4.8 Article

A Short-Lived but Highly Cytotoxic Vanadium(V) Complex as a Potential Drug Lead for Brain Cancer Treatment by Intratumoral Injections

期刊

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
卷 59, 期 37, 页码 15834-15838

出版社

WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.202005458

关键词

anti-cancer treatment; intratumoral injection; neuroprotection; non-innocent mixed ligands; vanadium

资金

  1. Australian Research Council (ARC) [DP130103566, DP160104172]
  2. University of Sydney
  3. Arthur Cope Foundation

向作者/读者索取更多资源

The chemistry and short lifetimes of metal-based anti-cancer drugs can be turned into an advantage for direct injections into tumors, which then allow the use of highly cytotoxic drugs. The release of their less toxic decomposition products into the blood will lead to decreased toxicity and can even have beneficial effects. We present a ternary V(V)complex,1([(VOLL2)-L-1], where L(1)isN-(salicylideneaminato)-N '-(2-hydroxyethyl)ethane-1,2-diamine and L(2)is 3,5-di-tert-butylcatechol), which enters cells intact to induce high cytotoxicity in a range of human cancer cells, including T98g (glioma multiforme), while its decomposition products in cell culture medium were approximate to 8-fold less toxic.1was 12-fold more toxic than cisplatin in T98g cells and 6-fold more toxic in T98g cells than in a non-cancer human cell line, HFF-1. Its high toxicity in T98g cells was retained in the presence of physiological concentrations of the two main metal-binding serum proteins, albumin and transferrin. These properties favor further development of1for brain cancer treatment by intratumoral injections.

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