92767-14-1Relevant articles and documents
Design, synthesis and in vitro evaluation of amidoximes as histone deacetylase inhibitors for cancer therapy
Jiao, Peifu,Jin, Peng,Li, Chencan,Cui, Lechao,Dong, Lihua,Pan, Bin,Song, Wentong,Ma, Liang,Dong, Jinlong,Song, Lei,Jin, Xinjie,Li, Faming,Wan, Maosheng,Lv, Zhitao,Geng, Qiaohong
, p. 4679 - 4683 (2016)
Amindoximes are geometric isomers of N-hydroxyamidines which are bioisosteres of hydroxamates. Since amindoxime group is capable of chelating transition metal ions including zinc ion, amindoximes should possess histone deacetylases (HDACs) inhibitory activity. In this work, we designed and synthesized a series of amindoximes, examined their inhibitory activities against HDACs, and investigated their cytotoxicity to human cancer cells. Preliminary results demonstrated that amindoximes possessed submicromolar HDACs inhibitory activity, with noteworthy enhancement compared with hydroxamates. Furthermore, the amindoximes arrested HCT116 and A549 cells in G2/M phase and showed good efficacy in inducing cells death. We provided a proof-of-concept that amindoximes could be used as HDACs inhibitors and hold great promise as epigenetic drugs.
Structure-activity relationship study of selective benzimidazole-based inhibitors of Cryptosporidium parvum IMPDH
Kirubakaran, Sivapriya,Gorla, Suresh Kumar,Sharling, Lisa,Zhang, Minjia,Liu, Xiaoping,Ray, Soumya S.,MacPherson, Iain S.,Striepen, Boris,Hedstrom, Lizbeth,Cuny, Gregory D.
scheme or table, p. 1985 - 1988 (2012/04/05)
Cryptosporidium parasites are important waterborne pathogens of both humans and animals. The Cryptosporidium parvum and Cryptosporidium hominis genomes indicate that the only route to guanine nucleotides is via inosine 5′-monophosphate dehydrogenase (IMPDH). Thus the inhibition of the parasite IMPDH presents a potential strategy for treating Cryptosporidium infections. A selective benzimidazole-based inhibitor of C. parvum IMPDH (CpIMPDH) was previously identified in a high throughput screen. Here we report a structure-activity relationship study of benzimidazole-based compounds that resulted in potent and selective inhibitors of CpIMPDH. Several compounds display potent antiparasitic activity in vitro.