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Items: 1 to 50 of 161

1.
2.

Discovery of potent and selective inhibitors of Toxoplasma gondii thymidylate synthase for opportunistic infections.

Zaware N, Sharma H, Yang J, Devambatla RK, Queener SF, Anderson KS, Gangjee A.

ACS Med Chem Lett. 2013 Oct 4;4(12):1148-1151.

3.

Trimethoprim resistance of dihydrofolate reductase variants from clinical isolates of Pneumocystis jirovecii.

Queener SF, Cody V, Pace J, Torkelson P, Gangjee A.

Antimicrob Agents Chemother. 2013 Oct;57(10):4990-8. doi: 10.1128/AAC.01161-13. Epub 2013 Jul 29.

4.

Design, synthesis, and molecular modeling of novel pyrido[2,3-d]pyrimidine analogues as antifolates; application of Buchwald-Hartwig aminations of heterocycles.

Gangjee A, Namjoshi OA, Raghavan S, Queener SF, Kisliuk RL, Cody V.

J Med Chem. 2013 Jun 13;56(11):4422-41. doi: 10.1021/jm400086g. Epub 2013 May 21.

5.

Kinetic and structural analysis for potent antifolate inhibition of Pneumocystis jirovecii, Pneumocystis carinii, and human dihydrofolate reductases and their active-site variants.

Cody V, Pace J, Queener SF, Adair OO, Gangjee A.

Antimicrob Agents Chemother. 2013 Jun;57(6):2669-77. doi: 10.1128/AAC.00172-13. Epub 2013 Apr 1.

6.

Inhibitors of eIF2╬▒ dephosphorylation slow replication and stabilize latency in Toxoplasma gondii.

Konrad C, Queener SF, Wek RC, Sullivan WJ Jr.

Antimicrob Agents Chemother. 2013 Apr;57(4):1815-22. doi: 10.1128/AAC.01899-12. Epub 2013 Feb 4.

7.

Crystallographic analysis reveals a novel second binding site for trimethoprim in active site double mutants of human dihydrofolate reductase.

Cody V, Pace J, Piraino J, Queener SF.

J Struct Biol. 2011 Oct;176(1):52-9. doi: 10.1016/j.jsb.2011.06.001. Epub 2011 Jun 13.

8.

Phosphorylation of eukaryotic initiation factor-2{alpha} promotes the extracellular survival of obligate intracellular parasite Toxoplasma gondii.

Joyce BR, Queener SF, Wek RC, Sullivan WJ Jr.

Proc Natl Acad Sci U S A. 2010 Oct 5;107(40):17200-5. doi: 10.1073/pnas.1007610107. Epub 2010 Sep 20.

9.

Design, synthesis, biological evaluation and computational investigation of novel inhibitors of dihydrofolate reductase of opportunistic pathogens.

Bag S, Tawari NR, Degani MS, Queener SF.

Bioorg Med Chem. 2010 May 1;18(9):3187-97. doi: 10.1016/j.bmc.2010.03.031. Epub 2010 Mar 18.

PMID:
20363634
11.

2,4-Diamino-5-methyl-6-substituted arylthio-furo[2,3-d]pyrimidines as novel classical and nonclassical antifolates as potential dual thymidylate synthase and dihydrofolate reductase inhibitors.

Gangjee A, Jain HD, Phan J, Guo X, Queener SF, Kisliuk RL.

Bioorg Med Chem. 2010 Jan 15;18(2):953-61. doi: 10.1016/j.bmc.2009.11.029. Epub 2009 Dec 26.

12.

Synthesis and biological evaluation of biguanide and dihydrotriazine derivatives as potential inhibitors of dihydrofolate reductase of opportunistic microorganisms.

Bag S, Tawari NR, Queener SF, Degani MS.

J Enzyme Inhib Med Chem. 2010 Jun;25(3):331-9. doi: 10.3109/14756360903179443.

PMID:
19874136
13.

Design, synthesis, and X-ray crystal structures of 2,4-diaminofuro[2,3-d]pyrimidines as multireceptor tyrosine kinase and dihydrofolate reductase inhibitors.

Gangjee A, Li W, Lin L, Zeng Y, Ihnat M, Warnke LA, Green DW, Cody V, Pace J, Queener SF.

Bioorg Med Chem. 2009 Oct 15;17(20):7324-36. doi: 10.1016/j.bmc.2009.08.044. Epub 2009 Aug 22.

14.

Selective antifolates for chemically labeling proteins in mammalian cells.

