39070-63-8Relevant articles and documents
MEBENDAZOLE POLYMORPH FOR TREATMENT AND PREVENTION OF TUMORS
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, (2016/09/22)
Mebendazole is an antiparasitic drug with over 40 years of safe use. Recently mebendazole was repurposed for glioblastoma therapy. Three polymorphs of mebendazole exist, but the relative polymorph content for existing drugs varies, and the therapeutic anti-cancer relevance of the different polymorphs was unknown. As an oral drug mebendazole polymorph C is a superior form, and it reaches the brain and brain tumors in effective concentrations. Efficacy is further improved by combining mebendazole with a P-glycoprotein inhibitor. Mebendazole may also be used for therapy of other cancers, as well as a chemo-preventative agent.
Design and synthesis of a novel candidate compound NTI-007 targeting sodium taurocholate cotransporting polypeptide [NTCP]-APOA1-HBx-Beclin1-mediated autophagic pathway in HBV therapy
Zhang, Jin,Fu, Lei-Lei,Tian, Mao,Liu, Hao-Qiu,Li, Jing-Jing,Li, Yan,He, Jun,Huang, Jian,Ouyang, Liang,Gao, Hui-Yuan,Wang, Jin-Hui
, p. 976 - 984 (2015/03/04)
Sodium taurocholate cotransporting polypeptide (NTCP) is a multiple transmembrane transporter predominantly expressed in the liver, functioning as a functional receptor for HBV. Through our continuous efforts to identify NTCP as a novel HBV target, we designed and synthesized a series of new compounds based on the structure of our previous compound NT-5. Molecular docking and MD simulation validated that a new compound named NTI-007 can tightly bind to NTCP, whose efficacy was also measured in vitro virological examination and cytotoxicity studies. Furthermore, autophagy was observed in NTI-007 incubated HepG2.2.15 cells, and results of q-PCR and Western blotting revealed that NTI-007 induced autophagy through NTCP-APOA1-HBx-Beclin1-mediated pathway. Taken together, considering crucial role of NTCP in HBV infection, NTCP-mediated autophagic pathway may provide a promising strategy of HBV therapy and given efficacy of NTI-007 triggering autophagy. Our study suggests pre-clinical potential of this compound as a novel anti-HBV drug candidate.
6-Lithioquinoxalines and Their Transformations
Dobrodei,El'tsov
, p. 620 - 629 (2007/10/03)
6-Bromo-2,3-diphenylquinoxaline reacts with butyllithium to give the 6-lithio derivative in a yield of more than 80%, which reacts with electrophiles such as benzophenone, Michler ketone, methyl ethyl ketone, iodine, selenium, and dimethylformamide to give the corresponding quinoxaline derivatives. 6-Bromo-2,3-dimethylquinoxaline is metallated with butyl- and phenyllithium at the methyl groups and benzene ring. These organolithium compounds react with benzophenone to give the corresponding diphenyl- and triaryl-carbinols, whose yield and ratio were determined by HPLC. These results open prospects for preparing new quinoxaline derivatives substituted at the annelated benzene ring.