63633-46-5Relevant academic research and scientific papers
Discovery of AG-270, a First-in-Class Oral MAT2A Inhibitor for the Treatment of Tumors with Homozygous MTAP Deletion
Konteatis, Zenon,Travins, Jeremy,Gross, Stefan,Marjon, Katya,Barnett, Amelia,Mandley, Everton,Nicolay, Brandon,Nagaraja, Raj,Chen, Yue,Sun, Yabo,Liu, Zhixiao,Yu, Jie,Ye, Zhixiong,Jiang, Fan,Wei, Wentao,Fang, Cheng,Gao, Yi,Kalev, Peter,Hyer, Marc L.,Delabarre, Byron,Jin, Lei,Padyana, Anil K.,Dang, Lenny,Murtie, Joshua,Biller, Scott A.,Sui, Zhihua,Marks, Kevin M.
supporting information, p. 4430 - 4449 (2021/05/06)
The metabolic enzyme methionine adenosyltransferase 2A (MAT2A) was recently implicated as a synthetic lethal target in cancers with deletion of the methylthioadenosine phosphorylase (MTAP) gene, which is adjacent to the CDKN2A tumor suppressor and codelet
INHIBITORS OF CELLULAR METABOLIC PROCESSES
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Page/Page column 175-176, (2018/03/25)
The invention provides inhibitor compounds of MAT2A that are useful as therapeutic agents for treating malignancies wherein the compounds have the general formula (I) : wherein ring A, ring B, ring C and, R1 are as described herein.
Synthesis of pyrazolo[5,1-d][1,2,3,5]tetrazine-4(3H)-ones
Gao, Yaojun,Lam, Yulin
experimental part, p. 69 - 74 (2010/10/04)
A solid-phase synthesis of 5-aminopyrazole has been developed and applied to the preparation of pyrazolo[5,1-d]-[1,2,3,5]tetrazine-4(3H)-ones. In this strategy, a one-pot reaction from 5-aminopyrazoles to the pyrazolo[5,1-d]-[1,2, 3,5]tetrazine-4(3H)-ones which provided the compounds in good yields was demonstrated. Using this synthetic strategy, we prepared a representative set of 16 pyrazolo[5,1-d][l,2,3,5]tetrazine-4(3H)-ones.
The conversion of isothiazoles into pyrazoles using hydrazine
Ioannidou, Heraklidia A.,Koutentis, Panayiotis A.
scheme or table, p. 7023 - 7037 (2009/12/06)
The conversion of isothiazoles into pyrazoles on treatment with hydrazine is investigated. The influence of various C-3, C-4 and C-5 isothiazole substituents and some limitations of this ring transformation are examined. When the isothiazole C-3 substituent is a good nucleofuge, 3-aminopyrazoles are obtained. However, when the 3-substituent is not a leaving group it is retained in the pyrazole product. Treatment of 4-bromo-3-chloro-5-phenylisothiazole 56 or 3-chloro-4,5-diphenylisothiazole 57 with anhydrous hydrazine at ca. 200 °C for a few minutes gives the corresponding 3-hydrazinoisothiazoles 61 and 64 respectively in high yields; the stability of these new hydrazines is investigated. 5,5′-Diphenyl-3,3′-biisothiazole-4,4′-dicarbonitrile 78 reacts with hydrazine to give 5,5′-diphenyl-3,3′-bi(1H-pyrazole)-4,4′-dicarbonitrile 79. Methylhydrazine reacts with 3-chloro-5-phenylisothiazole-4-carbonitrile 1 to give 3-(1-methylhydrazino)-5-phenylisothiazole-4-carbonitrile 83 and 3-amino-1-methyl-5-phenylpyrazole-4-carbonitrile 84. All products are fully characterised and rational mechanisms for the isothiazole into pyrazole transformation are proposed.
Pyrazolo[1,5-α]pyrimidines: Estrogen receptor ligands possessing estrogen receptor β antagonist activity
Compton, Dennis R.,Sheng, Shubin,Carlson, Kathryn E.,Rebacz, Natalie A.,Lee, In Young,Katzenellenbogen, Benita S.,Katzenellenbogen, John A.
, p. 5872 - 5893 (2007/10/03)
In our search for novel subtype-selective estrogen receptor (ER) ligands, we have examined various heterocyclic units as core structural elements. Here, we have investigated the fused, bicyclic pyrazolo[1,5-a]pyrimidine core, which is a system that allows
Pyrazolo[1,5-a]pyrimidines as estrogen receptor ligands: Defining the orientation of a novel heterocyclic core
Compton, Dennis R.,Carlson, Kathryn E.,Katzenellenbogen, John A.
, p. 5681 - 5684 (2007/10/03)
We investigated the pyrazolo[1,5-a]pyrimidine system as a novel heterocyclic scaffold for the development of estrogen receptor (ER) ligands. By altering the pattern of hydroxyl substitution, we established the orientation that is most favorable for ER bin
