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Volumn 19, Issue 1, 2009, Pages 21-26

Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors

Author keywords

EGFR; Epidermal growth factor receptor; ErbB 2; Inhibitor; Proline; Thieno 3,2 d pyrimidines

Indexed keywords

CARBAMIC ACID; EPIDERMAL GROWTH FACTOR RECEPTOR; EPIDERMAL GROWTH FACTOR RECEPTOR 2; PYRROLIDINYLACETYLENIC THIENO[3,2 D]PYRIMIDINE DERIVATIVE; THIENO[3,2 D]PYRIMIDINE DERIVATIVE; UNCLASSIFIED DRUG;

EID: 57749096199     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.11.023     Document Type: Article
Times cited : (21)

References (23)
  • 13
    • 57749090024 scopus 로고    scopus 로고
    • Waterson, A. G.; Petrov, K. G.; Hornberger, K. R.; Hubbard, R. D.; Sammond, D. M.; Smith, S. C.; Hinkle, K. W.; Stevens, K. L.; Uehling, D. E.; Dickerson, S. H.; Rusnak, D. W.; Spehar, G. M.; Wood, E. R.; Griffin, R. J. Bioorg. Med. Chem. Lett., submitted for publication.
    • Waterson, A. G.; Petrov, K. G.; Hornberger, K. R.; Hubbard, R. D.; Sammond, D. M.; Smith, S. C.; Hinkle, K. W.; Stevens, K. L.; Uehling, D. E.; Dickerson, S. H.; Rusnak, D. W.; Spehar, G. M.; Wood, E. R.; Griffin, R. J. Bioorg. Med. Chem. Lett., submitted for publication.
  • 16
    • 57749108786 scopus 로고    scopus 로고
    • note
    • Compound 4 (CAS#: 225385-03-5) has recently become commercially available through Medinoah Inc., Wallingford, CT. Synthetic details can be found in PCT Int. Appl. WO 99/24440. Compound 5 is prepared by displacement on the chloro of 4 with 3-chloro-4-(3-fluorobenzyloxy)aniline which is available through Affinitis Pharma LLC, New Haven, CT. Synthetic details can be found in PCT Int. Appl. WO 98/02437.
  • 17
    • 57749092410 scopus 로고    scopus 로고
    • note
    • The modification data was only acquired for EGFR using methods described in Ref. 12. These analogs have not been assayed versus ErbB-2 for potential reactivity.
  • 18
    • 57749098182 scopus 로고    scopus 로고
    • note
    • Thienopyrimidine analogs (6a-j) were found to be selective for the transformed cell lines (HN5 and BT474) versus a control human foreskin fibroblast cell line (HFF). Experimental protocols are described in Ref. 7.
  • 21
    • 57749100752 scopus 로고    scopus 로고
    • note
    • (4R)-4-Hydroxy-(2R)-proline 5g, $153; (4S)-4-Hydroxy-(2R)-proline 5g, $291, both from AstaTech, Bristol, PA. Advanced derivatives of the 2-(S) enantiomer, such as 10, are occasionally available, 5g, $169 from AstraTech.
  • 23
    • 0030201076 scopus 로고    scopus 로고
    • Dissociation-enhanced lanthanide fluorescence immunoassay (DELFIA), see: BT474 cells and their culture conditions are described in Ref. 7
    • Dissociation-enhanced lanthanide fluorescence immunoassay (DELFIA), see:. Braunwalder A.F., Yarwood D.R., Sills M.A., and Lipson K.E. Anal. Biochem. 238 (1996) 159 BT474 cells and their culture conditions are described in Ref. 7
    • (1996) Anal. Biochem. , vol.238 , pp. 159
    • Braunwalder, A.F.1    Yarwood, D.R.2    Sills, M.A.3    Lipson, K.E.4


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.