154650-16-5Relevant articles and documents
Dihydroisocoumarin derivative and preparation method and application thereof
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Paragraph 0039-0042; 0061-0065, (2022/01/10)
The present invention discloses a dihydroisocoumarin derivative and preparation method and application thereof, the dihydroisocoumarin derivative having a structure as shown in formula (I) or (II). The method of preparing dihydroisocoumarin derivatives of
Design, synthesis and biological evaluation of exiguamine A analogues as IDO1 inhibitors
Dong, Junmin,Pan, Xuan,Yang, Ying,Zhang, Guangyan,Xiao, Zhiyan,Liu, Zhanzhu
, (2021/06/22)
A series of exiguamine A analogues were designed and synthesized via 15 steps. Their inhibitory activities against IDO1 were tested and the structure-activity relationships were studied. Most compounds exhibited potent IDO1 inhibitory activities with IC50 values at the level of 10?7–10?8 M. Compound 21f was the most potent IDO1 inhibitor with an IC50 value of 65.3 nM, which was comparable with the positive control drug epacadostat (IC50 = 46 nM). Moreover, compound 21f showed higher selectivity for IDO1 over tryptophan 2,3-dioxygenase (TDO) and no cytotoxicity at its effective concentration, rending it justifiable for further optimization and evaluation.
QUINOXALINE DERIVATIVES
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Page/Page column 84, (2021/07/24)
The present invention relates to compounds according to general formula (I), which act as modulators of the glucocorticoid receptor and can be used in the treatment and/or prophylaxis of disorders which are at least partially mediated by the glucocorticoid receptor.