Ontology highlight
ABSTRACT:
SUBMITTER: Pletsas D
PROVIDER: S-EPMC4219134 | biostudies-literature | 2013 Sep
REPOSITORIES: biostudies-literature
Pletsas Dimitrios D Garelnabi Elrashied A E EA Li Li L Phillips Roger M RM Wheelhouse Richard T RT
Journal of medicinal chemistry 20130816 17
The antitumor prodrug temozolomide is compromised by its dependence for activity on DNA mismatch repair (MMR) and the repair of the chemosensitive DNA lesion, O6-methylguanine (O6-MeG), by O6-methylguanine-DNA-methyltransferase (E.C. 2.1.1.63, MGMT). Tumor response is also dependent on wild-type p53. Novel 3-(2-anilinoethyl)-substituted imidazotetrazines are reported that have activity independent of MGMT, MMR, and p53. This is achieved through a switch of mechanism so that bioactivity derives f ...[more]