Inhibitors of unactivated p38 MAP kinase

Bullington, James L.; Argentieri, Dennis; Averill, Kristin; Carter, Demetrius; Cavender, Druie; Fahmy, Bohumila; Fan, Xiaodong; Hall, Daniel; Heintzelman, Geoffrey R.; Jackson, Paul F.; Leung, Wai Ping; Li, Xun; Ling, Ping; Olini, Gilbert C.; Razler, Thomas M.; Reuman, Michael; Rupert, Kenneth C.; Russell, Ronald K.; Siekierka, John; Wadsworth, Scott; Wolff, Russell R.; Xiang, Bangping; Zhang, Yue Mei

doi:10.1016/j.bmcl.2006.08.101

Cited by 12 publications

(9 citation statements)

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“…Bullington and co-workers (Johnson & Johnson) prepared p38 map kinase inhibitor 582 for potential treatment of inflammatory diseases in excellent yield (93%) by reacting sterically congested 2-bromopyrrole 580 and acetylpiperazine 581 in the presence of Pd(OAc) 2 / L6 ( Scheme 142 a). 486 Additionally, Hanan and co-workers (Genentech) constructed a series of epidermal growth factor receptor (EGFR) inhibitors 586 via two consecutive C–N coupling steps. 487 First, aryl iodide 583 was combined with an ammonia equivalent in the presence of an L7 -based catalyst to yield intermediate 584 in 58% yield ( Scheme 142 b).…”

Section: Five-membered Heteroaryl Halidesmentioning

confidence: 99%

“…A variety of catalysts promote these C–N coupling reactions, although no examples involved five-membered heteroaryl halides bearing a free NH group. Bullington and co-workers (Johnson & Johnson) prepared p38 map kinase inhibitor 582 for potential treatment of inflammatory diseases in excellent yield (93%) by reacting sterically congested 2-bromopyrrole 580 and acetylpiperazine 581 in the presence of Pd(OAc) 2 / L6 (Scheme a) . Additionally, Hanan and co-workers (Genentech) constructed a series of epidermal growth factor receptor (EGFR) inhibitors 586 via two consecutive C–N coupling steps .…”

Section: Five-membered Heteroaryl Halidesmentioning

confidence: 99%

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Applications of Palladium-Catalyzed C–N Cross-Coupling Reactions

2016

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Pd-catalyzed cross-coupling reactions that form C–N bonds have become useful methods to synthesize anilines and aniline derivatives, an important class of compounds throughout chemical research. A key factor in the widespread adoption of these methods has been the continued development of reliable and versatile catalysts that function under operationally simple, user-friendly conditions. This review provides an overview of Pd-catalyzed N-arylation reactions found in both basic and applied chemical research from 2008 to the present. Selected examples of C–N cross-coupling reactions between nine classes of nitrogen-based coupling partners and (pseudo)aryl halides are described for the synthesis of heterocycles, medicinally relevant compounds, natural products, organic materials, and catalysts.

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Section: Five-membered Heteroaryl Halidesmentioning

confidence: 99%

Section: Five-membered Heteroaryl Halidesmentioning

confidence: 99%

Applications of Palladium-Catalyzed C–N Cross-Coupling Reactions

2016

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“…In addition, this compound also inhibits MAPK-activated protein kinase 2 (MAPKAPK2) and cytokine synthesis. Compound 31, a pyrimidinyl imidazole derivative, has a strong inhibitory efficacy on the unactivated p38, whereas its inhibitory efficacy on the activated p38 is pretty poor [20].…”

Section: P38 Pathway Inhibitorsmentioning

confidence: 99%

Mitogen-activated protein kinase pathway inhibitors: inhibitors for diseases?

Gong

2010

Front. Med. China

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Mitogen-activated protein kinase (MAPK) signaling pathway, one of the most important signaling pathways in eukaryotic organism, is involved in multiple cellular events such as cell growth, differentiation, and apoptosis. MAPK is of great importance to the normal function of organisms, while its dysfunction results in various diseases. So far, inhibitors specifically against each subfamilies of MAP kinase have been developed, while more endeavors are needed to discover the compounds selectively targeting a particular subfamily member. Most of the kinase inhibitors exert their functions in an ATPcompetitive way or a non-ATP-competitive way. Further studies on the effective mechanism of the MAPK inhibitors and their therapeutic roles in the treatment of diseases are helpful for the illumination of MAP kinase function, the development of novel inhibitors, and the therapy of diseases caused by the dysfunction of the MAPK pathway.

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“…As an example, pyrroles connected with imine-bearing azaarenes at the 3-position through a C–C bond are the privileged structural motifs of an enormous variety of bioactive molecules and chemosensors ( Scheme 1a ). 1 Structurally, the representative molecules A–F robustly indicate that distinct azaaryl groups and substituents as well as diverse substitution patterns would endow various important application potentials for such special pyrrole derivatives. To date, several direct functionalization examples via coupling pyrroles and derivatives with azaarene-based substrates have been described by Buchwald, Ellman and Bergman et al , which represent efficient approaches to afford simple 3-azaarene-substituted pyrroles.…”

Section: Introductionmentioning

confidence: 99%