Pedr├│ Rosa LE, Reddy DR, Queener SF, Miller LW.

Chembiochem. 2009 Jun 15;10(9):1462-4. doi: 10.1002/cbic.200900152. No abstract available.

15.

Correlations of inhibitor kinetics for Pneumocystis jirovecii and human dihydrofolate reductase with structural data for human active site mutant enzyme complexes.

Cody V, Pace J, Makin J, Piraino J, Queener SF, Rosowsky A.

Biochemistry. 2009 Mar 3;48(8):1702-11. doi: 10.1021/bi801960h.

16.

N9-substituted 2,4-diaminoquinazolines: synthesis and biological evaluation of lipophilic inhibitors of pneumocystis carinii and toxoplasma gondii dihydrofolate reductase.

Gangjee A, Adair OO, Pagley M, Queener SF.

J Med Chem. 2008 Oct 9;51(19):6195-200. doi: 10.1021/jm800694g. Epub 2008 Sep 5. Erratum in: J Med Chem. 2009 Aug 13;52(15):4979.

17.

Recombinant bovine dihydrofolate reductase produced by mutagenesis and nested PCR of murine dihydrofolate reductase cDNA.

Cody V, Mao Q, Queener SF.

Protein Expr Purif. 2008 Nov;62(1):104-10. doi: 10.1016/j.pep.2008.07.001. Epub 2008 Jul 17.

19.

Novel triazine JPC-2067-B inhibits Toxoplasma gondii in vitro and in vivo.

Mui EJ, Schiehser GA, Milhous WK, Hsu H, Roberts CW, Kirisits M, Muench S, Rice D, Dubey JP, Fowble JW, Rathod PK, Queener SF, Liu SR, Jacobus DP, McLeod R.

PLoS Negl Trop Dis. 2008 Mar 5;2(3):e190. doi: 10.1371/journal.pntd.0000190.

20.

Novel boron-containing, nonclassical antifolates: synthesis and preliminary biological and structural evaluation.

Reynolds RC, Campbell SR, Fairchild RG, Kisliuk RL, Micca PL, Queener SF, Riordan JM, Sedwick WD, Waud WR, Leung AK, Dixon RW, Suling WJ, Borhani DW.

J Med Chem. 2007 Jul 12;50(14):3283-9. Epub 2007 Jun 15.

PMID:
17569517
21.

Design and synthesis of classical and nonclassical 6-arylthio-2,4-diamino-5-ethylpyrrolo[2,3-d]pyrimidines as antifolates.

Gangjee A, Zeng Y, Talreja T, McGuire JJ, Kisliuk RL, Queener SF.

J Med Chem. 2007 Jun 28;50(13):3046-53. Epub 2007 Jun 7.

22.

Quinoline derivative MC1626, a putative GCN5 histone acetyltransferase (HAT) inhibitor, exhibits HAT-independent activity against Toxoplasma gondii.

Smith AT, Livingston MR, Mai A, Filetici P, Queener SF, Sullivan WJ Jr.

Antimicrob Agents Chemother. 2007 Mar;51(3):1109-11. Epub 2006 Dec 18.

25.

IMP dehydrogenase from the protozoan parasite Toxoplasma gondii.

Sullivan WJ Jr, Dixon SE, Li C, Striepen B, Queener SF.

Antimicrob Agents Chemother. 2005 Jun;49(6):2172-9.

26.
27.

Comparison of ternary complexes of Pneumocystis carinii and wild-type human dihydrofolate reductase with coenzyme NADPH and a novel classical antitumor furo[2,3-d]pyrimidine antifolate.

Cody V, Galitsky N, Luft JR, Pangborn W, Gangjee A, Devraj R, Queener SF, Blakley RL.

Acta Crystallogr D Biol Crystallogr. 1997 Nov 1;53(Pt 6):638-49.

PMID:
15299851
30.

Design, synthesis, and computational affinity prediction of ester soft drugs as inhibitors of dihydrofolate reductase from Pneumocystis carinii.

Graffner-Nordberg M, Kolmodin K, Aqvist J, Queener SF, Hallberg A.

Eur J Pharm Sci. 2004 May;22(1):43-54.

PMID:
15113582
31.

Structure determination of tetrahydroquinazoline antifolates in complex with human and Pneumocystis carinii dihydrofolate reductase: correlations between enzyme selectivity and stereochemistry.

Cody V, Luft JR, Pangborn W, Gangjee A, Queener SF.

Acta Crystallogr D Biol Crystallogr. 2004 Apr;60(Pt 4):646-55. Epub 2004 Mar 23.

