Keli Agama

Keli Agama

UNVERIFIED PROFILE

Are you Keli Agama?   Register this Author

Register author
Keli Agama

Keli Agama

Publications by authors named "Keli Agama"

Are you Keli Agama?   Register this Author

67Publications

1261Reads

9Profile Views

The antitumor activity of CYB-L10, a human topoisomerase IB catalytic inhibitor.

J Enzyme Inhib Med Chem 2019 Dec;34(1):818-822

a School of Pharmaceutical Sciences , Sun Yat-sen University , Guangzhou , China.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1080/14756366.2018.1516651DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6442119PMC
December 2019

Synthesis and biological evaluation of 5-aminoethyl benzophenanthridone derivatives as DNA topoisomerase IB inhibitors.

Eur J Med Chem 2019 Sep 30;178:81-92. Epub 2019 May 30.

School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, 510006, China; Guangdong Provincial Key Laboratory of New Drug Design and Evaluation, Guangzhou, 510006, China. Electronic address:

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejmech.2019.05.074DOI Listing
September 2019

Application of Sequential Palladium Catalysis for the Discovery of Janus Kinase Inhibitors in the Benzo[ c]pyrrolo[2,3- h][1,6]naphthyridin-5-one (BPN) Series.

J Med Chem 2018 12 21;61(23):10440-10462. Epub 2018 Nov 21.

Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy , Purdue University , West Lafayette , Indiana 47907 , United States.

View Article

Download full-text PDF

Source
http://pubs.acs.org/doi/10.1021/acs.jmedchem.8b00510
Publisher Site
http://dx.doi.org/10.1021/acs.jmedchem.8b00510DOI Listing
December 2018

Novel Fluoroindenoisoquinoline Non-Camptothecin Topoisomerase I Inhibitors.

Mol Cancer Ther 2018 08 10;17(8):1694-1704. Epub 2018 May 10.

Developmental Therapeutics Branch & Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, NIH, Bethesda, Maryland.

View Article

Download full-text PDF

Source
http://mct.aacrjournals.org/lookup/doi/10.1158/1535-7163.MCT
Publisher Site
http://dx.doi.org/10.1158/1535-7163.MCT-18-0028DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6072611PMC
August 2018

Distribution bias and biochemical characterization of TOP1MT single nucleotide variants.

Sci Rep 2017 08 17;7(1):8614. Epub 2017 Aug 17.

Laboratory of Molecular Pharmacology, Developmental Therapeutics Branch, Center for Cancer Research, NCI, National Institutes of Health, Bethesda, MD, 20892, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1038/s41598-017-09258-2DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5561071PMC
August 2017

Design and Synthesis of Chlorinated and Fluorinated 7-Azaindenoisoquinolines as Potent Cytotoxic Anticancer Agents That Inhibit Topoisomerase I.

J Med Chem 2017 07 28;60(13):5364-5376. Epub 2017 Jun 28.

Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, and the Purdue Center for Cancer Research, Purdue University , West Lafayette, Indiana 47907, United States.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/acs.jmedchem.6b01870DOI Listing
July 2017

Synthesis and Biological Evaluation of the First Triple Inhibitors of Human Topoisomerase 1, Tyrosyl-DNA Phosphodiesterase 1 (Tdp1), and Tyrosyl-DNA Phosphodiesterase 2 (Tdp2).

J Med Chem 2017 04 18;60(8):3275-3288. Epub 2017 Apr 18.

Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, and the Purdue Center for Cancer Research, Purdue University , West Lafayette, Indiana 47907, United States.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/acs.jmedchem.6b01565DOI Listing
April 2017

Phenanthriplatin Acts As a Covalent Poison of Topoisomerase II Cleavage Complexes.

ACS Chem Biol 2016 11 6;11(11):2996-3001. Epub 2016 Oct 6.

Department of Chemistry, Massachusetts Institute of Technology , Cambridge, Massachusetts 02139, United States.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/acschembio.6b00565DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5248983PMC
November 2016

Design, Synthesis, and Biological Evaluation of Potential Prodrugs Related to the Experimental Anticancer Agent Indotecan (LMP400).

J Med Chem 2016 05 20;59(10):4890-9. Epub 2016 Apr 20.

Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, and the Purdue Center for Cancer Research, Purdue University , West Lafayette, Indiana 47907, United States .

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/acs.jmedchem.6b00220DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5317102PMC
May 2016

Synthesis and biological evaluation of new fluorinated and chlorinated indenoisoquinoline topoisomerase I poisons.

