Chen, Shulun; Guo, Wei; Liu, Xiaohua; Sun, Pu; Wang, Yi; Ding, Chunyong; Meng, Linghua; Zhang, Ao published the artcile< Design, synthesis and antitumor study of a series of N-Cyclic sulfamoylaminoethyl substituted 1,2,5-oxadiazol-3-amines as new indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors>, Name: (9Z,12Z)-Methyl octadeca-9,12-dienoate, the main research area is cyclic sulfamoylaminoethyloxadiazolamine preparation antitumor indoleamine dioxygenase inhibitor human; Immunotherapy; Indoleamine 2,3-dioxygenase; Life span; Oxadiazole; PD-1.
Indoleamine 2,3-dioxygenase 1 (IDO1) plays a key role in tryptophan catabolism which is an important mechanism in immune tolerance. The small mol. epacadostat is the most advanced IDO1 inhibitor, but its phase III trials as a single agent or in combinations with PD-1 antibody failed to show appreciable objective responses. To gain more insight on the antitumor efficacy of IDO1 inhibitors, a series of analogs of epacadostat by incorporating a cyclic aminosulfonamide moiety as the sidechain capping functionality has been designed. N-(3-bromo-4-fluorophenyl)-4-((2-(1,1-dioxido-1,2,5-thiadiazolidin-2-yl)ethyl)amino)-N’-hydroxy-1,2,5-oxadiazole-3-carboximidamide was found to display significant potency against recombinant hIDO1 and hIDO1 expressed HEK293 cancer cells and this compound has improved physico-chem. properties, acceptable PK parameters as well as optimal cardiac safety. Similar to epacadostat, the above compound is ineffective as single agent in the CT-26 syngeneic xenograft model, however, the combination of this compound with PD-1 antibody showed both elevated tumor growth inhibition and prolonged median life span.
European Journal of Medicinal Chemistry published new progress about Antitumor agents. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Name: (9Z,12Z)-Methyl octadeca-9,12-dienoate.
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics