Gao, Xiu-zheng published the artcileDesign, synthesis and in vitro anticancer research of novel tetrandrine and fangchinoline derivatives, Related Products of bromides-buliding-blocks, the publication is Bioorganic Chemistry (2021), 104694, database is CAplus and MEDLINE.
Cancer treatment is one of the major public health issues in the world. Tetrandrine (Tet) and fangchinoline (d-Tet) are two bis-benzyl isoquinoline alkaloids extracted from Stephania tetrandra S. Moore, and their antitumor activities have been confirmed. However, the ED of Tet and d-Tet were much higher than that of the pos. control and failed to meet clin. standards Therefore, in this study, as a continuation of our previous work to study and develop high-efficiency and low-toxic antitumor lead compounds, twenty new Tet and d-Tet derivatives were designed, synthesized and evaluated as antitumor agents against six cancer cell lines (H460, H520, HeLa, HepG-2, MCF-7, SW480 cell lines) and BEAS-2B normal cells by CCK-8 anal. Ten derivatives showed better cytotoxic effects than the parent fangchinoline, of which I showed the strongest cell growth inhibitory activity with an IC50 value of 0.59μM against A549 cells. Subsequently, the antitumor mechanism of I was studied by flow cytometry, Hoechst 33258, JC-1 staining, cell scratch, transwell migration, and Western blotting assays. These results showed that compound I could inhibit A549 cell proliferation by arresting the G2/M cell cycle and inhibiting cell migration and invasion by reducing MMP-2 and MMP-9 expression. Meanwhile, I could induce apoptosis of A549 cells through the intrinsic pathway regulated by mitochondria. In addition, compound I inhibited the phosphorylation of PI3K, Akt and mTOR, suggesting a correlation between blocking the PI3K/Akt/mTOR pathway and the above antitumor activities. These results suggest that compound I may be a future drug for the development of new potential drug candidates against lung cancer.
Bioorganic Chemistry published new progress about 21101-63-3. 21101-63-3 belongs to bromides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Bromide,sulfides,Benzyl bromide,Benzene, name is (4-(Bromomethyl)phenyl)(trifluoromethyl)sulfane, and the molecular formula is C8H6BrF3S, Related Products of bromides-buliding-blocks.
Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary