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Journal of Enzyme Inhibition and Medicinal Chemistry Volume 35, 2020 - Issue 1
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Research Paper

Design of new disubstituted imidazo[1,2-b]pyridazine derivatives as selective Haspin inhibitors. Synthesis, binding mode and anticancer biological evaluation

Jonathan Eliea Institut de Chimie Organique et Analytique, Université d’Orléans, UMR CNRS 7311, Orléans Cedex 2, FranceView further author information
,
Omid Feizbakhshb Sorbonne Université/CNRS UMR8227, Station Biologique, Roscoff cedex, FranceView further author information
,
Nathalie Desbanb Sorbonne Université/CNRS UMR8227, Station Biologique, Roscoff cedex, FranceView further author information
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Béatrice Josselinb Sorbonne Université/CNRS UMR8227, Station Biologique, Roscoff cedex, France;c Sorbonne Université/CNRS FR2424, Plateforme de criblage KISSf (Kinase Inhibitor Specialized Screening facility) Station Biologique, Roscoff cedex, FranceView further author information
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Blandine Baratteb Sorbonne Université/CNRS UMR8227, Station Biologique, Roscoff cedex, France;c Sorbonne Université/CNRS FR2424, Plateforme de criblage KISSf (Kinase Inhibitor Specialized Screening facility) Station Biologique, Roscoff cedex, FranceView further author information
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Amandine Bescondb Sorbonne Université/CNRS UMR8227, Station Biologique, Roscoff cedex, FranceView further author information
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Julien Duezb Sorbonne Université/CNRS UMR8227, Station Biologique, Roscoff cedex, FranceView further author information
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Xavier Fantb Sorbonne Université/CNRS UMR8227, Station Biologique, Roscoff cedex, FranceView further author information
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Stéphane Bachb Sorbonne Université/CNRS UMR8227, Station Biologique, Roscoff cedex, France;c Sorbonne Université/CNRS FR2424, Plateforme de criblage KISSf (Kinase Inhibitor Specialized Screening facility) Station Biologique, Roscoff cedex, FranceView further author information
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Dominique Maried Sorbonne Université/CNRS UMR7144, Station Biologique, Roscoff cedex, FranceView further author information
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Matthieu Placea Institut de Chimie Organique et Analytique, Université d’Orléans, UMR CNRS 7311, Orléans Cedex 2, FranceView further author information
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Sami Ben Salaha Institut de Chimie Organique et Analytique, Université d’Orléans, UMR CNRS 7311, Orléans Cedex 2, FranceView further author information
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Agnes Chartiera Institut de Chimie Organique et Analytique, Université d’Orléans, UMR CNRS 7311, Orléans Cedex 2, FranceView further author information
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Sabine Berteina-Raboina Institut de Chimie Organique et Analytique, Université d’Orléans, UMR CNRS 7311, Orléans Cedex 2, FranceView further author information
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Apirat Chaikuade Institute for Pharmaceutical Chemistry, Johann Wolfgang Goethe University, Frankfurt am Main, Germany;f Structure Genomics Consortium, Johann Wolfgang Goethe University, Buchmann Institute for Molecular Life Sciences, Frankfurt am Main, GermanyView further author information
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Stefan Knappe Institute for Pharmaceutical Chemistry, Johann Wolfgang Goethe University, Frankfurt am Main, Germany;f Structure Genomics Consortium, Johann Wolfgang Goethe University, Buchmann Institute for Molecular Life Sciences, Frankfurt am Main, GermanyView further author information
,
Fabrice Carlesa Institut de Chimie Organique et Analytique, Université d’Orléans, UMR CNRS 7311, Orléans Cedex 2, FranceView further author information
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Pascal Bonneta Institut de Chimie Organique et Analytique, Université d’Orléans, UMR CNRS 7311, Orléans Cedex 2, FranceView further author information
,
Frédéric Burona Institut de Chimie Organique et Analytique, Université d’Orléans, UMR CNRS 7311, Orléans Cedex 2, FranceCorrespondence[email protected]
View further author information
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Sylvain Routiera Institut de Chimie Organique et Analytique, Université d’Orléans, UMR CNRS 7311, Orléans Cedex 2, FranceCorrespondence[email protected]
View further author information
&
Sandrine Ruchaudb Sorbonne Université/CNRS UMR8227, Station Biologique, Roscoff cedex, FranceCorrespondence[email protected]
View further author information
 show all
Pages 1840-1853 | Received 07 Jul 2020, Accepted 14 Sep 2020, Published online: 12 Oct 2020

