Ontology highlight
ABSTRACT:
SUBMITTER: Jin C
PROVIDER: S-EPMC5512130 | biostudies-literature | 2017 Jul
REPOSITORIES: biostudies-literature
Jin Chen C Wen Shuai S Zhang Qiumeng Q Zhu Qiwen Q Yu Jiahui J Lu Wei W
ACS medicinal chemistry letters 20170627 7
Due to the low esterase activity in human plasma, many ester and carbonate prodrugs tested in humans may be less effective than that in preclinical animals. In this letter, PTX and SN-38 were attached to the <i>N</i>-1 position of 2-nitroimidazole via a carbonate linker. Presumably, 2-aminoimidazole may help promote the intramolecular hydrolysis of the carbonate bond. The prodrugs exhibited a considerable stability in buffers at different pH values as well as in human plasma. Furthermore, a rapi ...[more]