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Items: 1 to 50 of 72

1.

A systematic study of nitrated indenoisoquinolines reveals a potent topoisomerase I inhibitor.

Morrell A, Antony S, Kohlhagen G, Pommier Y, Cushman M.

J Med Chem. 2006 Dec 28;49(26):7740-53.

2.

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

Nagarajan M, Morrell A, Ioanoviciu A, Antony S, Kohlhagen G, Agama K, Hollingshead M, Pommier Y, Cushman M.

J Med Chem. 2006 Oct 19;49(21):6283-9.

3.

Synthesis and biological evaluation of bisindenoisoquinolines as topoisomerase I inhibitors.

Nagarajan M, Morrell A, Antony S, Kohlhagen G, Agama K, Pommier Y, Ragazzon PA, Garbett NC, Chaires JB, Hollingshead M, Cushman M.

J Med Chem. 2006 Aug 24;49(17):5129-40.

PMID:
16913702
4.

Synthesis of benz[d]indeno[1,2-b]pyran-5,11-diones: versatile intermediates for the design and synthesis of topoisomerase I inhibitors.

Morrell A, Antony S, Kohlhagen G, Pommier Y, Cushman M.

Bioorg Med Chem Lett. 2006 Apr 1;16(7):1846-9. Epub 2006 Jan 25.

PMID:
16442283
5.

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.

Brantley E, Antony S, Kohlhagen G, Meng L, Agama K, Stinson SF, Sausville EA, Pommier Y.

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

PMID:
16331501
6.

Camptothecin analogs with enhanced activity against human breast cancer cells. I. Correlation of potency with lipophilicity and persistence in the cleavage complex.

Adams DJ, da Silva MW, Flowers JL, Kohlhagen G, Pommier Y, Colvin OM, Manikumar G, Wani MC.

Cancer Chemother Pharmacol. 2006 Jan;57(2):135-44. Epub 2005 Aug 23.

PMID:
16151810
7.
8.

A novel polypyrimidine antitumor agent FdUMP[10] induces thymineless death with topoisomerase I-DNA complexes.

Liao ZY, Sordet O, Zhang HL, Kohlhagen G, Antony S, Gmeiner WH, Pommier Y.

Cancer Res. 2005 Jun 1;65(11):4844-51.

9.

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

Antony S, Kohlhagen G, Agama K, Jayaraman M, Cao S, Durrani FA, Rustum YM, Cushman M, Pommier Y.

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

PMID:
15531731
10.

Synthesis and anticancer activity of simplified indenoisoquinoline topoisomerase I inhibitors lacking substituents on the aromatic rings.

Nagarajan M, Morrell A, Fort BC, Meckley MR, Antony S, Kohlhagen G, Pommier Y, Cushman M.

J Med Chem. 2004 Nov 4;47(23):5651-61.

PMID:
15509164
11.

Novel autoxidative cleavage reaction of 9-fluoredenes discovered during synthesis of a potential DNA-threading indenoisoquinoline.

Xiao X, Antony S, Kohlhagen G, Pommier Y, Cushman M.

J Org Chem. 2004 Oct 29;69(22):7495-501.

PMID:
15497974
12.

Phosphorylation of DNA topoisomerase I by the c-Abl tyrosine kinase confers camptothecin sensitivity.

Yu D, Khan E, Khaleque MA, Lee J, Laco G, Kohlhagen G, Kharbanda S, Cheng YC, Pommier Y, Bharti A.

J Biol Chem. 2004 Dec 10;279(50):51851-61. Epub 2004 Sep 24.

13.

Apoptotic topoisomerase I-DNA complexes induced by staurosporine-mediated oxygen radicals.

Sordet O, Khan QA, Plo I, Pourquier P, Urasaki Y, Yoshida A, Antony S, Kohlhagen G, Solary E, Saparbaev M, Laval J, Pommier Y.

J Biol Chem. 2004 Nov 26;279(48):50499-504. Epub 2004 Sep 22.

14.

Analysis of human topoisomerase I inhibition and interaction with the cleavage site +1 deoxyguanosine, via in vitro experiments and molecular modeling studies.

Laco GS, Du W, Kohlhagen G, Sayer JM, Jerina DM, Burke TG, Curran DP, Pommier Y.

Bioorg Med Chem. 2004 Oct 1;12(19):5225-35.

PMID:
15351405
15.
16.

Cytotoxicity, DNA strand breakage and DNA-protein crosslinking by a novel transplatinum compound in human A2780 ovarian and MCF-7 breast carcinoma cells.

Farrell N, Povirk LF, Dange Y, DeMasters G, Gupta MS, Kohlhagen G, Khan QA, Pommier Y, Gewirtz DA.

Biochem Pharmacol. 2004 Sep 1;68(5):857-66.

PMID:
15294448
17.

In vitro evaluation of dimethane sulfonate analogues with potential alkylating activity and selective renal cell carcinoma cytotoxicity.

Mertins SD, Myers TG, Holbeck SL, Medina-Perez W, Wang E, Kohlhagen G, Pommier Y, Bates SE.

