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Aurora kinase inhibitor patents and agents in clinical testing: an update (2011 – 2013)

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Gurubasavaraja Swamy P. M.Nahid Abbas, Prasad Sanjay Dhiwar, Ekta Singh, Abhishek Ghara & Arka Das. (2023) Discovery of potential Aurora-A kinase inhibitors by 3D QSAR pharmacophore modeling, virtual screening, docking, and MD simulation studies. Journal of Biomolecular Structure and Dynamics 41:1, pages 125-146.
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Xue-Li Jing & Shi-Wu Chen. (2021) Aurora kinase inhibitors: a patent review (2014-2020). Expert Opinion on Therapeutic Patents 31:7, pages 625-643.
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Jonathan Elie, Omid Feizbakhsh, Nathalie Desban, Béatrice Josselin, Blandine Baratte, Amandine Bescond, Julien Duez, Xavier Fant, Stéphane Bach, Dominique Marie, Matthieu Place, Sami Ben Salah, Agnes Chartier, Sabine Berteina-Raboin, Apirat Chaikuad, Stefan Knapp, Fabrice Carles, Pascal Bonnet, Frédéric Buron, Sylvain Routier & Sandrine Ruchaud. (2020) Design of new disubstituted imidazo[1,2-b]pyridazine derivatives as selective Haspin inhibitors. Synthesis, binding mode and anticancer biological evaluation. Journal of Enzyme Inhibition and Medicinal Chemistry 35:1, pages 1840-1853.
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Sailu Sarvagalla, Hsing Pang Hsieh & Mohane Selvaraj Coumar. (2016) Therapeutic polymeric nanoparticles and the methods of making and using thereof: a patent evaluation of WO2015036792. Expert Opinion on Therapeutic Patents 26:7, pages 751-755.
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Xin Jin, Qingqing Mo, Yu Zhang, Yue Gao, Yuan Wu, Jing Li, Xing Hao, Ding Ma, Qinglei Gao & Pingbo Chen. (2016) The p38 MAPK inhibitor BIRB796 enhances the antitumor effects of VX680 in cervical cancer. Cancer Biology & Therapy 17:5, pages 566-576.
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Alberto Leoni, Alessandra Locatelli, Rita Morigi & Mirella Rambaldi. (2016) 2-Indolinone a versatile scaffold for treatment of cancer: a patent review (2008–2014). Expert Opinion on Therapeutic Patents 26:2, pages 149-173.
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Zhen Xing, Sai Gao, Yan Duan, Haobo Han, Li Li, Yan Yang & Quanshun Li. (2015) Delivery of DNAzyme targeting aurora kinase A to inhibit the proliferation and migration of human prostate cancer. International Journal of Nanomedicine 10, pages 5715-5727.
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Jin-Ping Li, Yin-Xue Yang, Qi-Lun Liu, Shu-Ting Pan, Zhi-Xu He, Xueji Zhang, Tianxin Yang, Xiao-Wu Chen, Dong Wang, Jia-Xuan Qiu & Shu-Feng Zhou. (2015) The investigational Aurora kinase A inhibitor alisertib (MLN8237) induces cell cycle G2/M arrest, apoptosis, and autophagy via p38 MAPK and Akt/mTOR signaling pathways in human breast cancer cells. Drug Design, Development and Therapy 9, pages 1627-1652.
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Articles from other publishers (35)

Antal H. Kovacs, Dong Zhao & Jinqiang Hou. (2023) Aurora B Inhibitors as Cancer Therapeutics. Molecules 28:8, pages 3385.
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Muhammad Usama Tariq, Muhammad Furqan, Hira Parveen, Rahim Ullah, Muhammad Muddassar, Rahman Shah Zaib Saleem, Vassilios Bavetsias, Spiros Linardopoulos & Amir Faisal. (2021) CCT245718, a dual FLT3/Aurora A inhibitor overcomes D835Y-mediated resistance to FLT3 inhibitors in acute myeloid leukaemia cells. British Journal of Cancer 125:7, pages 966-974.
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Ya-Hui Chi, Teng-Kuang Yeh, Yi-Yu Ke, Wen-Hsing Lin, Chia-Hua Tsai, Wan-Ping Wang, Yen-Ting Chen, Yu-Chieh Su, Pei-Chen Wang, Yan-Fu Chen, Zhong-Wei Wu, Jen-Yu Yeh, Ming-Chun Hung, Mine-Hsine Wu, Jing-Ya Wang, Ching-Ping Chen, Jen-Shin Song, Chuan Shih, Chiung-Tong Chen & Chun-Ping Chang. (2021) Discovery and Synthesis of a Pyrimidine-Based Aurora Kinase Inhibitor to Reduce Levels of MYC Oncoproteins. Journal of Medicinal Chemistry 64:11, pages 7312-7330.