Bioorg Med Chem 2016 Apr 9;24(7):1469-79. Epub 2016 Feb 9.

Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, and the Purdue Center for Cancer Research, Purdue University, West Lafayette, IN 47907, United States. Electronic address:

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bmc.2016.02.015DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4789169PMC
April 2016

Investigation of the Structure-Activity Relationships of Aza-A-Ring Indenoisoquinoline Topoisomerase I Poisons.

J Med Chem 2016 04 12;59(8):3840-53. Epub 2016 Apr 12.

Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, and the Purdue Center for Cancer Research, Purdue University , West Lafayette, Indiana 47907, United States.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/acs.jmedchem.6b00003DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5317104PMC
April 2016

Characterization of DNA topoisomerase I in three SN-38 resistant human colon cancer cell lines reveals a new pair of resistance-associated mutations.

J Exp Clin Cancer Res 2016 Mar 31;35:56. Epub 2016 Mar 31.

National Institutes of Health, National Cancer Institute, Center for Cancer Research, Laboratory of Molecular Pharmacology, 37 Convent Drive, Building 37, Room 5068, Bethesda, MD, 20892-4255, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1186/s13046-016-0335-xDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4815242PMC
March 2016

Single-Molecule Supercoil Relaxation Assay as a Screening Tool to Determine the Mechanism and Efficacy of Human Topoisomerase IB Inhibitors.

Mol Cancer Ther 2015 Nov 8;14(11):2552-9. Epub 2015 Sep 8.

Laboratory of Single Molecule Biophysics, NHLBI, National Institutes of Health, Bethesda, Maryland.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1158/1535-7163.MCT-15-0454DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4636450PMC
November 2015

Discovery of potent indenoisoquinoline topoisomerase I poisons lacking the 3-nitro toxicophore.

J Med Chem 2015 May 24;58(9):3997-4015. Epub 2015 Apr 24.

†Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, and the Purdue Center for Cancer Research, Purdue University, 575 Stadium Mall Drive, West Lafayette, Indiana 47907, United States.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/acs.jmedchem.5b00303DOI Listing
May 2015

Synthesis and biological evaluation of nitrated 7-, 8-, 9-, and 10-hydroxyindenoisoquinolines as potential dual topoisomerase I (Top1)-tyrosyl-DNA phosphodiesterase I (TDP1) inhibitors.

J Med Chem 2015 Apr 26;58(7):3188-208. Epub 2015 Mar 26.

†Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, and the Purdue Center for Cancer Research, Purdue University, 575 Stadium Mall Drive, West Lafayette, Indiana 47907, United States.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/acs.jmedchem.5b00136DOI Listing
April 2015

Poisoning of mitochondrial topoisomerase I by lamellarin D.

Mol Pharmacol 2014 Aug 2;86(2):193-9. Epub 2014 Jun 2.

Developmental Therapeutics Branch and Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute (S.K., K.A., I.D.R., S.A., K.F., H.Z., Y.P.) and Laboratory of Molecular Biophysics, National Heart, Lung, and Blood Institute (Y.S., K.C.N.), National Institutes of Health, Bethesda, Maryland

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1124/mol.114.092833DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4127927PMC
August 2014

Mapping topoisomerase sites in mitochondrial DNA with a poisonous mitochondrial topoisomerase I (Top1mt).

J Biol Chem 2014 Jun 5;289(26):18595-602. Epub 2014 May 5.

From the Laboratory of Molecular Pharmacology, Developmental Therapeutics Branch, Center for Cancer Research, NCI, National Institutes of Health, Bethesda, Maryland 20892

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1074/jbc.M114.555367DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4140277PMC
June 2014

Design, synthesis, and biological evaluation of O-2-modified indenoisoquinolines as dual topoisomerase I-tyrosyl-DNA phosphodiesterase I inhibitors.

J Med Chem 2014 May 6;57(10):4324-36. Epub 2014 May 6.

Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, and the Purdue Center for Cancer Research, Purdue University , West Lafayette, Indiana 47907, United States.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/jm500294aDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4033654PMC
May 2014

Optimization of the lactam side chain of 7-azaindenoisoquinoline topoisomerase I inhibitors and mechanism of action studies in cancer cells.

J Med Chem 2014 Feb 6;57(4):1289-98. Epub 2014 Feb 6.

Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, and The Purdue Center for Cancer Research, Purdue University , West Lafayette, Indiana 47907, United States.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/jm401471vDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3983387PMC
February 2014

Synthesis and biological evaluation of new carbohydrate-substituted indenoisoquinoline topoisomerase I inhibitors and improved syntheses of the experimental anticancer agents indotecan (LMP400) and indimitecan (LMP776).

