Qiu, QQ; Zhu, JL; Chen, QT; Jiang, ZQ; Xu, JT; Jiang, XT; Huang, WL; Liu, ZQ; Ye, J; Xu, XJ in [Qiu, Qianqian; Zhu, Jilan; Chen, Qiutong; Jiang, Ziqian; Xu, Jiting; Jiang, Xueting; Liu, Zhongquan; Ye, Jing; Xu, Xiaojuan] Yancheng Teachers Univ, Sch Pharm, Jiangsu Prov Key Lab Coastal Wetland Bioresources, Yancheng 224007, Peoples R China; [Huang, Wenlong] China Pharmaceut Univ, Ctr Drug Discovery, State Key Lab Nat Med, Nanjing, Jiangsu, Peoples R China; [Huang, Wenlong] China Pharmaceut Univ, Jiangsu Key Lab Drug Discovery Metab Dis, Nanjing, Jiangsu, Peoples R China published Discovery of aromatic amides with triazole-core as potent reversal agents against P-glycoprotein-mediated multidrug resistance in 2019, Cited 49. Category: phthalazines. The Name is 4-Nitrobenzoic acid. Through research, I have a further understanding and discovery of 62-23-7.
P-glycoprotein (P-gp)-mediated multidrug resistance (MDR) is a major impediment for clinical cancer therapy. 19 novel aromatic amides with triazole-core as MDR reversal agents were designed and synthesized via click chemistry 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.
Category: phthalazines. About 4-Nitrobenzoic acid, If you have any questions, you can contact Qiu, QQ; Zhu, JL; Chen, QT; Jiang, ZQ; Xu, JT; Jiang, XT; Huang, WL; Liu, ZQ; Ye, J; Xu, XJ or concate me.
Reference:
Phthalazine – Wikipedia,
,Phthalazine | C8H6N2 – PubChem