55034-12-3Relevant articles and documents
Design, synthesis and biological evaluation of exiguamine A analogues as IDO1 inhibitors
Dong, Junmin,Liu, Zhanzhu,Pan, Xuan,Xiao, Zhiyan,Yang, Ying,Zhang, Guangyan
, (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.
Total synthesis of herbimycin A
Canova, Sophie,Bellosta, Veronique,Bigot, Antony,Mailliet, Patrick,Mignani, Serge,Cossy, Janine
, p. 145 - 148 (2007/10/03)
(Chemical Equation Presented) Hsp90 has recently emerged as a promising biological target for treatment of cancer. Herbimycin A and other members of the benzoquinoid ansamycin class of natural products are known to inhibit Hsp90 activity. The total synthesis of herbimycin A was achieved from the commercially available Roche ester 1 by using allylmetals to control the stereogenic centers at C6, C7, C10, C11, and C12 and a ring-closing metathesis to control the (Z)-double bond of the (E,Z)-dienic moiety.