Design, Synthesis and Biological Evaluation of the Novel Antitumor Agent 5-Bromobenzofuran-3(2H)-One and its Derivatives

Aurones and auronols are naturally occurring 2-benzylidenebenzofuranone-3(2H)-one derivatives. Aurones have a limited occurrence in fruits, vegetables, and bright yellow color to flowers such as cosmos and coreopsis. Aurones possess a wide range of biolog

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Design, Synthesis, and Biological Evaluation of the Novel Antitumor Agent 5-Bromobenzofuran-3(2H)-One and its Derivatives Lei Lv, Xiaomin Zhang, Jian Lv, Yao Zhou, Weiguo Hu, Peng Yu, Hua Sun and Yuou Teng Abstract Aurones and auronols are naturally occurring 2-benzylidenebenzofuranone-3(2H)-one derivatives. Aurones have a limited occurrence in fruits, vegetables, and bright yellow color to flowers such as cosmos and coreopsis. Aurones possess a wide range of biological activities, such as antitumor, antifungal, phytoalexin, and so on. Some aurone derivatives have been studied as antitumor drug molecules, but 2-benzylidene-5-bromobenzofuranone-3(2H)-one series have not been reported yet. In this paper, we’d like to report the design, synthesis, and biological evaluation of the novel aurone derivatives. All the newly synthesized compounds were characterized by 1H NMR and their antitumor activities were evaluated by using MTT method in HT-29, K562, and HepG2 cell lines. 5-bromo-2-(4-nitrobenzylidene) benzofuran-3(2H)-one demonstrated good antitumor activity against K562 cells with an IC50 of 0.37 lM. Keywords Aurone derivatives

 Synthesis  Antitumor  MTT

L. Lv  X. Zhang  J. Lv  Y. Zhou  P. Yu  H. Sun  Y. Teng (&) Key Laboratory of Industrial Microbiology, Ministry of Education, College of Biotechnology, Tianjin University of Science and Technology, Tianjin 300457, People’s Republic of China e-mail: [email protected] L. Lv  X. Zhang  J. Lv  Y. Zhou  P. Yu  H. Sun  Y. Teng Tianjin Key Laboratory of Industry Microbiology, College of Biotechnology, Tianjin University of Science and Technology, Tianjin 300457, People’s Republic of China W. Hu North China Pharmaceutical Co. Ltd, Hebei 050015, People’s Republic of China

T.-C. Zhang et al. (eds.), Proceedings of the 2012 International Conference on Applied Biotechnology (ICAB 2012), Lecture Notes in Electrical Engineering 250, DOI: 10.1007/978-3-642-37922-2_88, Ó Springer-Verlag Berlin Heidelberg 2014

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88.1 Introduction Aurones, a class of flavonoids found in fruits and flowers [1], possess a lot of biological activities such as antitumor, antifungal, and phytoalexin [2–4]. Their occurrence in marine organisms has been recently reported [5]. Compared to flavones, the medicinal literature on aurones is in its infancy with trends and design are just now emerging [6, 7]. Cancer is a global public health problem. Cancer chemoprevention aimed at reducing the risk of cancer by avoiding exposure to cancer-causing agents, enhancing the host defense capacity, adjusting lifestyle, supplementing with chemopreventive agents that inhibit, reverse, or block tumorigenesis [8–10]. In clinical practice with the usage of anticancer drugs, the phenomenon of resistance gradually emerged, thus a tremendous effort will be made to enhance the intracellular accumulation of antitumor agents in resistant cells [11, 12]. Aurones are recently attracting the interest of an increasing number of research groups. In this paper, we report our works made on the

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