PMID:
15039552
32.

Preliminary in vitro studies on two potent, water-soluble trimethoprim analogues with exceptional species selectivity against dihydrofolate reductase from Pneumocystis carinii and Mycobacterium avium.

Forsch RA, Queener SF, Rosowsky A.

Bioorg Med Chem Lett. 2004 Apr 5;14(7):1811-5. Erratum in: Bioorg Med Chem Lett. 2004 May 17;14(10):2693.

PMID:
15026078
33.

New 2,4-diamino-5-(2',5'-substituted benzyl)pyrimidines as potential drugs against opportunistic infections of AIDS and other immune disorders. Synthesis and species-dependent antifolate activity.

Rosowsky A, Forsch RA, Sibley CH, Inderlied CB, Queener SF.

J Med Chem. 2004 Mar 11;47(6):1475-86. Erratum in: J Med Chem. 2004 Jul 1;47(14):3705.

PMID:
14998335
35.

Synthesis and DHFR inhibitory activity of a series of 6-substituted-2,4-diaminothieno[2,3-d]pyrimidines.

Donkor IO, Li H, Queener SF.

Eur J Med Chem. 2003 Jun;38(6):605-11.

PMID:
12832132
36.

Molecular cloning and characterization of an SRCAP chromatin remodeling homologue in Toxoplasma gondii.

Sullivan WJ Jr, Monroy MA, Bohne W, Nallani KC, Chrivia J, Yaciuk P, Smith CK 2nd, Queener SF.

Parasitol Res. 2003 May;90(1):1-8. Epub 2003 Jan 28.

PMID:
12743798
39.

Analysis of quinazoline and pyrido[2,3-d]pyrimidine N9-C10 reversed-bridge antifolates in complex with NADP+ and Pneumocystis carinii dihydrofolate reductase.

Cody V, Galitsky N, Luft JR, Pangborn W, Queener SF, Gangjee A.

Acta Crystallogr D Biol Crystallogr. 2002 Sep;58(Pt 9):1393-9. Epub 2002 Aug 23.

PMID:
12198294
40.
41.

Structure-based enzyme inhibitor design: modeling studies and crystal structure analysis of Pneumocystis carinii dihydrofolate reductase ternary complex with PT653 and NADPH.

Cody V, Galitsky N, Luft JR, Pangborn W, Rosowsky A, Queener SF.

Acta Crystallogr D Biol Crystallogr. 2002 Jun;58(Pt 6 Pt 2):946-54. Epub 2002 May 29.

PMID:
12037296
43.

Synthesis of 2,4-diamino-6-(thioarylmethyl)pyrido[2,3-d]pyrimidines as dihydrofolate reductase inhibitors.

Gangjee A, Adair O, Queener SF.

Bioorg Med Chem. 2001 Nov;9(11):2929-35.

PMID:
11597474
44.

N,N'-bis[4-(N-alkylamidino)phenyl]homopiperazines as anti-Pneumocystis carinii agents.

Huang TL, Tao B, Quarshie Y, Queener SF, Donkor IO.

Bioorg Med Chem Lett. 2001 Oct 22;11(20):2679-81.

PMID:
11591500
45.

Isolation of rat dihydrofolate reductase gene and characterization of recombinant enzyme.

Wang Y, Bruenn JA, Queener SF, Cody V.

Antimicrob Agents Chemother. 2001 Sep;45(9):2517-23.

47.

Design, synthesis, computational prediction, and biological evaluation of ester soft drugs as inhibitors of dihydrofolate reductase from Pneumocystis carinii.

Graffner-Nordberg M, Kolmodin K, Aqvist J, Queener SF, Hallberg A.

J Med Chem. 2001 Jul 19;44(15):2391-402.

PMID:
11448221
48.

Synthesis, antifolate, and antitumor activities of classical and nonclassical 2-amino-4-oxo-5-substituted-pyrrolo[2,3-d]pyrimidines.

Gangjee A, Vidwans A, Elzein E, McGuire JJ, Queener SF, Kisliuk RL.

J Med Chem. 2001 Jun 7;44(12):1993-2003.

PMID:
11384244
49.
50.

Design, synthesis, and X-ray crystal structure of a potent dual inhibitor of thymidylate synthase and dihydrofolate reductase as an antitumor agent.

Gangjee A, Yu J, McGuire JJ, Cody V, Galitsky N, Kisliuk RL, Queener SF.

J Med Chem. 2000 Oct 19;43(21):3837-51.

PMID:
11052789

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