Li, Er-dong published the artcile2,4-Disubstituted quinazolines targeting breast cancer cells via EGFR-PI3K, Name: 1-(Chloromethyl)-4-(trifluoromethyl)benzene, the publication is European Journal of Medicinal Chemistry (2019), 36-47, database is CAplus and MEDLINE.
A series of novel 2,4-disubstituted quinazolines I [R = hexyl, cyclopentyl, Ph, etc.] were synthesized and evaluated for their anti-tumor activity against five human cancer cells (MDA-MB-231, MCF-7, PC-3, HGC-27 and MGC-803) using MTT assay. Among them, compound I [R = 4-F3CC6H4] showed the most potent cytotoxicity against breast cancer cells. Compound I [R = 4-F3CC6H4] also significantly inhibited the colony formation and migration of MDA-MB-231 and MCF-7 cells. Meanwhile, compound I [R = 4-F3CC6H4] induced cell cycle arrest at G1 phase and cell apoptosis, as well as increased accumulation of intracellular ROS. Furthermore, compound I [R = 4-F3CC6H4] exerted antitumor effects in-vitro via decreasing the expression of anti-apoptotic protein Bcl-2 and increasing the pro-apoptotic protein Bax and p53. Mechanistically, compound I [R = 4-F3CC6H4] markedly decreased p-EGFR and p-PI3K expression, which revealed that compound I [R = 4-F3CC6H4] targeted breast cancer cells via interfering with EGFR-PI3K signaling pathway. Mol. docking suggested that compound I [R = 4-F3CC6H4] could indeed bind into the active pocket of EGFR. All the findings suggest that compound I [R = 4-F3CC6H4] might be a valuable lead compound for antitumor agents targeting breast cancer cells.
European Journal of Medicinal Chemistry published new progress about 939-99-1. 939-99-1 belongs to chlorides-buliding-blocks, auxiliary class Fluoride,Chloride,Benzyl chloride,Benzene, name is 1-(Chloromethyl)-4-(trifluoromethyl)benzene, and the molecular formula is C8H6ClF3, Name: 1-(Chloromethyl)-4-(trifluoromethyl)benzene.
Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics