期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 26, 期 20, 页码 5103-5109出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2016.08.064
关键词
Temozolomide; Glioblastoma; Chemotheraphy; O-6-Methyl-2 '-deoxyguanosine (O-6-MedG)
资金
- Medivation
Temozolomide is a chemotherapeutic agent that is used in the treatment of glioblastoma and other malignant gliomas. It acts through DNA alkylation, but treatment is limited by its systemic toxicity and neutralization of DNA alkylation by upregulation of the O-6-methylguanine-DNA methyltransferase gene. Both of these limiting factors can be addressed by achieving higher concentrations of TMZ in the brain. Our research has led to the discovery of new analogs of temozolomide with improved brain: plasma ratios when dosed in vivo in rats. These compounds are imidazotetrazine analogs, expected to act through the same mechanism as temozolomide. With reduced systemic exposure, these new agents have the potential to improve efficacy and therapeutic index in the treatment of glioblastoma. (C) 2016 Published by Elsevier Ltd.
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