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Lotte Eijkenboom, Callista Mulder, Bert van der Reijden, Norah van Mello, Julia van Leersum, Thessa Koorenhof-Scheele, Didi Braat, Catharina Beerendonk & Ronald Peek. (2021) Purging human ovarian cortex of contaminating leukaemic cells by targeting the mitotic catastrophe signalling pathway. Journal of Assisted Reproduction and Genetics 38:6, pages 1571-1588.
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Simone Punt, Shruti Malu, Jodi A. McKenzie, Soraya Zorro Manrique, Elien M. Doorduijn, Rina M. Mbofung, Leila Williams, Deborah A. Silverman, Emily L. Ashkin, Ana Lucía Dominguez, Zhe Wang, Jie Qing Chen, Sourindra N. Maiti, Trang N. Tieu, Chengwen Liu, Chunyu Xu, Marie-Andrée Forget, Cara Haymaker, Jahan S. Khalili, Nikunj Satani, Florian Muller, Laurence J. N. Cooper, Willem W. Overwijk, Rodabe N. Amaria, Chantale Bernatchez, Timothy P. Heffernan, Weiyi Peng, Jason Roszik & Patrick Hwu. (2020) Aurora kinase inhibition sensitizes melanoma cells to T-cell-mediated cytotoxicity. Cancer Immunology, Immunotherapy 70:4, pages 1101-1113.
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Eric T. Miller, Sungyong You, Radu M. Cadaneanu, Minhyung Kim, Junhee Yoon, Sandy T. Liu, Xinmin Li, Lorna Kwan, Jennelle Hodge, Michael J. Quist, Catherine S. Grasso, Michael S. Lewis, Beatrice S. Knudsen, Michael R. Freeman & Isla P. Garraway. (2020) Chromosomal instability in untreated primary prostate cancer as an indicator of metastatic potential. BMC Cancer 20:1.
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Yingzi Zhang, Jiao Tian, Chi Qu, Yang Peng, Jinwei Lei, Lu Sun, Beige Zong & Shengchun Liu. (2020) A look into the link between centrosome amplification and breast cancer. Biomedicine & Pharmacotherapy 132, pages 110924.
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Qianqian Liu, Xiling Zhang, Haichao Tang, Jinwei Liu, Chen Fu, Mingli Sun, Lin Zhao, Minjie Wei, Zhaojin Yu & Ping Wang. (2019) Bioinformatics Analysis Suggests the Combined Expression of AURKB and KIF18B Being an Important Event in the Development of Clear Cell Renal Cell Carcinoma. Pathology & Oncology Research 26:3, pages 1583-1594.
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Shu-Yu Lin, Chun-Feng Chang, Mohane Selvaraj Coumar, Pei-Yi Chen, Fu-Ming Kuo, Chun-Hwa Chen, Mu-Chun Li, Wen-Hsing Lin, Po-Chu Kuo, Sing-Yi Wang, An-Siou Li, Chin-Yu Lin, Chen-Ming Yang, Teng-Kuang Yeh, Jen-Shin Song, John T.A. Hsu & Hsing-Pang Hsieh. (2020) Drug-like property optimization: Discovery of orally bioavailable quinazoline-based multi-targeted kinase inhibitors. Bioorganic Chemistry 98, pages 103689.
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Yu Xu, Shu-Yi Hao, Xiu-Juan Zhang, Wen-Bo Li, Xue-Peng Qiao, Zi-Xiao Wang & Shi-Wu Chen. (2020) Discovery of novel 2,4-disubstituted pyrimidines as Aurora kinase inhibitors. Bioorganic & Medicinal Chemistry Letters 30:3, pages 126885.
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Taoda Shi, ChristopherJ. Zerio, Jared Sivinski, Andrew J. Ambrose, Kohlson T. Moore, Thomas Buckley, Lynn Kaneko, Mae Zhang, Donna D. Zhang & Eli Chapman. (2019) A One-Step, Atom Economical Synthesis of Thieno[2,3- d ]pyrimidin-4-amine Derivatives by a Four-Component Reaction . European Journal of Organic Chemistry 2019:20, pages 3269-3272.
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Xinran Liu, Yuchen Chen, Yangkai Li, Robert B. Petersen & Kun Huang. (2019) Targeting mitosis exit: A brake for cancer cell proliferation. Biochimica et Biophysica Acta (BBA) - Reviews on Cancer 1871:1, pages 179-191.
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Sailu Sarvagalla, Safiulla Basha Syed & Mohane Selvaraj Coumar. 2019. In Silico Drug Design. In Silico Drug Design 743 780 .