J Med Chem 2014 Feb 11;57(4):1495-512. Epub 2014 Feb 11.

Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, and the Purdue Center for Cancer Research, Purdue University , West Lafayette, Indiana 47907, United States.

View Article

Download full-text PDF

Source
http://pubs.acs.org/doi/10.1021/jm401814y
Publisher Site
http://dx.doi.org/10.1021/jm401814yDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3983348PMC
February 2014

Epigenetic and genetic inactivation of tyrosyl-DNA-phosphodiesterase 1 (TDP1) in human lung cancer cells from the NCI-60 panel.

DNA Repair (Amst) 2014 Jan 16;13:1-9. Epub 2013 Dec 16.

Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, MD 20892, USA. Electronic address:

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.dnarep.2013.09.001DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3919147PMC
January 2014

Development of purely structure-based pharmacophores for the topoisomerase I-DNA-ligand binding pocket.

J Comput Aided Mol Des 2013 Dec 1;27(12):1037-49. Epub 2013 Dec 1.

Department of Pharmacology, School of Medical Sciences, University of New South Wales, Sydney, NSW, 2052, Australia.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1007/s10822-013-9695-xDOI Listing
December 2013

Synthesis and biological evaluation of indenoisoquinolines that inhibit both tyrosyl-DNA phosphodiesterase I (Tdp1) and topoisomerase I (Top1).

J Med Chem 2013 Jan 21;56(1):182-200. Epub 2012 Dec 21.

Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, and the Purdue Center for Cancer Research, Purdue University, West Lafayette, Indiana 47907, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/jm3014458DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3542538PMC
January 2013

Dibenzo[c,h][1,5]naphthyridinediones as topoisomerase I inhibitors: design, synthesis, and biological evaluation.

J Org Chem 2012 Jun 15;77(11):5167-72. Epub 2012 May 15.

Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy and The Purdue Center for Cancer Research, Purdue University, West Lafayette, Indiana 47907, United States.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/jo3006039DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3370419PMC
June 2012

Synthesis and biological evaluation of the first dual tyrosyl-DNA phosphodiesterase I (Tdp1)-topoisomerase I (Top1) inhibitors.

J Med Chem 2012 05 26;55(9):4457-78. Epub 2012 Apr 26.

Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, and the Purdue Center for Cancer Research, Purdue University, West Lafayette, Indiana 47907, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/jm300335nDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3350798PMC
May 2012

Exploring DNA topoisomerase I ligand space in search of novel anticancer agents.

PLoS One 2011 22;6(9):e25150. Epub 2011 Sep 22.

Department of Pharmacology, School of Medical Sciences, University of New South Wales, Sydney, Australia.

View Article

Download full-text PDF

Source
http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0025150PLOS
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3178613PMC
February 2012

Azaindenoisoquinolines as topoisomerase I inhibitors and potential anticancer agents: a systematic study of structure-activity relationships.

J Med Chem 2012 Feb 13;55(4):1682-97. Epub 2012 Feb 13.

Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, and The Purdue Center for Cancer Research, Purdue University, West Lafayette, Indiana 47907, United States.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/jm201512xDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3292051PMC
February 2012

Mus81-mediated DNA cleavage resolves replication forks stalled by topoisomerase I-DNA complexes.

J Cell Biol 2011 Nov;195(5):739-49

Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, MD 20892, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1083/jcb.201104003DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3257568PMC
November 2011

7-azaindenoisoquinolines as topoisomerase I inhibitors and potential anticancer agents.

J Med Chem 2011 Sep 8;54(17):6106-16. Epub 2011 Aug 8.

Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, and The Purdue Center for Cancer Research, Purdue University, West Lafayette, Indiana 47907, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/jm200719vDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3165090PMC
September 2011

Alcohol-, diol-, and carbohydrate-substituted indenoisoquinolines as topoisomerase I inhibitors: investigating the relationships involving stereochemistry, hydrogen bonding, and biological activity.

J Med Chem 2011 Jul 28;54(14):4937-53. Epub 2011 Jun 28.

Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, and the Purdue Center for Cancer Research, Purdue University, West Lafayette, Indiana 47907, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/jm101338zDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3151643PMC
July 2011

Poly(ADP-ribose) polymerase and XPF-ERCC1 participate in distinct pathways for the repair of topoisomerase I-induced DNA damage in mammalian cells.

