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Items: 1 to 20 of 107

1.

1,2,3-Triazole-containing uracil derivatives with excellent pharmacokinetics as a novel class of potent human deoxyuridine triphosphatase inhibitors.

Miyakoshi H, Miyahara S, Yokogawa T, Endoh K, Muto T, Yano W, Wakasa T, Ueno H, Chong KT, Taguchi J, Nomura M, Takao Y, Fujioka A, Hashimoto A, Itou K, Yamamura K, Shuto S, Nagasawa H, Fukuoka M.

J Med Chem. 2012 Jul 26;55(14):6427-37. doi: 10.1021/jm3004174. Epub 2012 Jul 3.

PMID:
22715973
2.

Discovery of a novel class of potent human deoxyuridine triphosphatase inhibitors remarkably enhancing the antitumor activity of thymidylate synthase inhibitors.

Miyahara S, Miyakoshi H, Yokogawa T, Chong KT, Taguchi J, Muto T, Endoh K, Yano W, Wakasa T, Ueno H, Takao Y, Fujioka A, Hashimoto A, Itou K, Yamamura K, Nomura M, Nagasawa H, Shuto S, Fukuoka M.

J Med Chem. 2012 Apr 12;55(7):2970-80. doi: 10.1021/jm201628y. Epub 2012 Mar 26.

PMID:
22339362
3.

Synthesis and discovery of N-carbonylpyrrolidine- or N-sulfonylpyrrolidine-containing uracil derivatives as potent human deoxyuridine triphosphatase inhibitors.

Miyakoshi H, Miyahara S, Yokogawa T, Chong KT, Taguchi J, Endoh K, Yano W, Wakasa T, Ueno H, Takao Y, Nomura M, Shuto S, Nagasawa H, Fukuoka M.

J Med Chem. 2012 Apr 12;55(7):2960-9. doi: 10.1021/jm201627n. Epub 2012 Mar 26.

PMID:
22404301
4.

Discovery of highly potent human deoxyuridine triphosphatase inhibitors based on the conformation restriction strategy.

Miyahara S, Miyakoshi H, Yokogawa T, Chong KT, Taguchi J, Muto T, Endoh K, Yano W, Wakasa T, Ueno H, Takao Y, Fujioka A, Hashimoto A, Itou K, Yamamura K, Nomura M, Nagasawa H, Shuto S, Fukuoka M.

J Med Chem. 2012 Jun 14;55(11):5483-96. doi: 10.1021/jm300416h. Epub 2012 May 30.

PMID:
22607122
6.

Design, synthesis and evaluation of novel uracil acetamide derivatives as potential inhibitors of Plasmodium falciparum dUTP nucleotidohydrolase.

McCarthy O, Musso-Buendia A, Kaiser M, Brun R, Ruiz-Perez LM, Johansson NG, Pacanowska DG, Gilbert IH.

Eur J Med Chem. 2009 Feb;44(2):678-88. doi: 10.1016/j.ejmech.2008.05.018. Epub 2008 Jul 10.

PMID:
18619713
7.

Synthesis and evaluation of 6-methylene-bridged uracil derivatives. Part 1: discovery of novel orally active inhibitors of human thymidine phosphorylase.

Yano S, Kazuno H, Suzuki N, Emura T, Wierzba K, Yamashita J, Tada Y, Yamada Y, Fukushima M, Asao T.

Bioorg Med Chem. 2004 Jul 1;12(13):3431-41.

PMID:
15186829
8.
9.

Design and synthesis of novel 5,6-disubstituted uracil derivatives as potent inhibitors of thymidine phosphorylase.

Nencka R, Votruba I, Hrebabecký H, Tloust'ová E, Horská K, Masojídková M, Holý A.

Bioorg Med Chem Lett. 2006 Mar 1;16(5):1335-7. Epub 2005 Dec 5.

PMID:
16337119
10.

The role of dUTPase and uracil-DNA repair in cancer chemotherapy.

Ladner RD.

Curr Protein Pept Sci. 2001 Dec;2(4):361-70. Review.

PMID:
12374095
11.

Deoxyuridine triphosphatase (dUTPase) expression and sensitivity to the thymidylate synthase (TS) inhibitor ZD9331.

Webley SD, Hardcastle A, Ladner RD, Jackman AL, Aherne GW.

