929617-41-4Relevant academic research and scientific papers
Bioisosteric replacements of the indole moiety for the development of a potent and selective PI3Kδ inhibitor: Design, synthesis and biological evaluation
Yang, Chengbin,Xu, Chenyue,Li, Zhipeng,Chen, Yi,Wu, Tianze,Hong, Hui,Lu, Mingzhu,Jia, Yu,Yang, Yongtai,Liu, Xiaofeng,Deng, Mingli,Chen, Zhenxia,Li, Qingquan,Ling, Yun,Zhou, Yaming
supporting information, (2021/07/10)
Based on indole scaffold, a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor, namely FD223, was developed by the bioisosteric replacement drug discovery approach and studied for the treatment of acute myeloid leukemia (AML). In vitro
ARYL, HETEROARY, AND HETEROCYCLIC PHARMACEUTICAL COMPOUNDS FOR TREATMENT OF MEDICAL DISORDERS
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Page/Page column 48, (2018/09/21)
Complement Factor D inhibitors, pharmaceutical compositions, and uses thereof, as well as processes for their manufacture are provided. The compounds provided include Formula I, Formula II, Formula III, Formula IV, and Formula V, or a pharmaceutically acceptable salt, prodrug, isotopic analog, N-oxide, or isolated isomer thereof, optionally in a pharmaceutically acceptable composition. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade.
ERK INHIBITORS
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Page/Page column 133; 134, (2016/07/05)
The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are ERK2 inhibitors. The invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of Formula (I) and a pharmaceutically acceptable carrier. The invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of Formula (I) and an effective amount of at least one other pharmaceutically active ingredient (such as, for example, a chemotherapeutic agent), and a pharmaceutically acceptable carrier.
Design and synthesis of pyridine-pyrazolopyridine-based inhibitors of protein kinase B/Akt
Zhu, Gui-Dong,Gong, Jianchun,Gandhi, Viraj B.,Woods, Keith,Luo, Yan,Liu, Xuesong,Guan, Ran,Klinghofer, Vered,Johnson, Eric F.,Stoll, Vincent S.,Mamo, Mulugeta,Li, Qun,Rosenberg, Saul H.,Giranda, Vincent L.
, p. 2441 - 2452 (2007/10/03)
Thr-211 is one of three different amino acid residues in the kinase domain of protein kinase B/Akt as compared to protein kinase A (PKA), a closely related analog in the same AGC family. In an attempt to improve the potency and selectivity of our indazole-pyridine series of Akt inhibitors over PKA, efforts have focused on the incorporation of a chemical functionality to interact with the hydroxy group of Thr-211. Several substituents including an oxygen anion, amino, and nitro groups have been introduced at the C-6 position of the indazole scaffold, leading to a significant drop in Akt potency. Incorporation of a nitrogen atom into the phenyl ring at the same position (i.e., 9f) maintained the Akt activity and, in some cases, improved the selectivity over PKA. The structure-activity relationships of the new pyridine-pyrazolopyridine series of Akt inhibitors and their structural features when bound to PKA are also discussed.
