15050-24-5Relevant articles and documents
Macrocyclic squaramides as ion pair receptors and fluorescent sensors selective towards sulfates
Zaleskaya, Marta,Jagleniec, Damian,Romański, Jan
, p. 3904 - 3915 (2021)
Through the high dilution technique, we obtained macrocyclic ion pair receptorsR1andR2, an anion receptorR3, and a fluorescent sensorR4using a combination of particular members of simple libraries consisting of synthesized diamines and methyl squarates, r
Multikilogram Synthesis of a Potent Dual Bcl-2/Bcl-xL Antagonist. 1. Manufacture of the Acid Moiety and Development of Some Key Reactions
Hardouin, Christophe,Baillard, Sandrine,Barière, Fran?ois,Copin, Chloé,Craquelin, Anthony,Janvier, Solenn,Lemaitre, Sylvain,Le Roux, Stéphane,Russo, Olivier,Samson, Sébastien
, p. 652 - 669 (2019/12/24)
Our efforts toward the process development of drug candidate 1 are described in a series of two papers. This manuscript focuses on the synthesis of kilogram quantities of acid precursor 2 to provide batches of material for preclinical studies and first-in
Hybrids of arenobufagin and benzoisoselenazol reducing the cardiotoxicity of arenobufagin
Hou, Wen,Huang, Zhi-Xing,Xu, Hong-Gui,Lin, Jing,Zhang, Dong-Mei,Peng, Qun-Long,Lin, Hui,Chang, Yi-Qun,Wang, Long-Hai,Yao, Zhe,Sun, Ping-Hua,Chen, Wei-Min
, p. 3391 - 3394 (2018/09/11)
Arenobufagin is a naturally occurring bufadienolide showing promising antitumor activity accompanied however with apparent cardiac toxicity. Following the recent discovery that oxidative damage possibly be an important cause of the cardiac toxicity of cardenolides, a strategy fusing the antitumor agent arenobufagin with a benzoisoselenazol fragment, a reactive oxygen species (ROS) scavenger, has been developed. Six novel hybrids were synthesized and their ROS scavenging activities as well as their in vitro cytotoxicity against the human hepatocellular carcinoma cell line HepG2, an adriamycin-resistant subline HepG2/ADM, and the human myocardial cell line AC16 were evaluated. The results indicate that the hybrids exhibit various degrees of in vitro ROS scavenging activities, and weaker cytotoxicity than that of arenobufagin against the myocardial cell line AC16. These findings suggest the feasibility of a strategy in which the cardiotoxicity of the potential antitumor agent arenobufagin is reduced.