Zobrazeno 1 - 10
of 81
pro vyhledávání: '"James R. Piper"'
Autor:
A. Heroux, David W. Borhani, Larry J. Ross, James R. Piper, Vibha Pathak, Anthony E. Klon, Cheryl A. Johnson
Publikováno v:
Journal of Molecular Biology. 320:677-693
The crystal structures of two human dihydrofolate reductase (hDHFR) ternary complexes, each with bound NADPH cofactor and a lipophilic antifolate inhibitor, have been determined at atomic resolution. The potent inhibitors 6-([5-quinolylamino]methyl)-
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::426691a981daf2394ebdf6e5b7252cbc
https://doi.org/10.1016/s0022-2836(02)00469-2
https://doi.org/10.1016/s0022-2836(02)00469-2
Publikováno v:
European Journal of Medicinal Chemistry. 36:237-242
N-[4-[[2,4-diamino-6-pteridinyl)methyl]amino]bicyclo[2.2.2]octane-1-carbonyl]-L-glutamic acid (1) was synthesized and tested for antifolate activity. N-(4-Aminobicyclo[2.2.2]octane-1-carbonyl-L-glutamic acid dimethyl ester (6), the side chain precurs
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::36ebe8a91cf790e5d2af894bbb55105d
https://doi.org/10.1016/s0223-5234(01)01224-7
https://doi.org/10.1016/s0223-5234(01)01224-7
Autor:
Francis M. Sirotnak, Balakrishnan Ramamurthy, Joseph A. Maddry, G. M. Otter, James R. Piper, Cheryl A. Johnson
Publikováno v:
Journal of Heterocyclic Chemistry. 32:1205-1212
5-Propyl-5-deaza and 5-butyl-5-deaza analogues of classical antifolates were synthesized by extensions of a previously reported general route which proceeds through 2,4-diamino-5-alkylpyrido[2,3-d]pyrimidine-6-carbonitrile intermediates followed by r
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::6a80d5a039998f1cb17e78b277042f88
https://doi.org/10.1002/jhet.5570320419
https://doi.org/10.1002/jhet.5570320419
Autor:
James R. Piper, Cheryl A. Johnson, Francis M. Sirotnak, Neeta D. Malik, Glenys M. Otter, Joseph A. Maddry, John J. McGuire
Publikováno v:
Journal of Medicinal Chemistry. 36:4161-4171
Analogues of classical antifolates with the 4-aminobenzoyl group replaced by 4-amino-1-naphthoyl were synthesized for study after molecular modeling indicated ample spatial accommodation for the naphthalene ring and even larger groups in models based
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::12f4111941a3f3ea7899b05e5c03d189
https://doi.org/10.1021/jm00078a004
https://doi.org/10.1021/jm00078a004
Publikováno v:
ChemInform. 23
Previous findings suggesting that 5,10-dialkyl-substituted derivatives of 5,10-dideazaaminopterin warranted study as potential antifolates prompted synthesis of 10-ethyl-5-methyl-5,10- dideazaaminopterin (12a). The key step in the synthetic route to
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::7e0946948743b8d9cb11c0c9fb179341
https://doi.org/10.1002/chin.199252219
https://doi.org/10.1002/chin.199252219
Autor:
G. M. Otter, Joseph A. Maddry, Balakrishnan Ramamurthy, Cheryl A. Johnson, James R. Piper, Francis M. Sirotnak
Publikováno v:
ChemInform. 26
5-Propyl-5-deaza and 5-butyl-5-deaza analogues of classical antifolates were synthesized by extensions of a previously reported general route which proceeds through 2,4-diamino-5-alkylpyrido[2,3-d]pyrimidine-6-carbonitrile intermediates followed by r
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::906575be37a29a4511d1d0bc11891ebb
https://doi.org/10.1002/chin.199551278
https://doi.org/10.1002/chin.199551278
Publikováno v:
ChemInform. 27
10-Deaza modifications of classical antifolate analogues bearing the 1,4-disubstituted naphthalene ring in place of the 1,4-disubstituted benzene ring were prepared and tested for antitumor activity. Naphthalene analogues (9a−c, respectively) of 10
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::6c5b8bbddaa4b7ff3475c0ad5c8b02d6
https://doi.org/10.1002/chin.199619233
https://doi.org/10.1002/chin.199619233
Publikováno v:
ChemInform. 32
N-[4-[[2,4-diamino-6-pteridinyl)methyl]amino]bicyclo[2.2.2]octane-1-carbonyl]-L-glutamic acid (1) was synthesized and tested for antifolate activity. N-(4-Aminobicyclo[2.2.2]octane-1-carbonyl-L-glutamic acid dimethyl ester (6), the side chain precurs
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::8dd70a5743c5c622ba9348b1bd00a3e9
https://doi.org/10.1002/chin.200140192
https://doi.org/10.1002/chin.200140192
Publikováno v:
Journal of Medicinal Chemistry. 35:332-337
5-Deaza-10-propargylfolic acid (4), an analogue of the thymidylate synthase (TS) inhibitor 10-propargyl-5,8-dideazafolic acid (PDDF, 1), was prepared via alkylation of diethyl N-[4-(propargylamino)benzoyl]-L-glutamate (7) by 2-amino-6-(bromomethyl)-4
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b0f35b41a5df5fb260866a15d991ae65
https://doi.org/10.1021/jm00080a019
https://doi.org/10.1021/jm00080a019
Autor:
Geeta Maharaj, John A. Montgomery, James H. Freisheim, Raymond L. Blakley, Robert F. Kulinski, James R. Appleman, Tavner J. Delcamp, James R. Piper
Publikováno v:
European Journal of Biochemistry. 196:271-280
Four spin-labeled inhibitors of dihydrofolate reductase (DHFR) have been synthesized, each of which has the 2,2,6,6-tetramethyl-1-piperidinyloxy (TEMPO) reporting group at a different distance from the 2,4-diaminopyrimidine moiety by which the inhibi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7e3c3e181f611de9fb527fb5bf3a6d58
https://doi.org/10.1111/j.1432-1033.1991.tb15814.x
https://doi.org/10.1111/j.1432-1033.1991.tb15814.x