Pan, Liangkun; Zheng, Qiang; Chen, Yu; Yang, Rui; Yang, Yanyan; Li, Zhongjun; Meng, Xiangbao published the artcile< Design, synthesis and biological evaluation of novel naphthoquinone derivatives as IDO1 inhibitors>, Recommanded Product: Thiazole-5-carboxyaldehyde, the main research area is naphthoquinone derivative preparation indoleamine dioxygenase inhibitor anticancer activity SAR; Cancer immunotherapy; Indoleamine 2,3-dioxygenase 1; Naphthoquinone derivatives; Tryptophan 2,3-dioxygenase.
Indoleamine 2,3-dioxygenase 1 mediated kynurenine pathway of tryptophan degradation is identified as an appealing and novel target in immunotherapy for the treatment of cancer. In this study, a novel series of naphthoquinone derivatives were synthesized, characterized and evaluated for their inhibitory activities against IDO1, and their structure-activity relationship was investigated. Among them, five compounds, e.g., I,displayed potent IDO1 inhibitory activities with IC50 values ranging between 18 and 61 nM, which are more potent than INCB024360 undergoing clin. trial III evaluation. In addition, three compounds, e.g. II, decreased the kynurenine levels in rat plasma by 30%-50%. Compounds exhibiting excellent IDO1 inhibitory activities were also evaluated for their inhibitory activities against tryptophan 2,3-dioxygenase (TDO). Of which, compound II (IDO1 IC50 = 120 nM) showed promising TDO inhibition (IC50 72 nM) and was identified as an IDO1/TDO dual inhibitor.
European Journal of Medicinal Chemistry published new progress about Antitumor agents. 1003-32-3 belongs to class thiazole, and the molecular formula is C4H3NOS, Recommanded Product: Thiazole-5-carboxyaldehyde.
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica