The effect of side-chain, para-aminobenzoyl region, and B-ring modifications on dihydrofolate reductase binding, influx via the reduced folate carrier, and cytotoxicity of the potent nonpolyglutamatable antifolate N(α)-(4-amino-4-deoxypteroyl)-N(δ)-hemiphthaloyl-L-ornithine

Pharmacology and Therapeutics

Volumn 85, Issue 3, 2000, Pages 191-205

  Rosowsky, Andre ^a   Wright, Joel E ^a   Vaidya, Chitra M ^a   Forsch, Ronald A ^a  

^a HARVARD MEDICAL SCHOOL   (United States)

Author keywords

Aminopterin analogs; Dihydrofolate reductase; Reduced folate carrier

Indexed keywords

AMINOPTERIN DERIVATIVE; DIHYDROFOLATE REDUCTASE; FOLIC ACID ANTAGONIST; LOMETREXOL; N [[5 [2 (2 AMINO 4,6,7,8 TETRAHYDRO 4 OXO 1H PYRIMIDO[5,4 B][1,4]THIAZIN 6 YL)ETHYL] 2 THIENYL]CARBONYL]GLUTAMIC ACID; NALPHA (4 AMINO 4 DEOXYPTEROYL) NDELTA HEMIPHTHALOYLORNITHINE; ORNITHINE DERIVATIVE; PEMETREXED; RALTITREXED;

ANTINEOPLASTIC ACTIVITY; CONFERENCE PAPER; CONTROLLED STUDY; CYTOTOXICITY; HUMAN; HUMAN CELL; IC 50; PRIORITY JOURNAL; STRUCTURE ACTIVITY RELATION; TUMOR CELL;

4-AMINOBENZOIC ACID; AMINOPTERIN; ANTINEOPLASTIC AGENTS; BINDING SITES; CELL DIVISION; DRUG RESISTANCE, MULTIPLE; DRUG SCREENING ASSAYS, ANTITUMOR; FOLIC ACID; FOLIC ACID ANTAGONISTS; HUMANS; ORNITHINE; PTERINS; REDUCING AGENTS; STRUCTURE-ACTIVITY RELATIONSHIP; TETRAHYDROFOLATE DEHYDROGENASE; TUMOR CELLS, CULTURED;

EID: 0034059805     PISSN: 01637258     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0163-7258(99)00055-8     Document Type: Conference Paper

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