Mol Cancer Ther. 2004 Jul;3(7):849-60.

18.

Synthesis of nitrated indenoisoquinolines as topoisomerase I inhibitors.

Morrell A, Antony S, Kohlhagen G, Pommier Y, Cushman M.

Bioorg Med Chem Lett. 2004 Jul 16;14(14):3659-63.

PMID:
15203138
19.

Topoisomerase I-DNA complexes contribute to arsenic trioxide-induced apoptosis.

Sordet O, Liao Z, Liu H, Antony S, Stevens EV, Kohlhagen G, Fu H, Pommier Y.

J Biol Chem. 2004 Aug 6;279(32):33968-75. Epub 2004 Jun 3.

20.

ABCG2 mediates differential resistance to SN-38 (7-ethyl-10-hydroxycamptothecin) and homocamptothecins.

Bates SE, Medina-Pérez WY, Kohlhagen G, Antony S, Nadjem T, Robey RW, Pommier Y.

J Pharmacol Exp Ther. 2004 Aug;310(2):836-42. Epub 2004 Apr 9.

PMID:
15075385
21.

Altered serine/arginine-rich protein phosphorylation and exonic enhancer-dependent splicing in Mammalian cells lacking topoisomerase I.

Soret J, Gabut M, Dupon C, Kohlhagen G, Stévenin J, Pommier Y, Tazi J.

Cancer Res. 2003 Dec 1;63(23):8203-11.

22.

Design, synthesis, and biological evaluation of indenoisoquinoline topoisomerase I inhibitors featuring polyamine side chains on the lactam nitrogen.

Nagarajan M, Xiao X, Antony S, Kohlhagen G, Pommier Y, Cushman M.

J Med Chem. 2003 Dec 18;46(26):5712-24.

PMID:
14667224
23.

Repair of and checkpoint response to topoisomerase I-mediated DNA damage.

Pommier Y, Redon C, Rao VA, Seiler JA, Sordet O, Takemura H, Antony S, Meng L, Liao Z, Kohlhagen G, Zhang H, Kohn KW.

Mutat Res. 2003 Nov 27;532(1-2):173-203. Review.

PMID:
14643436
25.

Inhibition of histone deacetylase increases cytotoxicity to anticancer drugs targeting DNA.

Kim MS, Blake M, Baek JH, Kohlhagen G, Pommier Y, Carrier F.

Cancer Res. 2003 Nov 1;63(21):7291-300.

26.

Position-specific trapping of topoisomerase II by benzo[a]pyrene diol epoxide adducts: implications for interactions with intercalating anticancer agents.

Khan QA, Kohlhagen G, Marshall R, Austin CA, Kalena GP, Kroth H, Sayer JM, Jerina DM, Pommier Y.

Proc Natl Acad Sci U S A. 2003 Oct 14;100(21):12498-503. Epub 2003 Oct 1.

27.

Association of XRCC1 and tyrosyl DNA phosphodiesterase (Tdp1) for the repair of topoisomerase I-mediated DNA lesions.

Plo I, Liao ZY, Barceló JM, Kohlhagen G, Caldecott KW, Weinfeld M, Pommier Y.

DNA Repair (Amst). 2003 Oct 7;2(10):1087-100.

PMID:
13679147
28.

Design, synthesis, and biological evaluation of cytotoxic 11-alkenylindenoisoquinoline topoisomerase I inhibitors and indenoisoquinoline-camptothecin hybrids.

Fox BM, Xiao X, Antony S, Kohlhagen G, Pommier Y, Staker BL, Stewart L, Cushman M.

J Med Chem. 2003 Jul 17;46(15):3275-82.

PMID:
12852757
29.

Dual role of glutathione in modulating camptothecin activity: depletion potentiates activity, but conjugation enhances the stability of the topoisomerase I-DNA cleavage complex.

Gamcsik MP, Kasibhatla MS, Adams DJ, Flowers JL, Colvin OM, Manikumar G, Wani M, Wall ME, Kohlhagen G, Pommier Y.

Mol Cancer Ther. 2001 Nov;1(1):11-20.

30.

Induction of breast cancer resistance protein by the camptothecin derivative DX-8951f is associated with minor reduction of antitumour activity.

van Hattum AH, Hoogsteen IJ, Schlüper HM, Maliepaard M, Scheffer GL, Scheper RJ, Kohlhagen G, Pommier Y, Pinedo HM, Boven E.

Br J Cancer. 2002 Sep 9;87(6):665-72.

31.

Gemcitabine (2',2'-difluoro-2'-deoxycytidine), an antimetabolite that poisons topoisomerase I.

Pourquier P, Gioffre C, Kohlhagen G, Urasaki Y, Goldwasser F, Hertel LW, Yu S, Pon RT, Gmeiner WH, Pommier Y.

Clin Cancer Res. 2002 Aug;8(8):2499-504.

32.
33.

Processing of nucleopeptides mimicking the topoisomerase I-DNA covalent complex by tyrosyl-DNA phosphodiesterase.

