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Rosowsky, Andre; Forsch, Ronald A; Wright, Joel E (2004) Synthesis and in vitro antifolate activity of rotationally restricted aminopterin and methotrexate analogues. J Med Chem 47:6958-63
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Wright, Joel E; Yurasek, Gregory K; Chen, Ying-Nan et al. (2003) Further studies on the interaction of nonpolyglutamatable aminopterin analogs with dihydrofolate reductase and the reduced folate carrier as determinants of in vitro antitumor activity. Biochem Pharmacol 65:1427-33
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Vaidya, Chitra M; Wright, Joel E; Rosowsky, Andre (2002) Synthesis and in vitro antitumor activity of new deaza analogues of the nonpolyglutamatable antifolate N(alpha)-(4-amino-4-deoxypteroyl)-N(delta)-hemiphthaloyl-L-ornithine (PT523). J Med Chem 45:1690-6
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Wright, Joel E; Rosowsky, Andre (2002) Synthesis and enzymatic activation of N-[N(alpha)-(4-amino-4-deoxypteroyl)-N(delta)-hemiphthaloyl-L-ornithiny]-L-phenylalanine, a candidate for antibody-directed enzyme prodrug therapy (ADEPT). Bioorg Med Chem 10:493-500
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Rosowsky, A; Wright, J E; Vaidya, C M et al. (2000) 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(alpha)-(4-amino-4-deoxypteroyl)-N(delta Pharmacol Ther 85:191-205
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Rosowsky, A; Wright, J E; Vaidya, C M et al. (2000) Analogues of the potent nonpolyglutamatable antifolate N(alpha)-(4-amino-4-deoxypteroyl)-N(delta)-hemiphthaloyl-L-ornithine (PT523) with modifications in the side chain, p-aminobenzoyl moiety, or 9,10-bridge: synthesis and in vitro antitumor activity. J Med Chem 43:1620-34
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Rosowsky, A (1999) PT523 and other aminopterin analogs with a hemiphthaloyl-L-ornithine side chain: exceptionally tight-binding inhibitors of dihydrofolate reductase which are transported by the reduced folate carrier but cannot form polyglutamates. Curr Med Chem 6:329-52
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Wright, J E; Pardo, M; Tretyakov, A et al. (1998) Pharmacokinetics, antifolate activity and tissue distribution of PT523 in SCC VII tumor-bearing mice. Cancer Chemother Pharmacol 42:300-6
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Rosowsky, A; Wright, J E; Vaidya, C M et al. (1998) Synthesis and potent antifolate activity and cytotoxicity of B-ring deaza analogues of the nonpolyglutamatable dihydrofolate reductase inhibitor Nalpha-(4-amino-4-deoxypteroyl)-Ndelta-hemiphthaloyl- L-ornithine (PT523). J Med Chem 41:5310-9
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Johnson, J M; Meiering, E M; Wright, J E et al. (1997) NMR solution structure of the antitumor compound PT523 and NADPH in the ternary complex with human dihydrofolate reductase. Biochemistry 36:4399-411
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