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Items: 1 to 20 of 197

1.

4,5-Dihydro-1H-pyrazolo[4,3-h]quinazolines as potent and selective Polo-like kinase 1 (PLK1) inhibitors.

Beria I, Valsasina B, Brasca MG, Ceccarelli W, Colombo M, Cribioli S, Fachin G, Ferguson RD, Fiorentini F, Gianellini LM, Giorgini ML, Moll JK, Posteri H, Pezzetta D, Roletto F, Sola F, Tesei D, Caruso M.

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6489-94. doi: 10.1016/j.bmcl.2010.09.060. Epub 2010 Sep 17.

PMID:
20932759
2.

Identification of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as a new class of orally and selective Polo-like kinase 1 inhibitors.

Beria I, Ballinari D, Bertrand JA, Borghi D, Bossi RT, Brasca MG, Cappella P, Caruso M, Ceccarelli W, Ciavolella A, Cristiani C, Croci V, De Ponti A, Fachin G, Ferguson RD, Lansen J, Moll JK, Pesenti E, Posteri H, Perego R, Rocchetti M, Storici P, Volpi D, Valsasina B.

J Med Chem. 2010 May 13;53(9):3532-51. doi: 10.1021/jm901713n.

PMID:
20397705
3.

NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor.

Beria I, Bossi RT, Brasca MG, Caruso M, Ceccarelli W, Fachin G, Fasolini M, Forte B, Fiorentini F, Pesenti E, Pezzetta D, Posteri H, Scolaro A, Re Depaolini S, Valsasina B.

Bioorg Med Chem Lett. 2011 May 15;21(10):2969-74. doi: 10.1016/j.bmcl.2011.03.054. Epub 2011 Mar 21.

PMID:
21470862
4.

Imidazopyridine derivatives as potent and selective Polo-like kinase (PLK) inhibitors.

Sato Y, Onozaki Y, Sugimoto T, Kurihara H, Kamijo K, Kadowaki C, Tsujino T, Watanabe A, Otsuki S, Mitsuya M, Iida M, Haze K, Machida T, Nakatsuru Y, Komatani H, Kotani H, Iwasawa Y.

Bioorg Med Chem Lett. 2009 Aug 15;19(16):4673-8. doi: 10.1016/j.bmcl.2009.06.084. Epub 2009 Jun 25.

PMID:
19589677
5.

Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors.

Caldarelli M, Angiolini M, Disingrini T, Donati D, Guanci M, Nuvoloni S, Posteri H, Quartieri F, Silvagni M, Colombo R.

Bioorg Med Chem Lett. 2011 Aug 1;21(15):4507-11. doi: 10.1016/j.bmcl.2011.05.122. Epub 2011 Jun 14.

PMID:
21723120
6.

NMS-P937, an orally available, specific small-molecule polo-like kinase 1 inhibitor with antitumor activity in solid and hematologic malignancies.

Valsasina B, Beria I, Alli C, Alzani R, Avanzi N, Ballinari D, Cappella P, Caruso M, Casolaro A, Ciavolella A, Cucchi U, De Ponti A, Felder E, Fiorentini F, Galvani A, Gianellini LM, Giorgini ML, Isacchi A, Lansen J, Pesenti E, Rizzi S, Rocchetti M, Sola F, Moll J.

Mol Cancer Ther. 2012 Apr;11(4):1006-16. doi: 10.1158/1535-7163.MCT-11-0765. Epub 2012 Feb 7.

7.

Heteroaryl-linked 5-(1H-benzimidazol-1-yl)-2-thiophenecarboxamides: potent inhibitors of polo-like kinase 1 (PLK1) with improved drug-like properties.

Rheault TR, Donaldson KH, Badiang-Alberti JG, Davis-Ward RG, Andrews CW, Bambal R, Jackson JR, Cheung M.

Bioorg Med Chem Lett. 2010 Aug 1;20(15):4587-92. doi: 10.1016/j.bmcl.2010.06.009. Epub 2010 Jun 8.

PMID:
20594842
8.

TAK-960, a novel, orally available, selective inhibitor of polo-like kinase 1, shows broad-spectrum preclinical antitumor activity in multiple dosing regimens.

Hikichi Y, Honda K, Hikami K, Miyashita H, Kaieda I, Murai S, Uchiyama N, Hasegawa M, Kawamoto T, Sato T, Ichikawa T, Cao S, Nie Z, Zhang L, Yang J, Kuida K, Kupperman E.

Mol Cancer Ther. 2012 Mar;11(3):700-9. doi: 10.1158/1535-7163.MCT-11-0762. Epub 2011 Dec 21.

9.

Identification of novel, potent and selective inhibitors of Polo-like kinase 1.

Chen S, Bartkovitz D, Cai J, Chen Y, Chen Z, Chu XJ, Le K, Le NT, Luk KC, Mischke S, Naderi-Oboodi G, Boylan JF, Nevins T, Qing W, Chen Y, Wovkulich PM.