Nucleic Acids Res 2011 May 11;39(9):3607-20. Epub 2011 Jan 11.

Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, National Institute of Health, Bethesda, MD 20892, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1093/nar/gkq1304DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3089458PMC
May 2011

A novel DNA topoisomerase I inhibitor with different mechanism from camptothecin induces G2/M phase cell cycle arrest to K562 cells.

Biochemistry 2010 Nov 8;49(47):10131-6. Epub 2010 Nov 8.

Institute of Medicinal Chemistry, Sun Yat-sen University, Guangzhou 510006, China.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/bi1009419DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3010555PMC
November 2010

The structure-activity relationships of A-ring-substituted aromathecin topoisomerase I inhibitors strongly support a camptothecin-like binding mode.

Bioorg Med Chem 2010 Aug 20;18(15):5535-52. Epub 2010 Jun 20.

Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmaceutical Sciences, and the Purdue Center for Cancer Research, Purdue University, West Lafayette, IN 47907, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bmc.2010.06.040DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2911012PMC
August 2010

Topoisomerase I levels in the NCI-60 cancer cell line panel determined by validated ELISA and microarray analysis and correlation with indenoisoquinoline sensitivity.

Mol Cancer Ther 2009 Jul 7;8(7):1878-84. Epub 2009 Jul 7.

Laboratory of Human Toxicology and Pharmacology, Applied/Developmental Research Support Directorate, Science Applications International Corporation-Frederick Inc, National Cancer Institute-Frederick, Frederick, MD 21702, USA.

View Article

Download full-text PDF

Source
http://mct.aacrjournals.org/cgi/doi/10.1158/1535-7163.MCT-09
Publisher Site
http://dx.doi.org/10.1158/1535-7163.MCT-09-0016DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2728499PMC
July 2009

The iron chelator Dp44mT causes DNA damage and selective inhibition of topoisomerase IIalpha in breast cancer cells.

Cancer Res 2009 Feb 27;69(3):948-57. Epub 2009 Jan 27.

US Department of Health and Human Services, Laboratory of Biochemistry, Center for Drug Evaluation and Research, Food and Drug Administration, Bethesda, Maryland, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1158/0008-5472.CAN-08-1437DOI Listing
February 2009

Targeting tumor cells expressing p53 with a water-soluble inhibitor of Hdm2.

Mol Cancer Ther 2008 Aug;7(8):2445-54

Laboratory of Protein Dynamics and Signaling, National Cancer Institute at Frederick, 1050 Boyles Street, Frederick, MD 21702, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1158/1535-7163.MCT-08-0063DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2588467PMC
August 2008

Aminoflavone induces oxidative DNA damage and reactive oxidative species-mediated apoptosis in breast cancer cells.

Int J Cancer 2008 Apr;122(7):1665-74

Department of Biochemistry and Microbiology, Loma Linda University School of Medicine, Loma Linda, CA 92350, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1002/ijc.23244DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2693190PMC
April 2008

Novel E-ring camptothecin keto analogues (S38809 and S39625) are stable, potent, and selective topoisomerase I inhibitors without being substrates of drug efflux transporters.

Mol Cancer Ther 2007 Dec;6(12 Pt 1):3229-38

Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, NIH, 37 Convent Drive, Building 37, Room 5068, Bethesda, MD 20892-4255, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1158/1535-7163.MCT-07-0441DOI Listing
December 2007

Batracylin (NSC 320846), a dual inhibitor of DNA topoisomerases I and II induces histone gamma-H2AX as a biomarker of DNA damage.

Cancer Res 2007 Oct;67(20):9971-9

Laboratory of Molecular Pharmacology and Developmental Therapeutics Program, National Cancer Institute, Department of Health and Human Services, Bethesda, Maryland 20892, USA.

View Article

Download full-text PDF

Source
http://cancerres.aacrjournals.org/cgi/doi/10.1158/0008-5472.
Publisher Site
http://dx.doi.org/10.1158/0008-5472.CAN-07-0804DOI Listing
October 2007

Investigation of the lactam side chain length necessary for optimal indenoisoquinoline topoisomerase I inhibition and cytotoxicity in human cancer cell cultures.

J Med Chem 2007 May 3;50(9):2040-8. Epub 2007 Apr 3.

Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmaceutical Sciences, and the Purdue Cancer Center, Purdue University, West Lafayette, Indiana 47907, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/jm0613119DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2519145PMC
May 2007

Repair of topoisomerase I-mediated DNA damage.

