Literature DB >> 16539403

Dihydropyrrolopyrazole transforming growth factor-beta type I receptor kinase domain inhibitors: a novel benzimidazole series with selectivity versus transforming growth factor-beta type II receptor kinase and mixed lineage kinase-7.

Hong-yu Li1, Yan Wang, Charles R Heap, Chi-Hsin R King, Sreenivasa R Mundla, Matthew Voss, David K Clawson, Lei Yan, Robert M Campbell, Bryan D Anderson, Jill R Wagner, Karen Britt, Ku X Lu, William T McMillen, Jonathan M Yingling.   

Abstract

Novel dihydropyrrolopyrazole-substituted benzimidazoles were synthesized and evaluated in vitro as inhibitors of transforming growth factor-beta type I receptor (TGF-beta RI), TGF-beta RII, and mixed lineage kinase-7 (MLK-7). These compounds were found to be potent TGF-beta RI inhibitors and selective versus TGF-beta RII and MLK-7 kinases. Benzimidazole derivative 8b was active in an in vivo target (TGF-beta RI) inhibition assay.

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Year:  2006        PMID： 16539403     DOI： 10.1021/jm058209g

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  17 in total

1.  Reduced SMAD7 leads to overactivation of TGF-beta signaling in MDS that can be reversed by a specific inhibitor of TGF-beta receptor I kinase.

Authors:  Li Zhou; Christine McMahon; Tushar Bhagat; Cristina Alencar; Yiting Yu; Melissa Fazzari; Davendra Sohal; Christoph Heuck; Krishna Gundabolu; Chun Ng; Yongkai Mo; Wa Shen; Amittha Wickrema; Guanghui Kong; Ellen Friedman; Lubomir Sokol; Ioannis Mantzaris; Giannis Mantzaris; Andrea Pellagatti; Jacqueline Boultwood; Leonidas C Platanias; Ulrich Steidl; Lei Yan; Jonathan M Yingling; Michael M Lahn; Alan List; Markus Bitzer; Amit Verma
Journal:  Cancer Res       Date:  2010-12-28       Impact factor: 12.701

2.  Molecular docking analysis of curcumin analogues against kinase domain of ALK5.

Authors:  Shivananda Kandagalla; B S Sharath; Basavapattana Rudresh Bharath; Umme Hani; Hanumanthappa Manjunatha
Journal:  In Silico Pharmacol       Date:  2017-11-18

3.  Discovery of 4-Azaindole Inhibitors of TGFβRI as Immuno-oncology Agents.

Authors:  Yong Zhang; Yufen Zhao; Andrew J Tebben; Steven Sheriff; Max Ruzanov; Mark P Fereshteh; Yi Fan; Jonathan Lippy; Jesse Swanson; Ching-Ping Ho; Barri S Wautlet; Anne Rose; Karen Parrish; Zheng Yang; Andrew F Donnell; Liping Zhang; Brian E Fink; Gregory D Vite; Karen Augustine-Rauch; Joseph Fargnoli; Robert M Borzilleri
Journal:  ACS Med Chem Lett       Date:  2018-10-17       Impact factor: 4.345

4.  GLUT10 is required for the development of the cardiovascular system and the notochord and connects mitochondrial function to TGFβ signaling.

Authors:  Andy Willaert; Sandeep Khatri; Bert L Callewaert; Paul J Coucke; Seth D Crosby; Joseph G H Lee; Elaine C Davis; Sruti Shiva; Michael Tsang; Anne De Paepe; Zsolt Urban
Journal:  Hum Mol Genet       Date:  2011-11-24       Impact factor: 6.150

5.  Eukaryotic Translation Initiation Factor 4E Is a Feed-Forward Translational Coactivator of Transforming Growth Factor β Early Protransforming Events in Breast Epithelial Cells.

Authors:  Lindsey Decarlo; Celine Mestel; Mary-Helen Barcellos-Hoff; Robert J Schneider
Journal:  Mol Cell Biol       Date:  2015-05-18       Impact factor: 4.272

6.  Inhibition of TGF-β signaling promotes expansion of human epidermal keratinocytes in feeder cell co-culture.

Authors:  Daisuke Suzuki; Filipa Pinto; Makoto Senoo
Journal:  Wound Repair Regen       Date:  2017-05-16       Impact factor: 3.617

7.  Targeting the Transforming Growth Factor-beta pathway inhibits human basal-like breast cancer metastasis.

Authors:  Vidya Ganapathy; Rongrong Ge; Alison Grazioli; Wen Xie; Whitney Banach-Petrosky; Yibin Kang; Scott Lonning; John McPherson; Jonathan M Yingling; Swati Biswas; Gregory R Mundy; Michael Reiss
Journal:  Mol Cancer       Date:  2010-05-26       Impact factor: 27.401

8.  Increase in tumour permeability following TGF-beta type I receptor-inhibitor treatment observed by dynamic contrast-enhanced MRI.

Authors:  T Minowa; K Kawano; H Kuribayashi; K Shiraishi; T Sugino; Y Hattori; M Yokoyama; Y Maitani
Journal:  Br J Cancer       Date:  2009-11-03       Impact factor: 7.640

Review 9.  Transforming growth factor-beta signaling: emerging stem cell target in metastatic breast cancer?

Authors:  Antoinette R Tan; Gabriela Alexe; Michael Reiss
Journal:  Breast Cancer Res Treat       Date:  2008-10-09       Impact factor: 4.872

10.  Structure-activity relationships of antitubercular nitroimidazoles. 2. Determinants of aerobic activity and quantitative structure-activity relationships.

Authors:  Pilho Kim; Sunhee Kang; Helena I Boshoff; Jan Jiricek; Margaret Collins; Ramandeep Singh; Ujjini H Manjunatha; Pornwaratt Niyomrattanakit; Liang Zhang; Michael Goodwin; Thomas Dick; Thomas H Keller; Cynthia S Dowd; Clifton E Barry
Journal:  J Med Chem       Date:  2009-03-12       Impact factor: 7.446
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