Literature DB >> 11378364

Indazolylamino quinazolines and pyridopyrimidines as inhibitors of the EGFr and C-erbB-2.

S Cockerill1, C Stubberfield, J Stables, M Carter, S Guntrip, K Smith, S McKeown, R Shaw, P Topley, L Thomsen, K Affleck, A Jowett, D Hayes, M Willson, P Woollard, D Spalding.   

Abstract

Described herein is the design and synthesis of indazolylaminopyridopyrimidines and quinazolines as inhibitors of the class 1 tyrosine kinase receptor family. Data is presented for N(4)-(1-benzyl-1H-indazol-5-yl)-N(6),N(6)-dimethylpyrido[3,4-d]pyrimidine-4,6-diamine 3B. This compound inhibited EGFr and c-erbB-2 enzymes selectively over other kinases. It inhibited the proliferation of a range of tumour cell lines in vitro and the growth of BT474 xenografts in SCID mice.

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Year:  2001        PMID: 11378364     DOI: 10.1016/s0960-894x(01)00219-0

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


  9 in total

1.  A model of acquired autoresistance to a potent ErbB2 tyrosine kinase inhibitor and a therapeutic strategy to prevent its onset in breast cancer.

Authors:  Wenle Xia; Sarah Bacus; Priti Hegde; Intisar Husain; Jay Strum; Leihua Liu; Georgina Paulazzo; Ljuba Lyass; Patricia Trusk; Jason Hill; Jennifer Harris; Neil L Spector
Journal:  Proc Natl Acad Sci U S A       Date:  2006-05-08       Impact factor: 11.205

2.  Graded activation of the MEK1/MT1-MMP axis determines renal epithelial cell tumor phenotype.

Authors:  Rajeev Mahimkar; Maria Alejandra Alfonso-Jaume; Leslie M Cape; Rajvir Dahiya; David H Lovett
Journal:  Carcinogenesis       Date:  2011-09-28       Impact factor: 4.944

3.  GW583340 and GW2974, human EGFR and HER-2 inhibitors, reverse ABCG2- and ABCB1-mediated drug resistance.

Authors:  Kamlesh Sodani; Amit K Tiwari; Satyakam Singh; Atish Patel; Zhi-Jie Xiao; Jun-Jiang Chen; Yue-Li Sun; Tanaji T Talele; Zhe-Sheng Chen
Journal:  Biochem Pharmacol       Date:  2012-03-07       Impact factor: 5.858

Review 4.  A Review on Fused Pyrimidine Systems as EGFR Inhibitors and Their Structure-Activity Relationship.

Authors:  Tanuja T Yadav; Gulam Moin Shaikh; Maushmi S Kumar; Meena Chintamaneni; Mayur Yc
Journal:  Front Chem       Date:  2022-06-13       Impact factor: 5.545

5.  A genetic screen for anchorage-independent proliferation in mammalian cells identifies a membrane-bound neuregulin.

Authors:  Davide Danovi; Catherine A Cremona; Gisela Machado-da-Silva; Sreya Basu; Luke A Noon; Simona Parrinello; Alison C Lloyd
Journal:  PLoS One       Date:  2010-07-26       Impact factor: 3.240

6.  Analysis of the ERK1,2 transcriptome in mammary epithelial cells.

Authors:  Constance Grill; Ferdous Gheyas; Priya Dayananth; Weihong Jin; Wei Ding; Ping Qiu; Luquan Wang; Ronald J Doll; Jessie M English
Journal:  Biochem J       Date:  2004-08-01       Impact factor: 3.857

7.  Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity.

Authors:  Theonie Anastassiadis; Sean W Deacon; Karthik Devarajan; Haiching Ma; Jeffrey R Peterson
Journal:  Nat Biotechnol       Date:  2011-10-30       Impact factor: 54.908

Review 8.  A review on the development of urease inhibitors as antimicrobial agents against pathogenic bacteria.

Authors:  Yuri F Rego; Marcelo P Queiroz; Tiago O Brito; Priscila G Carvalho; Vagner T de Queiroz; Ângelo de Fátima; Fernando Macedo
Journal:  J Adv Res       Date:  2018-05-04       Impact factor: 10.479

Review 9.  Applying computer simulations in battling with COVID-19, using pre-analyzed molecular and chemical data to face the pandemic.

Authors:  Mohammad Amin Khazeei Tabari; Hooman Khoshhal; Alireza Tafazoli; Mohanna Khandan; Abouzar Bagheri
Journal:  Inform Med Unlocked       Date:  2020-10-17
  9 in total

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