Synthesis of isoquinolinone-based tricycles as novel poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors
The isoquinolinone-based tricyclic compounds were designed and synthesized. Preliminary biological study of these compounds provided potent compounds 17a, 33b, 33c, 33d, and 33g with low nanomolar IC50s against PARP-1 enzyme.
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2014-06, Vol.24 (12), p.2669-2673 |
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| container_end_page | 2673 |
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| container_issue | 12 |
| container_start_page | 2669 |
| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 24 |
| creator | Chen, Jianyang Peng, Haixia He, Jinxue Huan, Xiajuan Miao, Zehong Yang, Chunhao |
| description | The isoquinolinone-based tricyclic compounds were designed and synthesized. Preliminary biological study of these compounds provided potent compounds 17a, 33b, 33c, 33d, and 33g with low nanomolar IC50s against PARP-1 enzyme. |
| doi_str_mv | 10.1016/j.bmcl.2014.04.061 |
| format | Article |
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| fulltext | fulltext |
| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2014-06, Vol.24 (12), p.2669-2673 |
| issn | 0960-894X 1464-3405 |
| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Antitumor Enzyme Activation - drug effects Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology Inhibitory Concentration 50 Isoquinolines - chemistry Isoquinolines - pharmacology Isoquinolinone-based tricycles Molecular Structure PARP-1 inhibitors Poly(ADP-ribose) Polymerase Inhibitors Poly(ADP-ribose) Polymerases - chemistry |
| title | Synthesis of isoquinolinone-based tricycles as novel poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors |
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