Synthesis and Bioactivity of Monocyclic beta-Lactams and 4-Thiazolidinones Derivatives Containing Acridinyl

文献类型： 外文期刊

第一作者： Mahsud, Liwayidin

作者： Mahsud, Liwayidin;Imerhasan, Mukhtar;Mahmud, Muhammad Amin;Helil, Setiwaldi;Liu Huajun

作者机构：

关键词： acridinyl;beta-lactam;thiazolidinone;synthesis;biological activity

期刊名称：CHINESE JOURNAL OF ORGANIC CHEMISTRY （ 影响因子：1.652； 五年影响因子：1.2 ）

ISSN： 0253-2786

年卷期： 2014 年 34 卷 6 期

页码：

收录情况： SCI

摘要： In this paper, 1-aryl-3-substituted-4-(9-acridinyl)azetidin-2-one derivatives L1 similar to L6 and 2-(9-acridinyl)-3-aryl-1,3-thiazolidin-4-one derivatives T1 similar to T3 were synthesized through [2+2] cycloaddition reaction and cyclocondensation reaction of N-(p-substitutedaryl)-C-(9-acridinyl)formaldimines Schiff base with ketene, which in situ generated from chloroacetyl chloride and benzyloxyacetyl chloride in the presence of triethylamine, and mercaptoacetic acid. The synthesized compounds have also been screened in vitro anticancer activities and the leukocyte common antigen activities. The results showed that the inhibitory activity of compound L4 is 79.4% on human tumor cell HL-60 (Leucocythemia), at the test concentration of 10 mu mol/L. The inhibitory activities of compounds L5, L6 and T3 on Cdc25B (Cell division cycle 25B) phosphatase are 80.64%, 99.75% and 99.34% at the test concentration of 20 mu g/mL, respectively. The inhibitory activities of compounds L6 and T3 on CD45 (leukocyte common antigen, LCA) protein tyrosine phosphatase A are 86.12% and 91.03% at the test concentration of 20 mu mol/mL, respectively. The structure-activity relationship of these compounds was investigated on the bases of bioassay experimental results of these compounds.

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