期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 209, 期 -, 页码 -出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2020.112946
关键词
Pyridazine; Anticancer; Drug-like scaffold; SAR
资金
- Chinese Ministry of Science and Technology [2016YFA0501800]
- National Natural Science Foundation of China [81470524, 81870297, 81703328]
- Henan Scientific Innovation Talent Team, Department of Education [19IRTSTHN001]
- Scientific Program of Henan Province [182102310070]
Identification of potent anticancer agents with high selectivity and low toxicity remains an ongoing challenge. Pyridazine, known for its advantageous physicochemical properties and antitumor potential, is considered a promising drug-like scaffold. This review focuses on the structure-activity relationship studies and design strategies of pyridazine derivatives as potential anticancer agents.
Identification of potent anticancer agents with high selectivity and low toxicity remains on the way to human health. Pyridazine featuring advantageous physicochemical properties and antitumor potential usually is regarded as a central core in numerous anticancer derivatives. There are several approved pyridazine-based drugs in the market and analogues currently going through different clinical phases or registration statuses, suggesting pyridazine as a promising drug-like scaffold. The current review is intended to provide a comprehensive and updated overview of pyridazine derivatives as potential anticancer agents. In particular, we focused on their structure-activity relationship (SAR) studies, design strategies, binding modes and biological activities in the hope of offering novel insights for further rational design of more active and less toxic anticancer drugs. (c) 2020 Elsevier Masson SAS. All rights reserved.
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