Novel triapine derivative induces copper-dependent cell death in hematopoietic cancers was written by Chen, Ge;Niu, Chunyi;Yi, Jianhua;Sun, Lin;Cao, Hengyi;Fang, Yanjia;Jin, Taijie;Li, Ying;Lou, Chunli;Kang, Jingwu;Wei, Wanguo;Zhu, Jidong. And the article was included in Journal of Medicinal Chemistry in 2019.Category: thiazole This article mentions the following:
Triapine, an iron chelator that inhibits ribonucleotide reductase, has been evaluated in clin. trials for cancer treatment. Triapine in combination with other chemotherapeutic agents shows promising efficacy in certain hematol. malignancies; however, it is less effective against many advanced solid tumors, probably due to the unsatisfactory potency and pharmacokinetic properties. In this report, we developed a triapine derivative IC25 (10(I)) with potent antitumor activity. I preferentially inhibited the proliferation of hematopoietic cancers by inducing mitochondria reactive oxygen species production and mitochondrial dysfunction. Unlike triapine, I executed cytotoxic action in a copper-dependent manner. I-induced up-expression of thioredoxin-interacting protein resulted in decreased thioredoxin activity to permit c-Jun N-terminal kinase and p38 activation and ultimately led to the execution of the cell death program. Remarkedly, I showed good bioavailability and inhibited tumor growth in mouse xenograft models. Taken together, our study identifies I as a copper-dependent antitumor agent, which may be applied to the treatment of hematopoietic cancers. In the experiment, the researchers used many compounds, for example, 5,6-Dimethoxybenzo[d]thiazol-2-amine (cas: 6294-52-6Category: thiazole).
5,6-Dimethoxybenzo[d]thiazol-2-amine (cas: 6294-52-6) belongs to thiazole derivatives. Thiazoles frequently appear in peptide studies. Thiazoles can also be used as protected formyl groups, which can be released in later stages of complex natural product synthesis.Various laboratory methods exist for the organic synthesis of thiazoles. For example, 2,4-dimethylthiazole is synthesized from thioacetamide and chloroacetone.Category: thiazole
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica