Synthesis, kinase inhibitory potencies and in vitro antiproliferative activity of isoindigo and 7′-azaisoindigo derivatives substituted by Sonogashira cross-coupling

Bouchikhi, Fadoua; Anizon, Fabrice; Moreau, Pascale

doi:10.1016/j.ejmech.2009.01.027

Cited by 21 publications

(7 citation statements)

References 10 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The exact mechanisms linking the trisomy of the chromosome 21 region that includes DYRK1A as well as other genes with the pathological phenotypes observed in DS are not well understood. However, a detailed analysis of several available mouse models of DS indicates that increased dosage of the DYRK1A gene is sufficient to induce learning defects in transgenic animals (Altafaj et al 2001;Bouchikhi et al 2009). …”

Section: Discussionmentioning

confidence: 99%

DYRK1A protein kinase promotes quiescence and senescence through DREAM complex assembly

Litovchick¹,

Florens²,

Swanson³

et al. 2011

Genes Dev.

272

364

View full text Add to dashboard Cite

In the absence of growth signals, cells exit the cell cycle and enter into G0 or quiescence. Alternatively, cells enter senescence in response to inappropriate growth signals such as oncogene expression. The molecular mechanisms required for cell cycle exit into quiescence or senescence are poorly understood. The DREAM (DP, RB [retinoblastoma] , E2F, and MuvB) complex represses cell cycle-dependent genes during quiescence. DREAM contains p130, E2F4, DP1, and a stable core complex of five MuvB-like proteins: LIN9, LIN37, LIN52, LIN54, and RBBP4. In mammalian cells, the MuvB core dissociates from p130 upon entry into the cell cycle and binds to BMYB during S phase to activate the transcription of genes expressed late in the cell cycle. We used mass spectroscopic analysis to identify phosphorylation sites that regulate the switch of the MuvB core from BMYB to DREAM. Here we report that DYRK1A can specifically phosphorylate LIN52 on serine residue 28, and that this phosphorylation is required for DREAM assembly. Inhibiting DYRK1A activity or point mutation of LIN52 disrupts DREAM assembly and reduces the ability of cells to enter quiescence or undergo Ras-induced senescence. These data reveal an important role for DYRK1A in the regulation of DREAM activity and entry into quiescence.

show abstract

Section: Discussionmentioning

confidence: 99%

DYRK1A protein kinase promotes quiescence and senescence through DREAM complex assembly

Litovchick¹,

Florens²,

Swanson³

et al. 2011

Genes Dev.

272

364

View full text Add to dashboard Cite

show abstract

“…This led to derivation of useful SAR or QSAR data with respect to specific kinases (e.g. Dyrk1A) [101][102][103].…”

Section: Polyphenol Structure-activity Rela-tionships (Sar) With Respmentioning

confidence: 99%

Natural Polyphenols that Display Anticancer Properties through Inhibition of Kinase Activity

Lamoral-Theys¹,

Pottier

Dufrasne³

et al. 2010

CMC

124

View full text Add to dashboard Cite

Over eleven hundred publications reporting anticancer activities of polyphenols have appeared in the peerreviewed literature. In addition, a search of the PubMed database using "polyphenols -cancer -review" as keywords produced over 320 hits for review articles (July 2009). Polyphenol anticancer activities include, among others, anti-oxidative, pro-apoptotic, DNA damaging, anti-angiogenic, and immunostimulatory effects. Targeting specific protein kinases to combat cancer represents a major focus of oncology research within the so-called targeted therapy approach. An exhaustive search of the PubMed database (July 2009) using "polyphenols -cancer -kinases" as keywords resulted in more than 130 hits, half of them having been published within the past five years. Furthermore, the PubMed database contains 25 reviews on the subject of anti-kinase activity of some specific polyphenols, including mainly curcumin and the green tea polyphenol (-)-epigallocatechin 3-gallate (EGCG). However, no attempt has been made yet to review this area of research in a comprehensive, general manner. The current review therefore aims to highlight those anticancer polyphenols that target specific kinases in various types of cancer. The present review also provides an in-depth analysis of polyphenol structure-activity relationships in relation to their anticancer activities and specific kinase targeting. Lastly, a number of polyphenols are identified as potential antitumor agents that could be used to combat biologically aggressive cancers, including metastasizing cancers, through the targeting of specific kinases.

show abstract

“…Therefore, the same team proposed the synthesis of the new 7′-azaisoindigo (Scheme 47), which was diversely substituted on both aromatic parts of the molecule (Fig. 29) (204,205). products into the desired isoindigo derivatives inclusive of N-methylated isoindigo (147) (Meisoindigo).…”

Section: Glycosylisoindigomentioning

confidence: 99%

A Colorful History: The Evolution of Indigoids

Gaboriaud‐Kolar

Nam

Skaltsounis

2014

Progress in the Chemistry of Organic Natural Products

View full text Add to dashboard Cite

Synthesis, kinase inhibitory potencies and in vitro antiproliferative activity of isoindigo and 7′-azaisoindigo derivatives substituted by Sonogashira cross-coupling

Cited by 21 publications

References 10 publications

DYRK1A protein kinase promotes quiescence and senescence through DREAM complex assembly

DYRK1A protein kinase promotes quiescence and senescence through DREAM complex assembly

Natural Polyphenols that Display Anticancer Properties through Inhibition of Kinase Activity

A Colorful History: The Evolution of Indigoids

Contact Info

Product

Resources

About