Quinolidene based monocarbonyl curcumin analogues as promising antimycobacterial agents: Synthesis and molecular docking study

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• 作者：Dnyaneshwar D. Subhedar^a ; Mubarak H. Shaikh^a ; Laxman Nawale^b ; Dhiman Sarkar^b ; Vijay M. Khedkar^b ; Bapurao B. Shingate^a ; ^{bapushingate@gmail.com}
• 关键词：Antitubercular activity ; Cytotoxicity ; Green protocol ; Knoevenagel condensation ; Molecular docking
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2017
• 出版时间：15 February 2017
• 年：2017
• 卷：27
• 期：4
• 页码：922-928
• 全文大小：1192 K
• 卷排序：27

文摘

A series of quinoline incorporated monocarbonyl curcumin analogues was efficiently synthesized using [HDBU][HSO4] as catalyst via Knoevenagel type condensation and evaluated for their in vitro antitubercular activity against Mycobacterium tuberculosis H37Ra (MTB) and Mycobacterium bovis BCG in dormant state. The analogues 3e, 3h, 4a and 4e exhibited very good antitubercular activity. The antiproliferative activity of the analogues against MCF-7, A549 and HCT-116 cell lines was evaluated using modified MTT assay and these compounds were found to be non-cytotoxic. Molecular docking study has been carried out against M. tuberculosis pantothenate synthetase (MTB PS) enzyme in an effort to enhance the understanding of their action as antitubercular agents. The potency, low cytotoxicity and selectivity of these analogues support them as valid leads for further optimization.