Liu, Liu published the artcileSyntheses, Biological Evaluations, and Mechanistic Studies of Benzo[c][1,2,5]oxadiazole Derivatives as Potent PD-L1 Inhibitors with In Vivo Antitumor Activity, Name: 2-Bromo-1-(bromomethyl)-3-iodobenzene, the publication is Journal of Medicinal Chemistry (2021), 64(12), 8391-8409, database is CAplus and MEDLINE.
A series of novel benzo[c][1,2,5]oxadiazole derivatives were designed, synthesized, and biol. evaluated as inhibitors of PD-L1. Among them, compound I [R = H] exhibited 1.8 nM IC50 value in a homogeneous time-resolved fluorescence (HTRF) assay, which was 20-fold more potent than the lead compound BMS-1016 (II). In the surface plasmon resonance (SPR) assay, compound I [R = H] bound to human PD-L1 (hPD-L1) with a KD value of 3.34 nM, without showing any binding to hPD-1. In the cell-based coculture assay, compound I [R = H] blocked PD-1/PD-L1 interaction with an EC50 value of 375 nM, while BMS-1016 had an EC50 value of 2075 nM. Moreover, compound I [R = Et] , an ester prodrug of compound I [R = H], was orally bioavailable and displayed significant antitumor effects in tumor models of syngeneic and PD-L1 humanized mice. Mechanistically, compound I [R = Et] exhibited significant in vivo antitumor effects probably through promoting antitumor immunity. Together, this series of benzoxadiazole PD-L1 inhibitors holds promise for tumor immunotherapy. Preclin. trials with selected compounds are ongoing in our laboratory
Journal of Medicinal Chemistry published new progress about 1261649-03-9. 1261649-03-9 belongs to iodides-buliding-blocks, auxiliary class Bromide,Iodide,Benzyl bromide,Benzene, name is 2-Bromo-1-(bromomethyl)-3-iodobenzene, and the molecular formula is C7H5Br2I, Name: 2-Bromo-1-(bromomethyl)-3-iodobenzene.
Referemce:
https://en.wikipedia.org/wiki/Iodide,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com