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Design, synthesis, and biological evaluation of novel thiazole derivatives as PI3K/mTOR dual inhibitors.


ABSTRACT: The development of anticancer drugs targeting both PI3K and mTOR pathways is recognized as a promising cancer therapeutic approach. In the current study, we designed and synthesized seventeen new thiazole compounds to investigate their effect on both PI3K and mTOR as well as their anti-apoptotic activity. All the synthesized thiazoles were investigated for their antiproliferative activity on a panel of 60 different cancer cell lines at the National Cancer Institute. Compounds 3b and 3e were selected for further investigation at five dose concentrations due to their effective growth inhibiting activity. Compounds 3b and 3e were further evaluated for their in vitro inhibitory activities against PI3Kα and mTOR compared to alpelisib and dactolisib, respectively as reference drugs. The i

SUBMITTER: Faggal SI 

PROVIDER: S-EPMC11427869 | biostudies-literature | 2024 Sep

REPOSITORIES: biostudies-literature