273399-95-4Relevant articles and documents
Synthesis and biological activity of squaramido-tethered bisbenzimidazoles as synthetic anion transporters
Wang, Zhong-Kun,Hong, Xiao-Qiao,Hu, Jinhui,Xing, Yuan-Yuan,Chen, Wen-Hua
, p. 3972 - 3980 (2021/02/02)
A series of squaramido-tethered bisbenzimidazoles were synthesized from the reaction of diethyl squarate with substituted 2-aminomethylbenzimidazoles. These conjugates exhibit moderate binding affinity toward chloride anions. They are able to facilitate the transmembrane transport of chloride anions most probably via an anion exchange process, and tend to be more active at acidic pH than at physiological pH. The viability of these conjugates toward four selected solid tumor cell lines was evaluated using an MTT assay and the results suggest that some of these conjugates exhibit moderate cytotoxicity probably in an apoptotic fashion.
Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer
Monastyrskyi, Andrii,Nilchan, Napon,Quereda, Victor,Noguchi, Yoshihiko,Ruiz, Claudia,Grant, Wayne,Cameron, Michael,Duckett, Derek,Roush, William
, p. 590 - 602 (2018/01/01)
Casein kinase 1δ/ε have been identified as promising therapeutic target for oncology application, including breast and brain cancer. Here, we described our continued efforts in optimization of a lead series of purine scaffold inhibitors that led to identification of two new CK1δ/ε inhibitors 17 and 28 displaying low nanomolar values in antiproliferative assays against the human MDA-MB-231 triple negative breast cancer cell line and have physical, in vitro and in vivo pharmacokinetic properties suitable for use in proof of principle animal xenograft studies against human cancers.
ANTI-INFECTIVE COMPOUNDS
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Page/Page column 45, (2015/02/25)
The present invention relates to small molecule compounds and their use in the treatment of bacterial infections, in particular Tuberculosis.