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CuSO4/sodium ascorbate catalysed synthesis of benzosuberone and 1,2,3-triazole conjugates: Design, synthesis and in vitro anti-proliferative activity
Journal of Saudi Chemical Society ( IF 5.6 ) Pub Date : 2019-05-11 , DOI: 10.1016/j.jscs.2019.05.002
CH.B. Praveena Devi , K. Vijay , B. Hari Babu , Syed Farooq Adil , M. Mujahid Alam , M. Vijjulatha , Mohd. Bismillah Ansari

A novel series of conjugates of benzosuberone and 1,2,3-triazole i.e. 3-(4-phenyl-1H-1,2,3-triazol-1-yl)propyl-9-chloro-2,3-dimethyl-6,7-dihydro-5H-benzo[7]annulene-8-carboxylic acids (8a-j) were synthesized in good to excellent yields catalysed by CuSO4 under milder reaction conditions and evaluated for their anti-proliferative activity. The structural elucidation of the prepared compounds was carried out using IR, 1H NMR, 13C NMR and Mass spectral analysis. The newly synthesized derivatives (8a-j) were evaluated for their anti-proliferative activity against four human cell lines and the novel derivatives showed moderate to excellent activity. The obtained results suggest that these compounds can be considered as new hits for anti-proliferative drug development programme and further SAR studies can help obtain better anticancer agents.



中文翻译:

CuSO 4 /抗坏血酸钠催化合成苯并亚砜和1,2,3-三唑共轭物:设计,合成及体外抗增殖活性

苯并亚砜和1,2,3-三唑的新型共轭物系列,即3-(4-苯基-1 H -1,2,3-三唑-1-基)丙基-9-氯-2,3-二甲基-在较温和的反应条件下,以CuSO 4催化以良好至极佳的产率合成了6,7-二氢-5 H-苯并[7]环戊烯-8-羧酸(8a-j),并评估了它们的抗增殖活性。使用IR,1 H NMR,13 C NMR和质谱分析进行制备的化合物的结构阐明。新合成的衍生物(8a-j)评估了它们对四种人类细胞系的抗增殖活性,并且该新型衍生物显示出中等至优异的活性。获得的结果表明,这些化合物可被视为抗增殖药物开发计划的新热点,进一步的SAR研究可帮助获得更好的抗癌药。

更新日期:2019-05-11
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