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Volumn 1, Issue 3, 2006, Pages 314-321

Identification of potent, selective protein kinase C inhibitors based on a phorbol skeleton

Author keywords

Enzymes; Fluoroalkyls; Inhibitors; Phorbol esters; Protein kinase C

Indexed keywords

ADENOSINE TRIPHOSPHATE; ENZYME INHIBITOR; PHORBOL ESTER; PROTEIN KINASE C;

EID: 33749180779     PISSN: 18614728     EISSN: 1861471X     Source Type: Journal    
DOI: 10.1002/asia.200600185     Document Type: Article
Times cited : (10)

References (52)
  • 6
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    • For a review of protein kinase inhibitors, see: A. J. Bridges, Chem. Rev. 2001, 101, 2541.
    • (2001) Chem. Rev. , vol.101 , pp. 2541
    • Bridges, A.J.1
  • 29
    • 33749175343 scopus 로고    scopus 로고
    • note
    • The calculated logP values of 3 and 4 are 2.49 and 2.18, respectively, which support our assumption.
  • 30
    • 0034926661 scopus 로고    scopus 로고
    • There may also be affinitive interactions between the perfluoroalkyl group and PKC. For a review of the effects of fluorine substituents on biological activity, see: a) B. E. Smart, J. Fluorine Chem. 2001, 109, 3. For recent reports of interesting effects of fluoroalkyl substituents on biological activity and molecular structure, see:
    • (2001) J. Fluorine Chem. , vol.109 , pp. 3
    • Smart, B.E.1
  • 35
    • 33749162009 scopus 로고    scopus 로고
    • note
    • 50 value of 6 than expected from its modest binding affinity is attributable to the partial agonistic character of 6. Even in the presence of a high concentration of 6, the PKC activity did not reach zero; see Supporting Information.
  • 38
    • 33749170917 scopus 로고    scopus 로고
    • note
    • For detailed synthetic procedures and spectroscopic data of 8, see Supporting Information.
  • 43
    • 37049072209 scopus 로고
    • T. Okada, Analyst 1993, 118, 959.
    • (1993) Analyst , vol.118 , pp. 959
    • Okada, T.1
  • 45
    • 33749184785 scopus 로고    scopus 로고
    • note
    • The same mechanism might be involved in the previous inhibitor 3.
  • 46
    • 33749175836 scopus 로고    scopus 로고
    • note
    • Preliminary studies indicated that 8 has no significant cancer cell (K562) growth inhibitory activity.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.