Prog Nucleic Acid Res Mol Biol 2006 ;81:179-229

Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, National Institutes of Health, DHHS, Bethesda, Maryland 20892, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/S0079-6603(06)81005-6DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2576451PMC
February 2007

Hereditary ataxia SCAN1 cells are defective for the repair of transcription-dependent topoisomerase I cleavage complexes.

DNA Repair (Amst) 2006 Dec 28;5(12):1489-94. Epub 2006 Aug 28.

Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, MD 20892, USA.

View Article

Download full-text PDF

Source
http://linkinghub.elsevier.com/retrieve/pii/S156878640600238
Publisher Site
http://dx.doi.org/10.1016/j.dnarep.2006.07.004DOI Listing
December 2006

Activation of aminoflavone (NSC 686288) by a sulfotransferase is required for the antiproliferative effect of the drug and for induction of histone gamma-H2AX.

Cancer Res 2006 Oct;66(19):9656-64

Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, NIH, Bethesda, MD 20892-4255, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1158/0008-5472.CAN-06-0796DOI Listing
October 2006

Synthesis and evaluation of indenoisoquinoline topoisomerase I inhibitors substituted with nitrogen heterocycles.

J Med Chem 2006 Oct;49(21):6283-9

Department of Medicinal Chemistry and Molecular Pharmacology, and the Purdue Cancer Center, School of Pharmacy and Pharmaceutical Sciences, Purdue University, West Lafayette, Indiana 47907, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/jm060564zDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2526314PMC
October 2006

Synthesis and biological assays of E-ring analogs of camptothecin and homocamptothecin.

Bioorg Med Chem 2006 Sep 21;14(18):6202-12. Epub 2006 Jun 21.

Department of Chemistry, University of Pittsburgh, Pittsburgh, PA 15260, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bmc.2006.05.073DOI Listing
September 2006

Bisindenoisoquinoline bis-1,3-{(5,6-dihydro-5,11-diketo-11H-indeno[1,2-c]isoquinoline)-6-propylamino}propane bis(trifluoroacetate) (NSC 727357), a DNA intercalator and topoisomerase inhibitor with antitumor activity.

Mol Pharmacol 2006 Sep 23;70(3):1109-20. Epub 2006 Jun 23.

Laboratory of Molecular Pharmacology, National Cancer Institute, 37 Convent Dr., Bldg. 37, Room 5068, National Institutes of Health, Bethesda, MD 20892-4255, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1124/mol.106.024372DOI Listing
September 2006

Synthesis and biological evaluation of bisindenoisoquinolines as topoisomerase I inhibitors.

J Med Chem 2006 Aug;49(17):5129-40

Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmaceutical Sciences and the Purdue Cancer Center, Purdue University, West Lafayette, Indiana 47907, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/jm060046oDOI Listing
August 2006

Anti-tumor drug candidate 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole induces single-strand breaks and DNA-protein cross-links in sensitive MCF-7 breast cancer cells.

Cancer Chemother Pharmacol 2006 Jul 6;58(1):62-72. Epub 2005 Dec 6.

Developmental Therapeutics Program, National Cancer Institute at Frederick, Building 1047, Room 7, MD 21701, USA.

View Article

Download full-text PDF

Source
http://link.springer.com/10.1007/s00280-005-0127-z
Publisher Site
http://dx.doi.org/10.1007/s00280-005-0127-zDOI Listing
July 2006

4-nitroquinoline-1-oxide induces the formation of cellular topoisomerase I-DNA cleavage complexes.

Cancer Res 2006 Jul;66(13):6540-5

Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute/NIH, Bethesda, MD 20892, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1158/0008-5472.CAN-05-4471DOI Listing
July 2006

Total and semisynthesis and in vitro studies of both enantiomers of 20-fluorocamptothecin.

Bioorg Med Chem Lett 2005 Nov;15(21):4736-40

Department of Chemistry, University of Pittsburgh, Pittsburgh, PA 15260, USA.

View Article

Download full-text PDF

Source
http://linkinghub.elsevier.com/retrieve/pii/S0960894X0500988
Publisher Site
http://dx.doi.org/10.1016/j.bmcl.2005.07.074DOI Listing
November 2005

Cellular topoisomerase I inhibition and antiproliferative activity by MJ-III-65 (NSC 706744), an indenoisoquinoline topoisomerase I poison.

Mol Pharmacol 2005 Feb 5;67(2):523-30. Epub 2004 Nov 5.

Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, 37 Convent Dr., National Institutes of Health, Bethesda, MD 20892, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1124/mol.104.003889DOI Listing
February 2005