1119076-06-0Relevant articles and documents
Design, synthesis, nitric oxide release and antibacterial evaluation of novel nitrated ocotillol-type derivatives
Bi, Yi,Yang, Xiao,Zhang, Tingting,Liu, Zeyun,Zhang, Xiaochen,Lu, Jing,Cheng, Keguang,Xu, Jinyi,Wang, Hongbo,Lv, Guangyao,Lewis, Peter John,Meng, Qingguo,Ma, Cong
, p. 71 - 80 (2015)
Abstract Nitric oxide (NO) and its auto-oxidation products are known to disrupt normal bacterial function and NO releasing molecules have the potential to be developed as antibacterial leads in drug discovery. We have designed and synthesized a series of
Discovery and synthesis of 3- and 21-substituted fusidic acid derivatives as reversal agents of P-glycoprotein-mediated multidrug resistance
Guo, Mengqi,Ren, Qianwen,Wang, Binghua,Ji, Wentao,Ni, Jingxuan,Feng, Yaqi,Bi, Yi,Tian, Jingwei,Wang, Hongbo
, (2019)
In this study, we synthesized 23 fusidic acid (FA) derivatives and screened them for tumor drug resistance reversal activity and cytotoxicity toward the KBV (multidrug-resistant oral epidermoid carcinoma) cell line based on MTT assay. Tumor resistance reversal activity of fusidic acid (FA) derivatives was discovered for the first time. Our results showed that compound 1 enhanced the cytotoxicity of paclitaxel toward the drug-resistant KBV cells at a concentration of 5 μM. And compound 1 sensitized KBV cells toward paclitaxel in arresting cells in the G2/M phase and inducing cell apoptosis. Further researches showed that compound 1 inhibited the drug efflux activity of P-glycoprotein (P-gp) by increasing the ATPase activity of P-gp without affecting its expression. The structure-activity relationships (SARs) of the FA derivatives were also preliminarily investigated. Our findings indicate that compound 1 is a promising lead compound for designing FA derivatives with improved tumor drug resistance reversal activity in the future.
Design, synthesis and biological evaluation of novel α-hederagenin derivatives with anticancer activity
Liu, Xian-xuan,Yang, Yan-ting,Wang, Xiao,Wang, Kai-yi,Liu, Jia-qi,Lei, Lei,Luo, Xiao-min,Zhai, Rong,Fu, Feng-hua,Wang, Hong-bo,Bi, Yi
, p. 427 - 439 (2017/10/17)
In an attempt to arrive at a more potent cytotoxic agent than the parent compound α-hederagenin (H), 24 α-hederagenin derivatives (5–8, 11–24, 27–28, 31–32, and 35–36) were synthesized in a concise and efficient strategy and screened for in vitro cytotoxicity against the human cancer cell lines MKN45 and KB. Among these compounds, the polyamine derivative 15 exhibited more potency than the parent compound with IC50 values in the range of 4.22 μM–8.05 μM. Compound 15 increased Bax/bcl-2 ratio that disrupted the mitochondrial potential and induced apoptosis. Therefore, the present studies highlight the importance of polyamine derivatives of α-hederagenin in the discovery and development of novel anticancer agents.
Iodination of verapamil for a stronger induction of death, through GSH efflux, of cancer cells overexpressing MRP1
Barattin, Régis,Perrotton, Thomas,Trompier, Doriane,Lorendeau, Doriane,Pietro, Attilio Di,D'Hardemare, Amaury Du Moulinet,Baubichon-Cortay, Hélne
experimental part, p. 6265 - 6274 (2010/10/19)
The multidrug resistance protein 1 (MRP1), involved in multidrug resistance (MDR) of cancer cells, was found to be modulated by verapamil, through stimulation of GSH transport, leading to apoptosis of MRP1-overexpressing cells. In this study, various iodi
