Zobrazeno 1 - 10
of 15
pro vyhledávání: '"Hiteshkumar D. Jain"'
Publikováno v:
Bioorganic & Medicinal Chemistry. 18:953-961
A novel classical antifolate N-{4-[(2,4-diamino-5-methyl-furo[2,3-d]pyrimidin-6-yl)thio]-benzoyl}-l-glutamic acid 5 and 11 nonclassical antifolates 6-16 were designed, synthesized, and evaluated as inhibitors of dihydrofolate reductase (DHFR) and thy
Publikováno v:
Journal of Medicinal Chemistry. 51:4589-4600
Novel classical antifolates (3 and 4) and 17 nonclassical antifolates (11-27) were synthesized as antitumor and/or antiopportunistic infection agents. Intermediates for the synthesis of 3, 4, and 11-27 were 2,4-diamino-5-alkylsubstituted-7H-pyrrolo[2
Publikováno v:
Anti-Cancer Agents in Medicinal Chemistry. 8:205-231
Antifolates that inhibit the key enzymes thymidylate synthase (TS) and dihydrofolate reductase (DHFR) have found clinical utility as antitumor and antiopportunistic agents. Methotrexate {MTX, (1)} and 5-fluorouracil (5-FU) were among the first clinic
Autor:
John J. McGuire, Xin Lin, Aleem Gangjee, Hiteshkumar D. Jain, Jaclyn Phan, Xiaohong Song, Roy L. Kisliuk
Publikováno v:
Journal of Medicinal Chemistry. 49:1055-1065
We designed and synthesized a classical analogue N-[4-[(2-amino-6-ethyl-3,4-dihydro-4-oxo-7H-pyrrolo[2,3-d]pyrimidin-5-yl)thio]benzoyl]-L-glutamic acid (4) and thirteen nonclassical analogues 5-17 as potential dual thymidylate synthase (TS) and dihyd
Publikováno v:
Journal of Heterocyclic Chemistry. 42:589-594
Nine novel nonclassical 2,4-diamino-6-methyl-5-mioarylsubstituted-7H-pyrrolo[2,3-d]pyrimidines 2-10 were synthesized as potential inhibitors of dihydrofolate reductase and as antitumor agents. The analogues contain various electron donating and elect
Publikováno v:
Journal of Medicinal Chemistry. 47:6730-6739
In an attempt to circumvent resistance to and toxicity of clinically used folate-based thymidylate synthase (TS) inhibitors that require folylpoly-gamma-glutamate synthetase (FPGS) for their antitumor activity, we designed and synthesized two classic
Autor:
James M. Cook, Hiteshkumar D. Jain, Subramanian Sankar, Samarpan Majumder, James P. Stables, Rahul V. Edwankar, Hao Zhou, Felix M. Rivas, Lauren Murphree, Shengming Huang, Chitra R. Edwankar, Werner Sieghart, Roman Furtmüller, Joachim Ramerstorfer, Bryan L. Roth
The antiseizure activity of benzodiazepines (BDZs) 1-5 in mice and rats as animal models is described. These BDZs have selective efficacy for alpha2beta3gamma2 and alpha3beta3gamma2 GABA(A)-receptors. Significant anticonvulsant activity with little o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::76d63f737fa4359697a8210faa497264
Autor:
Hideaki Kakeya, Hiroyuki Osada, Shuo Zhou, Jun Ma, Hiteshkumar D. Jain, James M. Cook, Xuebin Liao, Amy M. Deveau, Timothy L. Macdonald, Michael A. Johnson, Kirsten S. Smith, Xiaoxiang Liu, Christine M. Dieckhaus, Hao Zhou, Chunchun Zhang
Tryprostatin A is an inhibitor of breast cancer resistance protein, consequently a series of structure-activity studies on the cell cycle inhibitory effects of tryprostatin A analogues as potential antitumor antimitotic agents have been carried out.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a4cab7411a5ef1ee8fc6b5a3e6b0e304
https://europepmc.org/articles/PMC2435077/
https://europepmc.org/articles/PMC2435077/
Autor:
Aleem, Gangjee, Hiteshkumar D, Jain, Jaclyn, Phan, Xin, Lin, Xiaohong, Song, John J, McGuire, Roy L, Kisliuk
Publikováno v:
Journal of medicinal chemistry. 49(3)
We designed and synthesized a classical analogue N-[4-[(2-amino-6-ethyl-3,4-dihydro-4-oxo-7H-pyrrolo[2,3-d]pyrimidin-5-yl)thio]benzoyl]-L-glutamic acid (4) and thirteen nonclassical analogues 5-17 as potential dual thymidylate synthase (TS) and dihyd
Publikováno v:
ChemInform. 36
A series of ten novel 2-amino-4-oxo-5-[(substitutedbenzyl)thio]pyrrolo[2,3-d]pyrimidines 2-11 were synthesized as potential inhibitors of thymidylate synthase and as antitumor agents. The analogues contain various electron withdrawing and electron do