Literature DB >> 16806916

Inhibitors of epidermal growth factor receptor tyrosine kinase: optimisation of potency and in vivo pharmacokinetics.

Peter Ballard1, Robert H Bradbury, Craig S Harris, Laurent F A Hennequin, Mark Hickinson, Jason G Kettle, Jane Kendrew, Teresa Klinowska, Donald J Ogilvie, Stuart E Pearson, Emma J Williams, Ingrid Wilson.   

Abstract

The structure-activity and structure-property relationships of anilinoquinazoline inhibitors of EGFR were investigated. Strategies to lower volume of distribution and shorten half-life through structure and pKa modulation are discussed.

Entities:  

Mesh：

Substances：

Year:  2006        PMID： 16806916     DOI： 10.1016/j.bmcl.2006.06.054

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  6 in total

1.  Discovery of AZD8931, an Equipotent, Reversible Inhibitor of Signaling by EGFR, HER2, and HER3 Receptors.

Authors:  Bernard Barlaam; Judith Anderton; Peter Ballard; Robert H Bradbury; Laurent F A Hennequin; D Mark Hickinson; Jason G Kettle; George Kirk; Teresa Klinowska; Christine Lambert-van der Brempt; Cath Trigwell; John Vincent; Donald Ogilvie
Journal:  ACS Med Chem Lett       Date:  2013-05-31       Impact factor: 4.345

2.  Design and synthesis of novel Gefitinib analogues with improved anti-tumor activity.

Authors:  Xiaoqing Wu; Mingdong Li; Yang Qu; Wenhua Tang; Youguang Zheng; Jiqin Lian; Min Ji; Liang Xu
Journal:  Bioorg Med Chem       Date:  2010-04-21       Impact factor: 3.641

3.  Design, synthesis, and in vitro antitumor activity evaluation of novel 4-pyrrylamino quinazoline derivatives.

Authors:  Xiaoqing Wu; Mingdong Li; Wenhua Tang; Youguang Zheng; Jiqin Lian; Liang Xu; Min Ji
Journal:  Chem Biol Drug Des       Date:  2011-10-24       Impact factor: 2.817

4.  Development of a Potent Brain-Penetrant EGFR Tyrosine Kinase Inhibitor against Malignant Brain Tumors.

Authors:  Jonathan E Tsang; Lorenz M Urner; Gyudong Kim; Kingsley Chow; Lynn Baufeld; Kym Faull; Timothy F Cloughesy; Peter M Clark; Michael E Jung; David A Nathanson
Journal:  ACS Med Chem Lett       Date:  2020-05-01       Impact factor: 4.345

5.  Evaluation of 6-chloro-N-[3,4-disubstituted-1,3-thiazol-2(3H)-ylidene]-1,3-benzothiazol-2-amine Using Drug Design Concept for Their Targeted Activity Against Colon Cancer Cell Lines HCT-116, HCT15, and HT29.

Authors:  Ming-Li Zhu; Cui-Yue Wang; Cheng-Mian Xu; Wei-Ping Bi; Xiu-Ying ZHou
Journal:  Med Sci Monit       Date:  2017-03-05

6.  EGFR tyrosine kinase targeted compounds: in vitro antitumor activity and molecular modeling studies of new benzothiazole and pyrimido[2,1-b]benzothiazole derivatives.

Authors:  Moustafa T Gabr; Nadia S El-Gohary; Eman R El-Bendary; Mohamed M El-Kerdawy
Journal:  EXCLI J       Date:  2014-05-26       Impact factor: 4.068
  6 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.