
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.
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.
开发抗癌活性药物中间体。
吖啶酮衍生物具有广泛的药理活性：1）它们可嵌入DNA；2）与DNA形成共价键。
筛选新型吖啶酮衍生物对Cdc25b和SHP1的体外抗癌活性，并对构效关系进行初步研究。
实现了新型吖啶酮衍生物的合成及其对Cdc25b和SHP1的体外抗癌活性评估。从某些海洋生物（被囊动物和海鞘、海绵、海葵）和植物（澳大利亚灌丛灰树的树皮）物种中分离出含有吖啶结构的天然产物，如胱抑素A和山油柑碱。在此，我们报道了以蒙脱石K10为催化剂，在水中用铁/柠檬酸高效一锅法绿色合成12种新型3,4-二氢-1（2H）吖啶酮衍生物。此外，还检测了它们对Cdc25B和SHP1的抑制活性，其中某些特定衍生物的抑制活性比其他衍生物增强。
从2-硝基苯甲醛衍生物和1,3-环己二酮衍生物出发制备了12种新型吖啶酮衍生物，它们对Cdc25b和SHP1细胞表现出显著的抗癌活性。
对构效关系的初步研究表明了结构参数的影响，特别是芳香环结构和环己酮上取代基的性质的影响。其他：需要对构效关系进行进一步研究。
