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Volumn 8, Issue 3, 2013, Pages 521-526

A "Clickable" MTX Reagent as a Practical Tool for Profiling Small-Molecule-Intracellular Target Interactions via MASPIT

Author keywords

Click chemistry; MASPIT; Methotrexate conjugates; Profiling; Target identification; Three hybrid

Indexed keywords

ACETYLENE; AZIDE; CELL PROTEIN; METHOTREXATE; REVERSINE; TACROLIMUS; TAMOXIFEN; UNCLASSIFIED DRUG;

EID: 84874315356     PISSN: 18607179     EISSN: 18607187     Source Type: Journal    
DOI: 10.1002/cmdc.201200493     Document Type: Article
Times cited : (12)

References (25)
  • 1
    • 0034677966 scopus 로고    scopus 로고
    • J. Drews, Science 2000, 287, 1960-1964.
    • (2000) Science , vol.287 , pp. 1960-1964
    • Drews, J.1
  • 10
  • 21
    • 84874294110 scopus 로고    scopus 로고
    • The trimethylsilyl protecting group on the acetylene group is retained, as 4-ethynylphenol (contrary to its methoxy congener 4-ethynylanisole) is highly unstable. Alkylation of the phenol moiety to an ether group eliminates the instability, thus enabling removal of the TMS group.
    • The trimethylsilyl protecting group on the acetylene group is retained, as 4-ethynylphenol (contrary to its methoxy congener 4-ethynylanisole) is highly unstable. Alkylation of the phenol moiety to an ether group eliminates the instability, thus enabling removal of the TMS group.
  • 23
    • 84874337746 scopus 로고    scopus 로고
    • Both fluoride sources were necessary, as no single set of conditions in our hands proved successful to remove both the alkynylsilane and the silylether groups.
    • Both fluoride sources were necessary, as no single set of conditions in our hands proved successful to remove both the alkynylsilane and the silylether groups.
  • 24
    • 84874329339 scopus 로고    scopus 로고
    • The non-regiopure conjugate was generated analogously to its regioselective γcongener by only using a non-regioselective methotrexate PEG azide, prepared as described in the Supporting Information.
    • The non-regiopure conjugate was generated analogously to its regioselective γcongener by only using a non-regioselective methotrexate PEG azide, prepared as described in the Supporting Information.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.