Discovery, synthesis and biological evaluation of isoquinolones as novel and highly selective JNK inhibitors (2)

Asano, Yasutomi; Kitamura, Shuji; Ohra, Taiichi; Itoh, Fumio; Kajino, Masahiro; Tamura, Tomoko; Kaneko, Minoru; Ikeda, Shota; Igata, Hideki; Kawamoto, Takahiro; Sogabe, Satoshi; Matsumoto, Shimpei; Tanaka, Toshimasa; Yamaguchi, Masashi; Kimura, Hiroyuki; Fukumoto, Shoji

doi:10.1016/j.bmc.2008.02.028

Cited by 78 publications

(37 citation statements)

References 15 publications

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“…128 Lead compound 57 was derived from an HTS campaign as well as by combining the knowledge from an early SAR study with results from similar JNK inhibitors reported from Takeda 129,130 (Fig. 24).…”

Section: Quinolones and Azaquinolonesmentioning

confidence: 99%

Inhibitors of c-Jun N-Terminal Kinases: An Update

2014

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The c-Jun N-terminal kinases (JNKs) are serine/threonine kinases implicated in the pathogenesis of various diseases. Recent advances in the development of novel inhibitors of JNKs will be reviewed. Significant progress in the design of JNK inhibitors displaying selectivity versus other kinases has been achieved within the past 4 years. However, the development of isoform selective JNK inhibitors is still an open task.

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Section: Quinolones and Azaquinolonesmentioning

confidence: 99%

Inhibitors of c-Jun N-Terminal Kinases: An Update

2014

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“…Dihydro‐ and tetrahydroisoquinoline ring systems are commonly found as the core in a wide variety of natural products and drug molecules. They are also versatile intermediates for the synthesis of therapeutic agents such as Lck kinase inhibitors, JNK inhibitors, Rho‐kinase inhibitors, PTB‐1B inhibitors, anti‐HIV agents, smooth muscle relaxants, antitumor agents (saframycin B), topoisomerase I inhibitors, and anticancer agents . Because of their immense biological importance, many efforts have been made to construct such scaffolds .…”

Section: Figurementioning

confidence: 99%

Cinchonamine Squaramide Catalyzed Asymmetric aza‐Michael Reaction: Dihydroisoquinolines and Tetrahydropyridines

2018

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The first example of ac hiral cinchona-squaramide catalyzede nantioselective intramolecular aza-Michael addition for the synthesis of dihydroisoquinolines and tetrahydropyridines has been developed. In general, good yields and excellent enantioselctivities were observed. Broad classes of Michael acceptors,s uch as enones,e sters,t hioesters,a nd Weinreb amides,w ere successful substrates.T he possibility of recycling the catalysts has also been demonstrated. An oxidation of combined enamine and keto functionalities on chiral dihydroisoquinolines leads to asingle diastereomer of an architecturally unprecedented tetracyclic core without loss in enantioselectivity. Figure 1. Representativebioactive compounds.

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“…Isoquinolinones. Isoquinolinones are reported to cause allosteric modulation of metabotropic glutamate receptor 2 [51], and also it has JNK inhibitory action [52]. An emerald procedure was developed utilizing an efficient catalyst; that is, ZnO nanoparticles mediated the synthesis of Narylhomophthalimides and benzannelated isoquinolinones.…”

Section: Synthesis Of N-arylhomophthalimides and Benzannelatedmentioning

confidence: 99%

Function of Nanocatalyst in Chemistry of Organic Compounds Revolution: An Overview

Hemalatha

Madhumitha

Kajbafvala

et al. 2013

Journal of Nanomaterials

103

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Heterocyclic motif is an important scaffold which has both industrial and pharmaceutical applications. These motifs can be prepared using wide variety of reaction conditions such as the use of expensive catalyst, toxic solvent, harsh reaction condition like the use of base, high temperature, and multistep reaction. Although various methods are involved, the chemistry arena is now shifted towards the greener way of synthesis. Nanocatalyst constitutes an important role in the green synthesis. This is because the activity of the catalyst resides in the exposed portion of the particles. By decreasing the size of the catalyst, advantages such as more surface area would be exposed to the reactant, only negligible amount would be required to give the significant result and selectivity could be achieved, thereby, eliminating the undesired products. The current review enlists the various types of nanocatalyst involved in the heterocyclic ring formation and also some other important functionalization over the ring.

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Discovery, synthesis and biological evaluation of isoquinolones as novel and highly selective JNK inhibitors (2)

Cited by 78 publications

References 15 publications

Inhibitors of c-Jun N-Terminal Kinases: An Update

Inhibitors of c-Jun N-Terminal Kinases: An Update

Cinchonamine Squaramide Catalyzed Asymmetric aza‐Michael Reaction: Dihydroisoquinolines and Tetrahydropyridines

Function of Nanocatalyst in Chemistry of Organic Compounds Revolution: An Overview

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