Literature DB >> 15953730

RO4383596, an orally active KDR, FGFR, and PDGFR inhibitor: synthesis and biological evaluation.

Lee A McDermott1, Mary Simcox, Brian Higgins, Tom Nevins, Kenneth Kolinsky, Melissa Smith, Hong Yang, Jia K Li, Yingsi Chen, June Ke, Navita Mallalieu, Tom Egan, Stan Kolis, Aruna Railkar, Louise Gerber, Kin-Chun Luk.   

Abstract

(+/-)-1-(anti-3-Hydroxy-cyclopentyl)-3-(4-methoxy-phenyl)-7-phenylamino-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one (RO4383596) is a potent and selective inhibitor of the pro-angiogenic receptor tyrosine kinases KDR, FGFR, and PDGFR. This agent has an excellent pharmacokinetic profile and is highly efficacious in rodent models of angiogenesis upon oral administration.

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Year:  2005        PMID： 15953730     DOI： 10.1016/j.bmc.2005.05.012

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  8 in total

Review 1.  Adding to the mix: fibroblast growth factor and platelet-derived growth factor receptor pathways as targets in non-small cell lung cancer.

Authors:  S A Kono; L E Heasley; R C Doebele; D R Camidge
Journal:  Curr Cancer Drug Targets       Date:  2012-02       Impact factor: 3.428

2.  Fibroblast growth factor receptors are components of autocrine signaling networks in head and neck squamous cell carcinoma cells.

Authors:  Marianne E Marshall; Trista K Hinz; Scott A Kono; Katherine R Singleton; Brady Bichon; Kathryn E Ware; Lindsay Marek; Barbara A Frederick; David Raben; Lynn E Heasley
Journal:  Clin Cancer Res       Date:  2011-06-14       Impact factor: 12.531

3.  Rapidly acquired resistance to EGFR tyrosine kinase inhibitors in NSCLC cell lines through de-repression of FGFR2 and FGFR3 expression.

Authors:  Kathryn E Ware; Marianne E Marshall; Lydia R Heasley; Lindsay Marek; Trista K Hinz; Paula Hercule; Barbara A Helfrich; Robert C Doebele; Lynn E Heasley
Journal:  PLoS One       Date:  2010-11-29       Impact factor: 3.240

4.  Fibroblast growth factor (FGF) and FGF receptor-mediated autocrine signaling in non-small-cell lung cancer cells.

Authors:  Lindsay Marek; Kathryn E Ware; Alexa Fritzsche; Paula Hercule; Wallace R Helton; Jennifer E Smith; Lee A McDermott; Christopher D Coldren; Raphael A Nemenoff; Daniel T Merrick; Barbara A Helfrich; Paul A Bunn; Lynn E Heasley
Journal:  Mol Pharmacol       Date:  2008-10-10       Impact factor: 4.436

Review 5.  The fibroblast growth factor receptor signaling pathway as a mediator of intrinsic resistance to EGFR-specific tyrosine kinase inhibitors in non-small cell lung cancer.

Authors:  Scott A Kono; Marianne E Marshall; Kathryn E Ware; Lynn E Heasley
Journal:  Drug Resist Updat       Date:  2009-06-04       Impact factor: 18.500

Review 6.  Targeting RTK Signaling Pathways in Cancer.

Authors:  Tarik Regad
Journal:  Cancers (Basel)       Date:  2015-09-03       Impact factor: 6.639

Review 7.  Bicyclic 6 + 6 systems: the chemistry of pyrimido[4,5-d]pyrimidines and pyrimido[5,4-d]pyrimidines.

Authors:  M Monier; Doaa Abdel-Latif; Ahmed El-Mekabaty; Khaled M Elattar
Journal:  RSC Adv       Date:  2019-09-30       Impact factor: 4.036

8.  A mechanism of resistance to gefitinib mediated by cellular reprogramming and the acquisition of an FGF2-FGFR1 autocrine growth loop.

Authors:  K E Ware; T K Hinz; E Kleczko; K R Singleton; L A Marek; B A Helfrich; C T Cummings; D K Graham; D Astling; A-C Tan; L E Heasley
Journal:  Oncogenesis       Date:  2013-03-25       Impact factor: 7.485
  8 in total

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