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Volumn 21, Issue 4, 2011, Pages 1202-1205

Design and regioselective synthesis of a new generation of targeted therapeutics. Part 3: Folate conjugates of aminopterin hydrazide for the treatment of inflammation

Author keywords

Disulfide linkers; Folate; Folate receptor targeting; Folate aminopterin hydrazide conjugate; Inflammation

Indexed keywords

2 [4 BENZOYLAMINO] 5 OXO 5 [N' [2 (PYRIDIN 2 YLDISULFANYL)ETHOXYCARBONYL]HYDRAZINO] PENTANOIC ACID; AMINOPTERIN; AMINOPTERIN DERIVATIVE; AMINOPTERIN HYDRAZIDE; ANTIINFLAMMATORY AGENT; CYSTEINE; FOLATE RECEPTOR; FOLIC ACID; UNCLASSIFIED DRUG;

EID: 79851511691     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.12.085     Document Type: Article
Times cited : (17)

References (46)
  • 36
  • 39
    • 79851515461 scopus 로고    scopus 로고
    • note
    • += Calculated 668.2; found 668.2.
  • 40
    • 79851509915 scopus 로고    scopus 로고
    • note
    • 3 solution (bubbled with argon for 10 min before use) until the pH of the resulting solution reached 6.9. 1 equiv of 4 in THF was added quickly and the resulting homogenous solution was stirred under argon for 15 min. The reaction progress was checked by analytical HPLC. The mixture was diluted with of phosphate buffer and the THF was removed under vacuum. The cloudy solution was centrifuged and filtered. The yellow filtrate was purified by preparative HPLC.
  • 41
    • 79851515654 scopus 로고    scopus 로고
    • note
    • 2+]/2 = Calculated 767.2; found 767.4.
  • 42
    • 79851512640 scopus 로고    scopus 로고
    • note
    • 2+]/2 = Calculated 1119.09; found 1119.10.
  • 43
    • 79851512842 scopus 로고    scopus 로고
    • note
    • The species which reduces the disulfide bond to free thiol in the endosome is not known, but the reduction is unlikely to result from disulfide exchange with small thiol-containing molecules due to the relatively low pH. The use of DTT or another reductant such as glutathione does not accurately mimic the biological system. See Ref. 13.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.