Yi-Yu Ke, Chun-Ping Chang, Wen-Hsing Lin, Chia-Hua Tsai, I-Chen Chiu, Wan-Ping Wang, Pei-Chen Wang, Pei-Yi Chen, Wen-Hsin Lin, Chun-Feng Chang, Po-Chu Kuo, Jen-Shin Song, Chuan Shih, Hsing-Pang Hsieh & Ya-Hui Chi. (2018) Design and synthesis of BPR1K653 derivatives targeting the back pocket of Aurora kinases for selective isoform inhibition. European Journal of Medicinal Chemistry 151, pages 533-545.
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Sofie Martens, Vera Goossens, Lars Devisscher, Sam Hofmans, Polien Claeys, Marnik Vuylsteke, Nozomi Takahashi, Koen Augustyns & Peter Vandenabeele. (2018) RIPK1-dependent cell death: a novel target of the Aurora kinase inhibitor Tozasertib (VX-680). Cell Death & Disease 9:2.
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Chiung-Yao Fang, Jeng-Sheng Chen, Shun-Kai Chang & Cheng-Huang Shen. (2018) Reversine induces autophagic cell death through the AMP-activated protein kinase pathway in urothelial carcinoma cells. Anti-Cancer Drugs 29:1, pages 29-39.
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Sandhya Noronha, Lauren A. C. Alt, Taylor E. Scimeca, Omran Zarou, Justyna Obrzut, Brian Zanotti, Elizabeth A. Hayward, Akhil Pillai, Shubha Mathur, Joseph Rojas, Ribhi Salamah, Nalini Chandar & Michael J. Fay. (2017) Preclinical evaluation of the Aurora kinase inhibitors AMG 900, AZD1152-HQPA, and MK-5108 on SW-872 and 93T449 human liposarcoma cells. In Vitro Cellular & Developmental Biology - Animal 54:1, pages 71-84.
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N Yang, C Wang, Z Wang, S Zona, S-X Lin, X Wang, M Yan, F-M Zheng, S-S Li, B Xu, L Bella, J-S Yong, E W-F Lam & Q Liu. (2017) FOXM1 recruits nuclear Aurora kinase A to participate in a positive feedback loop essential for the self-renewal of breast cancer stem cells. Oncogene 36:24, pages 3428-3440.
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Fuchen Liu, Guangyong Wang, Xiaoqiang Wang, Zhihui Che, Wei Dong, Xinggang Guo, Zhenguang Wang, Ping Chen, Daisen Hou, Qi Zhang, Wenli Zhang, Yida Pan, Dongqin Yang & Hui Liu. (2017) Targeting high Aurora kinases expression as an innovative therapy for hepatocellular carcinoma. Oncotarget 8:17, pages 27953-27965.
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Sailu Sarvagalla & Mohane Selvaraj Coumar. 2017. Pharmaceutical Sciences. Pharmaceutical Sciences 1115 1143 .
Yung Chang Hsu, Mohane Selvaraj Coumar, Wen-Chieh Wang, Hui-Yi Shiao, Yi-Yu Ke, Wen-Hsing Lin, Ching-Chuan Kuo, Chun-Wei Chang, Fu-Ming Kuo, Pei-Yi Chen, Sing-Yi Wang, An-Siou Li, Chun-Hwa Chen, Po-Chu Kuo, Ching-Ping Chen, Ming-Hsine Wu, Chen-Lung Huang, Kuei-Jung Yen, Yun-I Chang, John T.-A. Hsu, Chiung-Tong Chen, Teng-Kuang Yeh, Jen-Shin Song, Chuan Shih & Hsing-Pang Hsieh. (2016) Discovery of BPR1K871, a quinazoline based, multi-kinase inhibitor for the treatment of AML and solid tumors: Rational design, synthesis, in vitro and in vivo evaluation . Oncotarget 7:52, pages 86239-86256.
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Edmilson Ozorio dos Santos, Tatiana Correa Carneiro-Lobo, Mateus Nobrega Aoki, Elena Levantini & Daniela Sanchez Bassères. (2016) Aurora kinase targeting in lung cancer reduces KRAS-induced transformation. Molecular Cancer 15:1.
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Timothy P. Heffron. (2016) Small Molecule Kinase Inhibitors for the Treatment of Brain Cancer. Journal of Medicinal Chemistry 59:22, pages 10030-10066.
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Senna Sakai, Hiroto Izumi, Yukiko Yoshiura, Yoshifumi Nakayama, Takahiro Yamaguchi, Yoshikazu Harada, Chiho Koi, Hiroyuki Kurata & Yasuo Morimoto. (2016) In vitro evaluation of a combination treatment involving anticancer agents and an aurora kinase B inhibitor. Oncology Letters 12:5, pages 4263-4269.
