925672-88-4Relevant academic research and scientific papers
Nickel-Catalyzed Tandem Reaction of Functionalized Arylacetonitriles with Arylboronic Acids in 2-MeTHF: Eco-Friendly Synthesis of Aminoisoquinolines and Isoquinolones
Zhen, Qianqian,Chen, Lepeng,Qi, Linjun,Hu, Kun,Shao, Yinlin,Li, Renhao,Chen, Jiuxi
supporting information, p. 106 - 111 (2019/12/11)
The first example of the nickel-catalyzed tandem addition/cyclization of 2-(cyanomethyl)benzonitriles with arylboronic acids in 2-MeTHF has been developed, which provides the facile synthesis of aminoisoquinolines with good functional group tolerance under mild conditions. This chemistry has also been successfully applied to the synthesis of isoquinolones by the tandem reaction of methyl 2-(cyanomethyl)benzoates with arylboronic acids. The use of the bio-based and green solvent 2-MeTHF as the reaction medium makes the synthesis process environmentally benign. The synthetic utility of this chemistry is also indicated by the synthesis of biologically active molecules.
Regioselective Access to 3-Aryl-1-aminoisoquinolines via Nickel(I)-Catalyzed C-C and C-N Cascade Coupling Reactions from the Substituted 2-(Cyanomethyl)benzonitriles
Yang, Xicheng,Yu, Haihua,Xu, Yulong,Shao, Liming
, p. 9682 - 9695 (2018/09/06)
A novel and regioselective Ni(I) catalyzed C-C and C-N cascade coupling reactions has been developed. The cascade furnishes atom-economic access to 40 3-aryl-1-aminoisoquinolines. The regioselectivity of C(sp3)-cyano group over C(sp2
Isoquinoline-1,3-diones as Selective Inhibitors of Tyrosyl DNA Phosphodiesterase II (TDP2)
Kankanala, Jayakanth,Marchand, Christophe,Abdelmalak, Monica,Aihara, Hideki,Pommier, Yves,Wang, Zhengqiang
supporting information, p. 2734 - 2746 (2016/04/10)
Tyrosyl DNA phosphodiesterase II (TDP2) is a recently discovered enzyme that specifically repairs DNA damages induced by topoisomerase II (Top2) poisons and causes resistance to these drugs. Inhibiting TDP2 is expected to enhance the efficacy of clinically important Top2-targeting anticancer drugs. However, TDP2 as a therapeutic target remains poorly understood. We report herein the discovery of isoquinoline-1,3-dione as a viable chemotype for selectively inhibiting TDP2. The initial hit compound 43 was identified by screening our in-house collection of synthetic compounds. Further structure-activity relationship (SAR) studies identified numerous analogues inhibiting TDP2 in low micromolar range without appreciable inhibition against the homologous TDP1 at the highest testing concentration (111 μM). The best compound 64 inhibited recombinant TDP2 with an IC50 of 1.9 μM. The discovery of this chemotype may provide a platform toward understanding TDP2 as a drug target.
FLUOROISOQUINOLINE SUBSTITUTED THIAZOLE COMPOUNDS AND METHODS OF USE
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Page/Page column 54-55, (2010/08/08)
The invention relates to thiazole compounds of Formula (I) and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein. The invention also relates to the therapeutic use of such thiazole compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.
THIADIAZOLE MODULATORS OF PKB
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Page/Page column 188-189, (2009/03/07)
The invention relates to thiazole compounds of Formula I and Formula II and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein. The invention also relates to the th
HETEROCYCLIC MODULATORS OF PKB
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Page/Page column 159, (2009/03/07)
The invention relates to heterocyclic compounds of Formula I and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein Formula (I). The invention also relates to the therapeutic use of such compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.
An efficient synthesis of 1,6- and 1,7-dibromo-3-aminoisoquinolines: versatile templates for the preparation of functionalized isoquinolines
Frohn, Mike,Bürli, Roland W.,Riahi, Bobby,Hungate, Randall W.
, p. 487 - 489 (2008/02/04)
An efficient synthetic route to 1,6- and 1,7-dibromo-3-aminoisoquinoline was devised. These intermediates served as ideal templates for the preparation of 3-aminoisoquinoline analogues functionalized at C(6) or C(7).
