Synthesis and Structure−Activity Relationships of 2-Amino-1-aroylnaphthalene and 2-Hydroxy-1-aroylnaphthalenes as Potent Antitubulin Agents
G. Randheer ReddyDivision of Biotechnology and Pharmaceutical Research, National Health Research Institutes, No. 35, Keyan Road, Zhunan Town, Miaoli County 350, Taiwan, Republic of China, National Institute of Cancer Research, National Health Research Institutes, Tainan 704, Taiwan, ROC, Department of Chemical and Materials Engineering, Technology and Science Institute of Northern Taiwan, Taipei 112, Taiwan, ROC, Division of Hematology/Oncology, Department of Internal Medicine, National Cheng Kung University Hospital,Ching‐Chuan KuoDivision of Biotechnology and Pharmaceutical Research, National Health Research Institutes, No. 35, Keyan Road, Zhunan Town, Miaoli County 350, Taiwan, Republic of China, National Institute of Cancer Research, National Health Research Institutes, Tainan 704, Taiwan, ROC, Department of Chemical and Materials Engineering, Technology and Science Institute of Northern Taiwan, Taipei 112, Taiwan, ROC, Division of Hematology/Oncology, Department of Internal Medicine, National Cheng Kung University Hospital,Uan‐Kang TanDivision of Biotechnology and Pharmaceutical Research, National Health Research Institutes, No. 35, Keyan Road, Zhunan Town, Miaoli County 350, Taiwan, Republic of China, National Institute of Cancer Research, National Health Research Institutes, Tainan 704, Taiwan, ROC, Department of Chemical and Materials Engineering, Technology and Science Institute of Northern Taiwan, Taipei 112, Taiwan, ROC, Division of Hematology/Oncology, Department of Internal Medicine, National Cheng Kung University Hospital,Mohane Selvaraj CoumarDivision of Biotechnology and Pharmaceutical Research, National Health Research Institutes, No. 35, Keyan Road, Zhunan Town, Miaoli County 350, Taiwan, Republic of China, National Institute of Cancer Research, National Health Research Institutes, Tainan 704, Taiwan, ROC, Department of Chemical and Materials Engineering, Technology and Science Institute of Northern Taiwan, Taipei 112, Taiwan, ROC, Division of Hematology/Oncology, Department of Internal Medicine, National Cheng Kung University Hospital,Chi‐Yen ChangDivision of Biotechnology and Pharmaceutical Research, National Health Research Institutes, No. 35, Keyan Road, Zhunan Town, Miaoli County 350, Taiwan, Republic of China, National Institute of Cancer Research, National Health Research Institutes, Tainan 704, Taiwan, ROC, Department of Chemical and Materials Engineering, Technology and Science Institute of Northern Taiwan, Taipei 112, Taiwan, ROC, Division of Hematology/Oncology, Department of Internal Medicine, National Cheng Kung University Hospital,Yi‐Kun ChiangDivision of Biotechnology and Pharmaceutical Research, National Health Research Institutes, No. 35, Keyan Road, Zhunan Town, Miaoli County 350, Taiwan, Republic of China, National Institute of Cancer Research, National Health Research Institutes, Tainan 704, Taiwan, ROC, Department of Chemical and Materials Engineering, Technology and Science Institute of Northern Taiwan, Taipei 112, Taiwan, ROC, Division of Hematology/Oncology, Department of Internal Medicine, National Cheng Kung University Hospital,Mei-Jung LaiDivision of Biotechnology and Pharmaceutical Research, National Health Research Institutes, No. 35, Keyan Road, Zhunan Town, Miaoli County 350, Taiwan, Republic of China, National Institute of Cancer Research, National Health Research Institutes, Tainan 704, Taiwan, ROC, Department of Chemical and Materials Engineering, Technology and Science Institute of Northern Taiwan, Taipei 112, Taiwan, ROC, Division of Hematology/Oncology, Department of Internal Medicine, National Cheng Kung University Hospital,Jiann‐Yih YehDivision of Biotechnology and Pharmaceutical Research, National Health Research Institutes, No. 35, Keyan Road, Zhunan Town, Miaoli County 350, Taiwan, Republic of China, National Institute of Cancer Research, National Health Research Institutes, Tainan 704, Taiwan, ROC, Department of Chemical and Materials Engineering, Technology and Science Institute of Northern Taiwan, Taipei 112, Taiwan, ROC, Division of Hematology/Oncology, Department of Internal Medicine, National Cheng Kung University Hospital,Su‐Ying WuDivision of Biotechnology and Pharmaceutical Research, National Health Research Institutes, No. 35, Keyan Road, Zhunan Town, Miaoli County 350, Taiwan, Republic of China, National Institute of Cancer Research, National Health Research Institutes, Tainan 704, Taiwan, ROC, Department of Chemical and Materials Engineering, Technology and Science Institute of Northern Taiwan, Taipei 112, Taiwan, ROC, Division of Hematology/Oncology, Department of Internal Medicine, National Cheng Kung University Hospital,Jang‐Yang ChangDivision of Biotechnology and Pharmaceutical Research, National Health Research Institutes, No. 35, Keyan Road, Zhunan Town, Miaoli County 350, Taiwan, Republic of China, National Institute of Cancer Research, National Health Research Institutes, Tainan 704, Taiwan, ROC, Department of Chemical and Materials Engineering, Technology and Science Institute of Northern Taiwan, Taipei 112, Taiwan, ROC, Division of Hematology/Oncology, Department of Internal Medicine, National Cheng Kung University Hospital,Jing‐Ping LiouDivision of Biotechnology and Pharmaceutical Research, National Health Research Institutes, No. 35, Keyan Road, Zhunan Town, Miaoli County 350, Taiwan, Republic of China, National Institute of Cancer Research, National Health Research Institutes, Tainan 704, Taiwan, ROC, Department of Chemical and Materials Engineering, Technology and Science Institute of Northern Taiwan, Taipei 112, Taiwan, ROC, Division of Hematology/Oncology, Department of Internal Medicine, National Cheng Kung University Hospital,Hsing‐Pang HsiehDivision of Biotechnology and Pharmaceutical Research, National Health Research Institutes, No. 35, Keyan Road, Zhunan Town, Miaoli County 350, Taiwan, Republic of China, National Institute of Cancer Research, National Health Research Institutes, Tainan 704, Taiwan, ROC, Department of Chemical and Materials Engineering, Technology and Science Institute of Northern Taiwan, Taipei 112, Taiwan, ROC, Division of Hematology/Oncology, Department of Internal Medicine, National Cheng Kung University Hospital,
2008en
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Annotatsiya
A series of aroylnaphthalene derivatives were prepared as bioisosteres of combrestatin A-4 and evaluated for anticancer activity. 2-Amino-1-aroylnaphthalene and 2-hydroxy-1-aroylnaphthalene, 9 and 8, respectively, showed strong antiproliferative activity with IC(50) values of 2.1-26.3 nM against a panel of human cancer cell lines including multiple-drug resistant cell line. Compound 9 demonstrated better antiproliferative activity and has a comparable tubulin binding efficacy as that of colchicine.
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