Synthesis and biological evaluation of novel carbazolyl glyoxamides as anticancer and antibacterial agents
Synthesis and biological evaluation of novel carbazolyl glyoxamides as anticancer and antibacterial agents
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DOI：
10.1039/c5ra27175d
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发表时间：
2016-01-01
期刊：
影响因子：
3.9
通讯作者：
Kumar, Dalip
中科院分区：
文献类型：
--
作者：
Reddy, Venkataramana P. O.;Tantak, Mukund P.;Kumar, Dalip
以乙醛酸和芳胺为原料，HATU为偶联试剂，在微波辐射下合成了24个咔唑基乙二醛酰胺化合物14 a-x。对所合成的咔唑基乙二醛酰胺类化合物进行了体外抗癌和抗菌活性评价。在合成的咔唑基乙二醛酰胺中，化合物14 l和14 q对乳腺癌细胞系表现出最强的细胞毒性，IC 50值分别为9.3和9.8 μ M。此外，卡巴唑基乙二醛酰胺的半胱天冬酶-3测定表明，这些化合物诱导Jurkat细胞中的凋亡性细胞死亡。此外，一些合成的咔唑基乙二醛酰胺14 g、14 k、14 l和14 n对选定的细菌菌株表现出与氯霉素相当或甚至更好的抗菌活性（MIC - 8-16 μ g mL（-1））。
A new library of 24 carbazolyl glyoxamides 14a-x were designed and synthesized from glyoxalic acids and arylamines in the presence of HATU as a coupling reagent under MW irradiation. The synthesized carbazolyl glyoxamideswere evaluated for their in vitro anticancer and antibacterial activities. Of the synthesized carbazolyl glyoxamides, compounds 14l and 14q exhibited the most potent cytotoxicity towards a breast cancer cell line with IC50 values of 9.3 and 9.8 mu M, respectively. Further, caspase-3 assay for carbazolyl glyoxamides indicated that these compounds induced apoptotic cell death in Jurkat cells. Furthermore, some of the synthesized carbazolyl glyoxamides 14g, 14k, 14l and 14n exhibited comparable or even better antibacterial activity (MIC - 8-16 mu g mL(-1)) than chloramphenicol against the selected bacterial strains.