1248587-70-3Relevant academic research and scientific papers
Efficient photocaging of a tight-binding bisubstrate inhibitor of cAMP-dependent protein kinase
S?rmus, Tanel,Lavogina, Darja,Enkvist, Erki,Uri, Asko,Viht, Kaido
, p. 11147 - 11150 (2019)
Photocaging of a tight-binding bisubstrate inhibitor of cAMP-dependent protein kinase (PKA) with a nitrodibenzofuran-based group fully abolished its inhibitory potency. The affinity difference between the photocaged and the active inhibitor was over 5 orders of magnitude. The photocaged inhibitor disrupted the PKA holoenzyme in cell lysates upon photolysis under a 398 nm LED.
Alpha,beta-unsaturated ketone compound containing aromatic heterocycles and preparation method and application thereof
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Paragraph 0113-0114; 0119-0120, (2018/11/27)
The invention provides an alpha,beta-unsaturated ketone compound containing aromatic heterocycles and a preparation method and an application thereof. The compound has strong anti-tumor activity, andhas a structure represented by the formula (I) defined in the specification.
Aminomethyl-containing piperazinone compound as well as preparation method and application thereof
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Paragraph 0120; 0121; 0124; 0125, (2018/09/28)
The invention discloses an aminomethyl-containing piperazinone compound as well as a preparation method and application thereof. The compound has a structure shown as a general formula (I). The invention further provides the preparation method and the application of the compound. The compound disclosed by the invention has certain activity of inhibiting AKT1 kinase and activity of inhibiting the growth of PC-3 tumor cells, and is used for preparing an anti-tumor medicine. The formula I is shown in the description.
Structural optimization elaborates novel potent Akt inhibitors with promising anticancer activity
Liu, Yang,Yin, Yanzhen,Zhang, Zhen,Li, Carrie J.,Zhang, Hui,Zhang, Daoguang,Jiang, Changying,Nomie, Krystle,Zhang, Liang,Wang, Michael L.,Zhao, Guisen
, p. 543 - 551 (2017/07/12)
Targeting of Akt has been validated as a well rationalized approach to cancer treatment, and represents a promising therapeutic strategy for aggressive hematologic malignancies. We describe herein an exploration of novel Akt inhibitors for cancer therapy through structural optimization of previously described 4-(piperazin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine derivatives. Our studies yielded a novel series of pyrrolopyrimidine based phenylpiperidine carboxamides capable of potent inhibition of Akt1. Notably, 10h exhibited robust antiproliferative effects in both mantle cell lymphoma cell lines and primary patient tumor cells. Low micromolar doses of 10h induced cell apoptosis and cell cycle arrest in G2/M phase, and significantly downregulated the phosphorylation of Akt downstream effectors GSK3β and S6 in Jeko-1 cells.
A nitrogen-containing heterocyclic phenyl piperidine compound and its preparation method and application
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Paragraph 0047-0051, (2017/09/01)
The invention discloses a nitrogen-containing heterocyclic phenyl piperidine compound or pharmaceutical salt thereof. The general structural formula a of the compound is as shown in specification, wherein R represents hydrogen, mono-substituted or poly-substituted halogen, methyl, methoxyl, tertiary butyl or trifluoromethyl; and R2 is hydrogen, chlorine, bromine, methyl or ethyl. The compound disclosed by the invention is novel in structure; and by introducing the active amino in the form of a piperidine ring, the configuration of the side-chain amino is reinforced and the rigidity of the compound is enhanced. Through the design transformation, the Akt1 kinase inhibitory activity and the PC-3 cell line growth inhibitory activity of the compound are significantly enhanced.
Discovery of 4-(Piperazin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine Derivatives as Akt Inhibitors
Liu, Yang,Yin, Yanzhen,Zhang, Jingya,Nomie, Krystle,Zhang, Liang,Yang, Dezhi,Wang, Michael L.,Zhao, Guisen
, p. 356 - 362 (2016/05/19)
A series of 4-(piperazin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine derivatives was synthesized and evaluated as Akt inhibitors by optimization of a weak screening lead (1). Typically, compounds 5q and 5t significantly improved the Akt1 inhibitory potency with IC
Palladium-catalyzed amination of unprotected halo-7-azaindoles
Henderson, Jaclyn L.,McDermott, Sarah M.,Buchwald, Stephen L.
supporting information; experimental part, p. 4438 - 4441 (2010/12/20)
Simple and efficient procedures for the Pd-catalyzed cross-coupling of primary and secondary amines with halo-7-azaindoles(pyrrolo[2,3-b]pyridine) are presented. Previously, no general method was available to ensure the highly selective reaction of the heteroaryl halide in the presence of the unprotected azaindole N-H. Using palladium precatalysts recently reported by our group, such reactions are easily accomplished under mild conditions that can be applied to cross-coupling reactions with a wide array of aliphatic and aromatic amines.
AKT PROTEIN KINASE INHIBITORS
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Page/Page column 111, (2008/06/13)
The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula: A-L-CR where CR is a cyclical core group, L is a linking group and A is as defined herein. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