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Terungwa H. Iorkula, Bryce A. Tolman, Scott R. Burt & Matt A. Peterson. (2024) An efficient synthesis of C-6 aminated 3-bromoimidazo[1,2-b]pyridazines. Synthetic Communications 54:2, pages 121-132.
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Sreenivas Avula, Xudan Peng, Xingfen Lang, Micky Tortorella, Béatrice Josselin, Stéphane Bach, Stephane Bourg, Pascal Bonnet, Frédéric Buron, Sandrine Ruchaud, Sylvain Routier & Cleopatra Neagoie. (2022) Design and biological evaluation of substituted 5,7-dihydro-6H-indolo[2,3-c]quinolin-6-one as novel selective Haspin inhibitors. Journal of Enzyme Inhibition and Medicinal Chemistry 37:1, pages 1632-1650.
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Eun-Ji Kwon, Karishma K. Mashelkar, Juhee Seo, Yoon-Ze Shin, Kisu Sung, Sung Chul Jang, Sang Won Cheon, Haeseung Lee, Hyuk Woo Lee, Gyudong Kim, Byung Woo Han, Sang Kook Lee, Lak Shin Jeong & Hyuk-Jin Cha. (2023) In Silico Discovery of 5′-Modified 7-Deoxy-7-ethynyl-4′-thioadenosine as a HASPIN Inhibitor and Its Synergistic Anticancer Effect with the PLK1 Inhibitor. ACS Central Science 9:6, pages 1140-1149.
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Y.-Y. Hou, W.-J. Ye, S.-S. Wang, F. Wu, C.-S. Zhao & Z.-X. Zhou. (2023) Synthesis, Crystal Structure, and DFT Study of Ethyl 6-Chloro-3-fluoroimidazo[1,2-b]pyridazine-2-carboxylate. Russian Journal of General Chemistry 93:5, pages 1193-1200.
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Yongjian Liu, Hongliu Yang, Yongsheng Fang, Yantao Xing, Xinxin Pang, Yang Li, Yuanyuan Zhang & Yonggang Liu. (2023) Function and inhibition of Haspin kinase: targeting multiple cancer therapies by antimitosis. Journal of Pharmacy and Pharmacology 75:4, pages 445-465.
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Simon Garnier, Kévin Brugemann, Agnieszka Zak, Johnny Vercouillie, Marie Potier-Cartereau, Mathieu Marchivie, Sylvain Routier & Frédéric Buron. (2022) A Facile One-Pot Synthesis of New Poly Functionalized Pyrrolotriazoles via a Regioselective Multicomponent Cyclisation and Suzuki–Miyaura Coupling Reactions. Catalysts 12:8, pages 828.
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Wael Zeinyeh, Yannick J. Esvan, Béatrice Josselin, Mathilde Defois, Blandine Baratte, Stefan Knapp, Apirat Chaikuad, Fabrice Anizon, Francis Giraud, Sandrine Ruchaud & Pascale Moreau. (2022) Synthesis and biological evaluation of Haspin inhibitors: Kinase inhibitory potency and cellular activity. European Journal of Medicinal Chemistry 236, pages 114369.
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Ahmed El Akkaoui, Jamal Koubachi, Gérald Guillaumet & Saïd El Kazzouli. (2021) Synthesis and Functionalization of Imidazo[1,2‐ b ]Pyridazine by Means of Metal‐Catalyzed Cross‐Coupling Reactions . ChemistrySelect 6:34, pages 8985-9011.
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