4.5 Review

Antitumour Anthracyclines: Progress and Perspectives

期刊

CHEMMEDCHEM
卷 15, 期 11, 页码 933-948

出版社

WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.202000131

关键词

cardiotoxicity; doxorubicin; drug discovery; multidrug resistance; topoisomerases

资金

  1. Fundacao de Amparo a Pesquisa do Estado de Sao Paulo (FAPESP) [2015/10837-0, 2016/211946]
  2. Coordenacao de Aperfeicoamento de Pessoal de Nivel Superior (CAPES) [001]

向作者/读者索取更多资源

Anthracyclines are ranked among the most effective chemotherapeutics against cancer. They are glycoside drugs comprising the amino sugar daunosamine linked to a hydroxy anthraquinone aglycone, and act by DNA intercalation, oxidative stress generation and topoisomerase II poisoning. Regardless of their therapeutic value, multidrug resistance and severe cardiotoxicity are important limitations of anthracycline treatment that have prompted the discovery of novel analogues. This review covers the most clinically relevant anthracyclines and their development over decades, since the first discovered natural prototypes to recent semisynthetic and synthetic derivatives. These include registered drugs, drug candidates undergoing clinical trials, and compounds under pre-clinical investigation. The impact of the structural modifications on antitumour activity, toxicity and resistance profile is addressed.

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