Br J Cancer. 2000 Sep;83(6):792-9.

12.

Modified 5'-trityl nucleosides as inhibitors of Plasmodium falciparum dUTPase.

Ruda GF, Nguyen C, Ziemkowski P, Felczak K, Kasinathan G, Musso-Buendia A, Sund C, Zhou XX, Kaiser M, Ruiz-Pérez LM, Brun R, Kulikowski T, Johansson NG, González-Pacanowska D, Gilbert IH.

ChemMedChem. 2011 Feb 7;6(2):309-20. doi: 10.1002/cmdc.201000445. Epub 2011 Jan 18.

PMID:
21246738
13.

Synthesis and antitumor activity of 1,2,4-triazoles having 1,4-benzodioxan fragment as a novel class of potent methionine aminopeptidase type II inhibitors.

Hou YP, Sun J, Pang ZH, Lv PC, Li DD, Yan L, Zhang HJ, Zheng EX, Zhao J, Zhu HL.

Bioorg Med Chem. 2011 Oct 15;19(20):5948-54. doi: 10.1016/j.bmc.2011.08.063. Epub 2011 Sep 1.

PMID:
21925884
14.

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
15.

Structure-based design and subsequent optimization of 2-tolyl-(1,2,3-triazol-1-yl-4-carboxamide) inhibitors of p38 MAP kinase.

Cogan DA, Aungst R, Breinlinger EC, Fadra T, Goldberg DR, Hao MH, Kroe R, Moss N, Pargellis C, Qian KC, Swinamer AD.

Bioorg Med Chem Lett. 2008 Jun 1;18(11):3251-5. doi: 10.1016/j.bmcl.2008.04.043. Epub 2008 Apr 25.

PMID:
18462940
16.

5-Substituted N(4)-hydroxy-2'-deoxycytidines and their 5'-monophosphates: synthesis, conformation, interaction with tumor thymidylate synthase, and in vitro antitumor activity.

Felczak K, Miazga A, Poznański J, Bretner M, Kulikowski T, Dzik JM, Gołos B, Zieliński Z, Cieśla J, Rode W.

J Med Chem. 2000 Nov 30;43(24):4647-56.

PMID:
11101356
17.

Synthesis and evaluation of 6-methylene-bridged uracil derivatives. Part 2: optimization of inhibitors of human thymidine phosphorylase and their selectivity with uridine phosphorylase.

Yano S, Kazuno H, Sato T, Suzuki N, Emura T, Wierzba K, Yamashita J, Tada Y, Yamada Y, Fukushima M, Asao T.

Bioorg Med Chem. 2004 Jul 1;12(13):3443-50.

PMID:
15186830
18.

Structural basis and SAR for G007-LK, a lead stage 1,2,4-triazole based specific tankyrase 1/2 inhibitor.

Voronkov A, Holsworth DD, Waaler J, Wilson SR, Ekblad B, Perdreau-Dahl H, Dinh H, Drewes G, Hopf C, Morth JP, Krauss S.

J Med Chem. 2013 Apr 11;56(7):3012-23. doi: 10.1021/jm4000566. Epub 2013 Mar 29.

PMID:
23473363
19.

Novel amide derivatives as inhibitors of histone deacetylase: design, synthesis and SAR.

Andrianov V, Gailite V, Lola D, Loza E, Semenikhina V, Kalvinsh I, Finn P, Petersen KD, Ritchie JW, Khan N, Tumber A, Collins LS, Vadlamudi SM, Björkling F, Sehested M.

Eur J Med Chem. 2009 Mar;44(3):1067-85. doi: 10.1016/j.ejmech.2008.06.020. Epub 2008 Jun 27.

PMID:
18672316
20.

Design and synthesis of novel imidazole-substituted dipeptide amides as potent and selective inhibitors of Candida albicans myristoylCoA:protein N-myristoyltransferase and identification of related tripeptide inhibitors with mechanism-based antifungal activity.

Devadas B, Freeman SK, Zupec ME, Lu HF, Nagarajan SR, Kishore NS, Lodge JK, Kuneman DW, McWherter CA, Vinjamoori DV, Getman DP, Gordon JI, Sikorski JA.

J Med Chem. 1997 Aug 1;40(16):2609-25.

PMID:
9258368

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