期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 69, 期 -, 页码 609-621出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2013.09.016
关键词
Antitumor agents; Bifunctional DNA cross-linking agents; Bis(hydroxymethyl)pyrroles; Cytotoxicity; Hybrid pharmacophore; Indolizino[6,7-b]indole
资金
- National Science Council, Taiwan [NSC 101-2325-B-001-037, NSC 101-2325-B-001-002]
- Academia Sinica, Taipei, Taiwan [AS-100-TP-B13]
Bifunctional DNA cross-linking agents are widely used as chemotherapeutic agents in clinics. The advance in the development of these agents as potential antitumor agents has generated various types of bis(hydroxymethyl)pyrrole analogs. In order to develop highly effective anticancer agents, it is necessary to understand the chemophysical properties, structure activity relationships, therapeutic potency, toxicity/safety, and pharmacokinetics of these DNA cross-linking agents. This review presents an overview of the recent advances in developing various types of bis(hydroxymethyl)pyrrole analogs with potential antitumor activity to provide more information for future drug design and strategies for combination chemotherapy. The rational drug design, chemical syntheses, antitumor activity, mechanism of action, and development of combined chemotherapy regimens, including a DNA repair inhibitor, are discussed. (C) 2013 Elsevier Masson SAS. All rights reserved.
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