Discovery of Novel c-Met Inhibitors Bearing a 3-Carboxyl Piperidin-2-one Scaffold
A series of compounds containing a novel 3-carboxypiperidin-2-one scaffold based on the lead structure BMS-777607 were designed, synthesized and evaluated for their c-Met kinase inhibition and cytotoxicity against MKN45 cancer cell lines. The results indicated that five compounds exhibited significa...
| Main Authors: | , , , , , , , |
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| Format: | Article |
| Language: | English |
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MDPI AG
2014-02-01
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| Series: | Molecules |
| Subjects: | |
| Online Access: | http://www.mdpi.com/1420-3049/19/2/2655 |
| _version_ | 1811312499373375488 |
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| author | Wei Zhang Jing Ai Dakuo Shi Xia Peng Yinchun Ji Jian Liu Meiyu Geng Yingxia Li |
| author_facet | Wei Zhang Jing Ai Dakuo Shi Xia Peng Yinchun Ji Jian Liu Meiyu Geng Yingxia Li |
| author_sort | Wei Zhang |
| collection | DOAJ |
| description | A series of compounds containing a novel 3-carboxypiperidin-2-one scaffold based on the lead structure BMS-777607 were designed, synthesized and evaluated for their c-Met kinase inhibition and cytotoxicity against MKN45 cancer cell lines. The results indicated that five compounds exhibited significant inhibitory effect on c-Met with IC50 values of 8.6−81 nM and four compounds showed potent inhibitory activity against MKN45 cell proliferation, with IC50s ranging from 0.57−16 μM. |
| first_indexed | 2024-04-13T10:37:15Z |
| format | Article |
| id | doaj.art-8f446716483845c2ba40060c4ebe6d73 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-04-13T10:37:15Z |
| publishDate | 2014-02-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-8f446716483845c2ba40060c4ebe6d732022-12-22T02:50:01ZengMDPI AGMolecules1420-30492014-02-011922655267310.3390/molecules19022655molecules19022655Discovery of Novel c-Met Inhibitors Bearing a 3-Carboxyl Piperidin-2-one ScaffoldWei Zhang0Jing Ai1Dakuo Shi2Xia Peng3Yinchun Ji4Jian Liu5Meiyu Geng6Yingxia Li7School of Pharmacy, Fudan University, Shanghai 201203, ChinaDivision of Antitumor Pharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, ChinaSchool of Pharmacy, Ocean University of China, Qingdao 266003, ChinaDivision of Antitumor Pharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, ChinaDivision of Antitumor Pharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, ChinaSchool of Pharmacy, Fudan University, Shanghai 201203, ChinaDivision of Antitumor Pharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, ChinaSchool of Pharmacy, Fudan University, Shanghai 201203, ChinaA series of compounds containing a novel 3-carboxypiperidin-2-one scaffold based on the lead structure BMS-777607 were designed, synthesized and evaluated for their c-Met kinase inhibition and cytotoxicity against MKN45 cancer cell lines. The results indicated that five compounds exhibited significant inhibitory effect on c-Met with IC50 values of 8.6−81 nM and four compounds showed potent inhibitory activity against MKN45 cell proliferation, with IC50s ranging from 0.57−16 μM.http://www.mdpi.com/1420-3049/19/2/2655c-Metsynthesiskinase inhibitor3-carboxypiperidin-2-one |
| spellingShingle | Wei Zhang Jing Ai Dakuo Shi Xia Peng Yinchun Ji Jian Liu Meiyu Geng Yingxia Li Discovery of Novel c-Met Inhibitors Bearing a 3-Carboxyl Piperidin-2-one Scaffold Molecules c-Met synthesis kinase inhibitor 3-carboxypiperidin-2-one |
| title | Discovery of Novel c-Met Inhibitors Bearing a 3-Carboxyl Piperidin-2-one Scaffold |
| title_full | Discovery of Novel c-Met Inhibitors Bearing a 3-Carboxyl Piperidin-2-one Scaffold |
| title_fullStr | Discovery of Novel c-Met Inhibitors Bearing a 3-Carboxyl Piperidin-2-one Scaffold |
| title_full_unstemmed | Discovery of Novel c-Met Inhibitors Bearing a 3-Carboxyl Piperidin-2-one Scaffold |
| title_short | Discovery of Novel c-Met Inhibitors Bearing a 3-Carboxyl Piperidin-2-one Scaffold |
| title_sort | discovery of novel c met inhibitors bearing a 3 carboxyl piperidin 2 one scaffold |
| topic | c-Met synthesis kinase inhibitor 3-carboxypiperidin-2-one |
| url | http://www.mdpi.com/1420-3049/19/2/2655 |
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