Bioorg Med Chem Lett. 2012 Jan 15;22(2):1247-50. doi: 10.1016/j.bmcl.2011.11.052. Epub 2011 Dec 1.

PMID:
22172702
10.

SBE13 joins the family of Polo-like kinase 1 (Plk1) inhibitors.

Liu X.

Cell Cycle. 2010 Feb 1;9(3):445-6. Epub 2010 Feb 1. No abstract available.

PMID:
20130451
11.

A pan-specific inhibitor of the polo-box domains of polo-like kinases arrests cancer cells in mitosis.

Reindl W, Yuan J, Krämer A, Strebhardt K, Berg T.

Chembiochem. 2009 May 4;10(7):1145-8. doi: 10.1002/cbic.200900059.

PMID:
19350612
12.

Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding.

Emmitte KA, Adjabeng GM, Andrews CW, Alberti JG, Bambal R, Chamberlain SD, Davis-Ward RG, Dickson HD, Hassler DF, Hornberger KR, Jackson JR, Kuntz KW, Lansing TJ, Mook RA Jr, Nailor KE, Pobanz MA, Smith SC, Sung CM, Cheung M.

Bioorg Med Chem Lett. 2009 Mar 15;19(6):1694-7. doi: 10.1016/j.bmcl.2009.01.094. Epub 2009 Jan 31. Erratum in: Bioorg Med Chem Lett. 2009 May 1;19(9):2604. Adjebang, George M [corrected to Adjabeng, George M].

PMID:
19237286
13.

Distinct concentration-dependent effects of the polo-like kinase 1-specific inhibitor GSK461364A, including differential effect on apoptosis.

Gilmartin AG, Bleam MR, Richter MC, Erskine SG, Kruger RG, Madden L, Hassler DF, Smith GK, Gontarek RR, Courtney MP, Sutton D, Diamond MA, Jackson JR, Laquerre SG.

Cancer Res. 2009 Sep 1;69(17):6969-77. doi: 10.1158/0008-5472.CAN-09-0945. Epub 2009 Aug 18.

14.

Selectivity-determining residues in Plk1.

Kothe M, Kohls D, Low S, Coli R, Rennie GR, Feru F, Kuhn C, Ding YH.

Chem Biol Drug Des. 2007 Dec;70(6):540-6. Epub 2007 Nov 13.

PMID:
18005335
15.

Phosphopeptides with improved cellular uptake properties as ligands for the polo-box domain of polo-like kinase 1.

Richter S, Neundorf I, Loebner K, Gräber M, Berg T, Bergmann R, Steinbach J, Pietzsch J, Wuest F.

Bioorg Med Chem Lett. 2011 Aug 15;21(16):4686-9. doi: 10.1016/j.bmcl.2011.06.103. Epub 2011 Jun 30.

PMID:
21778054
16.

Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.

Zhang Q, Xia Z, Mitten MJ, Lasko LM, Klinghofer V, Bouska J, Johnson EF, Penning TD, Luo Y, Giranda VL, Shoemaker AR, Stewart KD, Djuric SW, Vasudevan A.

Bioorg Med Chem Lett. 2012 Dec 15;22(24):7615-22. doi: 10.1016/j.bmcl.2012.10.009. Epub 2012 Oct 11.

PMID:
23103095
17.

Small-molecular, non-peptide, non-ATP-competitive polo-like kinase 1 (Plk1) inhibitors with a terphenyl skeleton.

Mita Y, Noguchi-Yachide T, Ishikawa M, Hashimoto Y.

Bioorg Med Chem. 2013 Feb 1;21(3):608-17. doi: 10.1016/j.bmc.2012.11.054. Epub 2012 Dec 11.

PMID:
23276450
18.

Identification of novel polo-like kinase 1 inhibitors by a hybrid virtual screening.

Lu S, Sun SL, Liu HC, Chen YD, Yuan HL, Gao YP, Yang P, Lu T.

Chem Biol Drug Des. 2012 Aug;80(2):328-39. doi: 10.1111/j.1747-0285.2012.01412.x. Epub 2012 Jun 8.

PMID:
22583481
19.

Identification of 2-anilino-9-methoxy-5,7-dihydro-6H-pyrimido[5,4-d][1]benzazepin-6-ones as dual PLK1/VEGF-R2 kinase inhibitor chemotypes by structure-based lead generation.

Egert-Schmidt AM, Dreher J, Dunkel U, Kohfeld S, Preu L, Weber H, Ehlert JE, Mutschler B, Totzke F, Schächtele C, Kubbutat MH, Baumann K, Kunick C.

J Med Chem. 2010 Mar 25;53(6):2433-42. doi: 10.1021/jm901388c.

PMID:
20170163
20.

Inhibitors of Polo-like kinase reveal roles in spindle-pole maintenance.

McInnes C, Mazumdar A, Mezna M, Meades C, Midgley C, Scaerou F, Carpenter L, Mackenzie M, Taylor P, Walkinshaw M, Fischer PM, Glover D.

Nat Chem Biol. 2006 Nov;2(11):608-17. Epub 2006 Oct 8.

PMID:
17028581

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