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- Title
Design, Synthesis, and Biological Evaluation of Novel Thienopyrimidine Derivatives as PI3Kα Inhibitors.
- Authors
Yu, Lide; Wang, Qinqin; Wang, Caolin; Zhang, Binliang; Yang, Zunhua; Fang, Yuanying; Zhu, Wufu; Zheng, Pengwu
- Abstract
Three series of novel thienopyrimidine derivatives 9a–l, 15a–l, and 18a–h were designed and synthesized, and their IC50 values against four cancer cell lines HepG-2, A549, PC-3, and MCF-7 were evaluated. Most compounds show moderate cytotoxicity against the tested cancer cell lines. The most promising compound 9a showed moderate activity with IC50 values of 12.32 ± 0.96, 11.30 ± 1.19, 14.69 ± 1.32, and 9.80 ± 0.93 µM, respectively. The inhibitory activities of compounds 9a and 15a against PI3Kα and mTOR kinase were further evaluated. Compound 9a exhibited PI3Kα kinase inhibitory activity with IC50 of 9.47 ± 0.63 µM. In addition, docking studies of compounds 9a and 15a were also investigated.
- Subjects
CELL lines; CANCER cells
- Publication
Molecules, 2019, Vol 24, Issue 19, p3422
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules24193422