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Min Yan, Chunli Wang, Bin He, Mengying Yang, Mengying Tong, Zijie Long, Bing Liu, Fei Peng, Lingzhi Xu, Yan Zhang, Dapeng Liang, Haixin Lei, Sen Subrata, Keith W. Kelley, Eric W.-F. Lam, Bilian Jin & Quentin Liu. (2016) Aurora-A Kinase: A Potent Oncogene and Target for Cancer Therapy. Medicinal Research Reviews 36:6, pages 1036-1079.
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Zhu Xingyu, Ma Peijie, Peng Dan, Wang Youg, Wang Daojun, Chen Xinzheng, Zhang Xijun & Song Yangrong. (2016) Quercetin suppresses lung cancer growth by targeting Aurora B kinase. Cancer Medicine 5:11, pages 3156-3165.
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Karen W. L. Yee, Hsiao-Wei T. Chen, David W. Hedley, Sue Chow, Joseph Brandwein, Andre C. Schuh, Aaron D. Schimmer, Vikas Gupta, Deborah Sanfelice, Tara Johnson, Lisa W. Le, Jamie Arnott, Mark R. Bray, Carolyn Sidor & Mark D. Minden. (2016) A phase I trial of the aurora kinase inhibitor, ENMD-2076, in patients with relapsed or refractory acute myeloid leukemia or chronic myelomonocytic leukemia. Investigational New Drugs 34:5, pages 614-624.
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Matej Janeček, Maxim Rossmann, Pooja Sharma, Amy Emery, David J. Huggins, Simon R. Stockwell, Jamie E. Stokes, Yaw S. Tan, Estrella Guarino Almeida, Bryn Hardwick, Ana J. Narvaez, Marko Hyvönen, David R. Spring, Grahame J. McKenzie & Ashok R. Venkitaraman. (2016) Allosteric modulation of AURKA kinase activity by a small-molecule inhibitor of its protein-protein interaction with TPX2. Scientific Reports 6:1.
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Dhanasekaran Karthigeyan, Sudhevan Surabhi, Pushpak Mizar, Siddhanta Soumik, Amrita Banerjee, Sarmistha Halder Sinha, Dipak Dasgupta, Chandrabhas Narayana & Tapas K. Kundu. (2016) A Dual Non-ATP Analogue Inhibitor of Aurora Kinases A and B, Derived from Resorcinol with a Mixed Mode of Inhibition. Chemical Biology & Drug Design 87:6, pages 958-967.
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Woong-Hee Kim, Haihong Shen, Da-Woon Jung & Darren R. Williams. (2016) Some leopards can change their spots: potential repositioning of stem cell reprogramming compounds as anti-cancer agents. Cell Biology and Toxicology 32:3, pages 157-168.
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Sailu Sarvagalla & Mohane Selvaraj Coumar. 2016. Applied Case Studies and Solutions in Molecular Docking-Based Drug Design. Applied Case Studies and Solutions in Molecular Docking-Based Drug Design 249 277 .
Nhung Thi My Hoang, Thuong Thien PhuongTrang Thi Nhu Nguyen, Yen Thi Hai Tran, Anh Thi Ngoc Nguyen, Thanh Lai Nguyen & Khanh Thi Van Bui. (2016) <i>In Vitro</i> Characterization of Derrone as an Aurora Kinase Inhibitor. Biological & Pharmaceutical Bulletin Biological and Pharmaceutical Bulletin 39:6, pages 935-945.
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Todd B. Sells, Ryan Chau, Jeffrey A. Ecsedy, Rachel E. Gershman, Kara Hoar, Jessica Huck, David A. Janowick, Vivek J. Kadambi, Patrick J. LeRoy, Matthew Stirling, Stephen G. Stroud, Tricia J. Vos, Gabriel S. Weatherhead, Deborah R. Wysong, Mengkun Zhang, Suresh K. Balani, Joseph B. Bolen, Mark G. Manfredi & Christopher F. Claiborne. (2015) MLN8054 and Alisertib (MLN8237): Discovery of Selective Oral Aurora A Inhibitors. ACS Medicinal Chemistry Letters 6:6, pages 630-634.
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Hye Jin Chung, Kyeong Ryang Park, Hyo Jeong Lee, Jongkook Lee, Jeong-Hyun Kim, Yong-Chul Kim & Sun-Young Han. (2015) Effects of KRC-108 on the Aurora A activity and growth of colorectal cancer cells. Biochemical and Biophysical Research Communications 461:4, pages 605-611.
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Ying Su, Sijun Pan, Zhengqiu Li, Lin Li, Xiaoyuan Wu, Piliang Hao, Siu Kwan Sze & Shao Q. Yao. (2015) Multiplex Imaging and Cellular Target Identification of Kinase Inhibitors via an Affinity-Based Proteome Profiling Approach. Scientific Reports 5:1.
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