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Novel Inhibitors of DNA Repair Enzyme TDP1 Combining Monoterpenoid and Adamantane Fragments.

Anticancer Agents Med Chem. 2019-01; 
MozhaitsevEvgenii S,ZakharenkoAlexandra L,SuslovEvgeniy V,KorchaginaDina V,ZakharovaOlga D,Vasil'evaInna A,ChepanovaArina A,BlackEllena,PatelJinal,ChandRaina,ReynissonJóhannes,LeungIvanhoe K H,VolchoKonstantin P,SalakhutdinovNariman F,LavrikOl
Products/Services Used Details Operation
Custom Vector Construction … Novosibirsk, Russia. 2.3.2. Binding Studies Plasmid that encodes human TDP1 (residues 149-608) was purchased from GenScript. The vector was pET-28a(+). The TDP1 sequence that was published by Interthal et al. was … Get A Quote

摘要

The DNA repair enzyme tyrosyl-DNA-phosphodiesterase 1 (TDP1) is a current inhibition target to improve the efficacy of cancer chemotherapy. Previous studies showed that compounds combining adamantane and monoterpenoid fragments are active against TDP1 enzyme. This investigation is focused on the synthesis of monoterpenoid derived esters of 1-adamantane carboxylic acid as TDP1 inhibitors.

关键词

3,7-dimethyloctanol,Citronellol,chemical space,cytotoxicity,esters,inhibitors,molecular modelling,terp