메뉴 건너뛰기




Volumn 41, Issue 5, 2004, Pages 787-793

Synthesis and antifolate activity of new pyrrolo[2,3-d]pyrimidine and thieno[2,3-d]pyrimidine inhibitors of dihydrofolate reductase

Author keywords

[No Author keywords available]

Indexed keywords

DIHYDROFOLATE REDUCTASE INHIBITOR; FOLIC ACID ANTAGONIST; N [4 [N [(2,4 DIAMINOTHIENO[2,3 D]PYRIMIDIN 5 YL)METHYL]AMINO]BENZOYL]GLUTAMIC ACID; NALPHA (4 AMINO 4 DEOXYPTEROYL) NDELTA HEMIPHTHALOYLORNITHINE; NALPHA [4 [N [(2,4 DIAMINOPYRROLO[2,3 D]PYRIMIDIN 5 YL)METHYL]AMINO]BENZOYL] NDELTA HEMIPHTHALOYLORNITHINE; NALPHA [4 [N [(2,4 DIAMINOTHIENO[2,3 D]PYRIMIDIN 5 YL)METHYL]AMINO]BENZOYL]GLUTAMIC ACID; PYRROLO[2,3 D]PYRIMIDINE DERIVATIVE; THIENO[2,3 D]PYRIMIDINE DERIVATIVE; UNCLASSIFIED DRUG;

EID: 6344269171     PISSN: 0022152X     EISSN: None     Source Type: Journal    
DOI: 10.1002/jhet.5570410523     Document Type: Article
Times cited : (5)

References (25)
  • 18
    • 6344241102 scopus 로고    scopus 로고
    • note
    • The spatial orientation of the side chain in the furan analogue 9 in its ternary complex with NADPH and human DHFR has been found by X-ray crystallographic analysis to be different from that of the side chain in MTX [17], and this may also be true in the case of the thiophene analogue 12.
  • 20
    • 6344277335 scopus 로고    scopus 로고
    • note
    • m for these compounds was outside the scope of this work.
  • 21
    • 6344287874 scopus 로고    scopus 로고
    • note
    • Because the binding of diaminoheterocyclic antifolates to the active site of DHFR is thermodynamically reversible except in those instances where a covalent bond is formed, it is generally considered that an excess of free drug is important as a way to minimize dissociation of the antifolate from the enzyme, thereby maximally prolonging DNA synthesis inhibition.
  • 25
    • 6344277336 scopus 로고    scopus 로고
    • note
    • 3 as the base, this statement was an error [14b] and we subsequently returned to the original procedure using NaOMe [22].


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.