Reference of 6-Morpholinobenzo[d]thiazol-2-amineOn October 30, 2014 ,《Design, synthesis, and structure-activity relationships of novel benzothiazole derivatives bearing the ortho-hydroxy N-carbamoylhydrazone moiety as potent antitumor agents》 was published in European Journal of Medicinal Chemistry. The article was written by Ma, Junjie; Chen, Dong; Lu, Kuan; Wang, Lihui; Han, Xiaoqi; Zhao, Yanfang; Gong, Ping. The article contains the following contents:
A series of novel benzothiazole derivatives bearing the ortho-hydroxy N-carbamoylhydrazone moiety were designed and synthesized and their cytotoxic activities against five cancer cell lines (NCI-H226, SK-N-SH, HT29, MKN45, and MDA-MB-231) were screened in vitro. Most of them showed moderate to excellent activity against all the tested cell lines. Two compounds (procaspase-3 EC50 = 1.42 μM and procaspase-3 EC50 = 0.25 μM) exhibited excellent antitumor activity with IC50 values ranging from 0.14 μM to 0.98 μM against all cancer cell lines, which were 1.8-8.7 times more active than the first procaspase activating compound (PAC-1) (procaspase-3 EC50 = 4.08 μM). The structure-activity relationship analyses indicated that the introduction of a lipophilic group (a benzyloxy or heteroaryloxy group) at the 4-position of the 2-hydroxyphenyl ring was beneficial to antitumor activity, and the presence of substituents containing nitrogen that are pos. charged at physiol. pH could also improve antitumor activity. It was also confirmed that the steric effect of the 4-position substituent of the benzyloxy group had a significant influence on cytotoxic activity.6-Morpholinobenzo[d]thiazol-2-amine(cas: 94641-22-2Reference of 6-Morpholinobenzo[d]thiazol-2-amine) was used in this study.
6-Morpholinobenzo[d]thiazol-2-amine(cas: 94641-22-2) belongs to thiazoles. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities.Reference of 6-Morpholinobenzo[d]thiazol-2-amineTheir presence in peptides or their ability to bind proteins, DNA and RNA has led to many synthetic studies and new applications.
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica