17 Papers
161 Citations
Jim Pace is an academic researcher from Hauptman-Woodward Medical Research Institute. The author has contributed to research in topics: Dihydrofolate reductase & Trimetrexate. The author has an hindex of 8, co-authored 17 publications.
Chat about Author
Papers
Design, Synthesis, and X-ray Crystal Structure of Classical and Nonclassical 2-Amino-4-oxo-5-substituted-6-ethylthieno[2,3-d]pyrimidines as Dual Thymidylate Synthase and Dihydrofolate Reductase Inhibitors and as Potential Antitumor Agents
TL;DR: Compound 2 was an excellent dual inhibitor of human TS and human DHFR and afforded nanomolar GI50 values against tumor cells in culture and X-ray crystal structures of 2 and 1 showed for the first time that the thieno[2,3-d]pyrimidine ring binds in a "folate" mode.
New insights into DHFR interactions: analysis of Pneumocystis carinii and mouse DHFR complexes with NADPH and two highly potent 5-(omega-carboxy(alkyloxy) trimethoprim derivatives reveals conformational correlations with activity and novel parallel ring stacking interactions.
TL;DR: The data suggest that the enhanced inhibitory activity of PY1011 compared with PY957 is, in part, due to the favorable contacts with Phe69 of pcDHFR by the methylene carbons of the inhibitor side chain that are oriented by the triple bond of the 1‐pentynyl side chain.
39
Design, synthesis, and X-ray crystal structures of 2,4-diaminofuro[2,3-d]pyrimidines as multireceptor tyrosine kinase and dihydrofolate reductase inhibitors.
Aleem Gangjee,Wei Li,Lu Lin,Yibin Zeng,Michael A. Ihnat,Linda A. Warnke,Dixy W. Green,Vivian Cody,Jim Pace,Sherry F. Queener +9 more
TL;DR: Inhibition of EGFR and PDGFR-beta were discovered for saturated C9-homologated analogs 9 and 10 that were absent in the saturated C8-C9 unsaturated compounds 2-7 and catalytic reduction gave the saturated 8-13.
36
Kinetic and Structural Analysis for Potent Antifolate Inhibition of Pneumocystis jirovecii, Pneumocystis carinii, and Human Dihydrofolate Reductases and Their Active-Site Variants
TL;DR: In this paper, the first kinetic and structural data for 2,4-diamino-6-[(2',5'-dichloro anilino)methyl]pyrido[2,3-d]pyrimidine (OAAG324) were reported.
22
Structural analysis of Pneumocystis carinii and human DHFR complexes with NADPH and a series of five potent 6-[5'-(ω-carboxyalkoxy)benzyl]pyrido[2,3-d]pyrimidine derivatives.
Vivian Cody,Vivian Cody,Jim Pace +2 more
TL;DR: Structural results suggest that the weaker binding of this series compared with that of their pyrimidine homologs in part arises from the flexibility observed in their side-chain conformations, which do not optimize intermolecular contact to Arg75.
21