Debéthune L, Kohlhagen G, Grandas A, Pommier Y.

Nucleic Acids Res. 2002 Mar 1;30(5):1198-204.

34.
35.

Characterization of BTBD1 and BTBD2, two similar BTB-domain-containing Kelch-like proteins that interact with Topoisomerase I.

Xu L, Yang L, Hashimoto K, Anderson M, Kohlhagen G, Pommier Y, D'Arpa P.

BMC Genomics. 2002;3:1. Epub 2002 Jan 7.

36.
37.

Human mitochondrial topoisomerase I.

Zhang H, Barceló JM, Lee B, Kohlhagen G, Zimonjic DB, Popescu NC, Pommier Y.

Proc Natl Acad Sci U S A. 2001 Sep 11;98(19):10608-13. Epub 2001 Aug 28.

38.

Characterization of a novel topoisomerase I mutation from a camptothecin-resistant human prostate cancer cell line.

Urasaki Y, Laco GS, Pourquier P, Takebayashi Y, Kohlhagen G, Gioffre C, Zhang H, Chatterjee D, Pantazis P, Pommier Y.

Cancer Res. 2001 Mar 1;61(5):1964-9.

40.
41.

The novel silatecan 7-tert-butyldimethylsilyl-10-hydroxycamptothecin displays high lipophilicity, improved human blood stability, and potent anticancer activity.

Bom D, Curran DP, Kruszewski S, Zimmer SG, Thompson Strode J, Kohlhagen G, Du W, Chavan AJ, Fraley KA, Bingcang AL, Latus LJ, Pommier Y, Burke TG.

J Med Chem. 2000 Oct 19;43(21):3970-80.

PMID:
11052802
42.

Synthesis of new indeno[1,2-c]isoquinolines: cytotoxic non-camptothecin topoisomerase I inhibitors.

Cushman M, Jayaraman M, Vroman JA, Fukunaga AK, Fox BM, Kohlhagen G, Strumberg D, Pommier Y.

J Med Chem. 2000 Oct 5;43(20):3688-98.

PMID:
11020283
43.

Position-specific trapping of topoisomerase I-DNA cleavage complexes by intercalated benzo[a]- pyrene diol epoxide adducts at the 6-amino group of adenine.

Pommier Y, Laco GS, Kohlhagen G, Sayer JM, Kroth H, Jerina DM.

Proc Natl Acad Sci U S A. 2000 Sep 26;97(20):10739-44.

44.

Induction of topoisomerase I cleavage complexes by 1-beta -D-arabinofuranosylcytosine (ara-C) in vitro and in ara-C-treated cells.

Pourquier P, Takebayashi Y, Urasaki Y, Gioffre C, Kohlhagen G, Pommier Y.

Proc Natl Acad Sci U S A. 2000 Feb 15;97(4):1885-90.

45.

Benzo[a]pyrene diol epoxide adducts in DNA are potent suppressors of a normal topoisomerase I cleavage site and powerful inducers of other topoisomerase I cleavages.

Pommier Y, Kohlhagen G, Pourquier P, Sayer JM, Kroth H, Jerina DM.

Proc Natl Acad Sci U S A. 2000 Feb 29;97(5):2040-5.

46.

Camptothecin resistance: role of the ATP-binding cassette (ABC), mitoxantrone-resistance half-transporter (MXR), and potential for glucuronidation in MXR-expressing cells.

Brangi M, Litman T, Ciotti M, Nishiyama K, Kohlhagen G, Takimoto C, Robey R, Pommier Y, Fojo T, Bates SE.

Cancer Res. 1999 Dec 1;59(23):5938-46.

47.

DNA protein cross-links produced by NSC 652287, a novel thiophene derivative active against human renal cancer cells.

Nieves-Neira W, Rivera MI, Kohlhagen G, Hursey ML, Pourquier P, Sausville EA, Pommier Y.

Mol Pharmacol. 1999 Sep;56(3):478-84.

PMID:
10462535
48.

Topoisomerase poisoning activity of novel disaccharide anthracyclines.

Guano F, Pourquier P, Tinelli S, Binaschi M, Bigioni M, Animati F, Manzini S, Zunino F, Kohlhagen G, Pommier Y, Capranico G.

Mol Pharmacol. 1999 Jul;56(1):77-84.

PMID:
10385686
49.

Poisoning of human DNA topoisomerase I by ecteinascidin 743, an anticancer drug that selectively alkylates DNA in the minor groove.

Takebayashi Y, Pourquier P, Yoshida A, Kohlhagen G, Pommier Y.

Proc Natl Acad Sci U S A. 1999 Jun 22;96(13):7196-201.

50.

The ras oncogene-mediated sensitization of human cells to topoisomerase II inhibitor-induced apoptosis.

Koo HM, Gray-Goodrich M, Kohlhagen G, McWilliams MJ, Jeffers M, Vaigro-Wolff A, Alvord WG, Monks A, Paull KD, Pommier Y, Vande Woude GF.

J Natl Cancer Inst. 1999 Feb 3;91(3):236-44.

PMID:
10037101

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