Discovery of thiosemicarbazone-containing compounds with potent anti-proliferation activity against drug-resistant K562/A02 cells was written by Gu, Xiaoke;Li, Xin;Guan, Mingyu;Jiang, Chunyu;Song, Qinghua;Sun, Nan;Zou, Yueting;Zhou, Qingqing;Chen, Jing;Qiu, Jingying. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2020.Related Products of 91-02-1 This article mentions the following:
P-glycoprotein (P-gp)-mediated multidrug resistance (MDR) is a major obstacle to successful chemotherapy for leukemia. A series of thiosemicarbazone-containing compounds were synthesized. Biol. evaluation showed that the most active compound (E)-6-(2-(1-(4-bromophenyl)ethylidene)hydrazine-1-carbothioamido)-N-hydroxyhexanamide displayed potent anti-leukemia activity against P-gp overexpressing drug-resistant K562/A02 cells, with an IC50 value of 0.44娓璏. Notably, compound (E)-6-(2-(1-(4-bromophenyl)ethylidene)hydrazine-1-carbothioamido)-N-hydroxyhexanamide exhibited a selective killing effect on K562/A02 cells by dose-dependently increasing the intracellular levels of reactive oxygen species (ROS), thus exerting a potential collateral sensitivity (CS)-promoting effect in vitro. Moreover, compound (E)-6-(2-(1-(4-bromophenyl)ethylidene)hydrazine-1-carbothioamido)-N-hydroxyhexanamide could inhibit HDAC1 and HDAC6, and induce the apoptosis of K562/A02 cells by increasing the expression of Bax, decreasing Bcl-2 protein level, and promoting the cleavage of caspase-3 and PARP, resp. Overall, (E)-6-(2-(1-(4-bromophenyl)ethylidene)hydrazine-1-carbothioamido)-N-hydroxyhexanamide may be a potential anti-cancer agent against drug-resistant myelogenous leukemia. In the experiment, the researchers used many compounds, for example, Phenyl(pyridin-2-yl)methanone (cas: 91-02-1Related Products of 91-02-1).
Phenyl(pyridin-2-yl)methanone (cas: 91-02-1) belongs to pyridine derivatives. Pyridine has a conjugated system of six 锜?electrons that are delocalized over the ring. The molecule is planar and, thus, follows the H鐪塩kel criteria for aromatic systems. Reduced pyridines, namely tetrahydropyridines, dihydropyridines and piperidines, are found in numerous natural and synthetic compounds. The synthesis and reactivity of these compounds have often been driven by the fact many of these compounds have interesting and unique pharmacological properties. Related Products of 91-02-1