Discovery of aromatic amides with triazole-core as potent reversal agents against P-glycoprotein-mediated multidrug resistance was written by Qiu, Qianqian;Zhu, Jilan;Chen, Qiutong;Jiang, Ziqian;Xu, Jiting;Jiang, Xueting;Huang, Wenlong;Liu, Zhongquan;Ye, Jing;Xu, Xiaojuan. And the article was included in Bioorganic Chemistry in 2019.Quality Control of 6,7-Dimethoxy-1,2,3,4-tetrahydroisoquinoline hydrochloride This article mentions the following:
P-glycoprotein (P-gp)-mediated multidrug resistance (MDR) is a major impediment for clin. cancer therapy. 19 novel aromatic amides with triazole-core as MDR reversal agents were designed and synthesized via click chem. to reverse MDR. Among them, compound 42 was identified as the most promising candidate with high potency (EC50 = 78.1 ± 5.4 nM), low cytotoxity (SI > 1282) and persistent duration in reversing doxorubicin (DOX) resistance in K562/A02 cells. 42 also enhanced the potency of other P-gp associated cytotoxic agents with different structures. In further study, remarkably increased intracellular accumulation of Rh123 and DOX in K562/A02 cells was achieved by compound 42, while CYP3A4 activity had no change by compound 42. These results indicate that compound 42 as a relatively safe modulator of P-gp-mediated MDR has good potential for further development. In the experiment, the researchers used many compounds, for example, 6,7-Dimethoxy-1,2,3,4-tetrahydroisoquinoline hydrochloride (cas: 2328-12-3Quality Control of 6,7-Dimethoxy-1,2,3,4-tetrahydroisoquinoline hydrochloride).
6,7-Dimethoxy-1,2,3,4-tetrahydroisoquinoline hydrochloride (cas: 2328-12-3) belongs to tetrahydroisoquinoline derivatives. Tetrahydroisoquinoline motif is often present in natural products with a broad range of biological and pharmacological activities. In particular, 1-benzyl1,2,3,4-tetrahydroisoquinolines are dopamine receptor antagonists. The dopamine-derived tetrahydroisoquinolines (TIQ) synthesized endogeneously from aldehydes and catecholamines have shown to modulate neurotransmission, central metabolism and motor activity.Quality Control of 6,7-Dimethoxy-1,2,3,4-tetrahydroisoquinoline hydrochloride
Referemce:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem