-
1
-
-
75449116535
-
When analoging is not enough: Scaffold discovery in medicinal chemistry
-
H. Zhao I. Akritopoulou-Zanze When analoging is not enough: scaffold discovery in medicinal chemistry Expert Opin. Drug Discov. 5 2010 123 134
-
(2010)
Expert Opin. Drug Discov.
, vol.5
, pp. 123-134
-
-
Zhao, H.1
Akritopoulou-Zanze, I.2
-
4
-
-
79960422784
-
A diversity-oriented-synthesis protocol for scaffold discovery based on a general synthetic route to spirocycles
-
F.-A. Kang Z. Sui A diversity-oriented-synthesis protocol for scaffold discovery based on a general synthetic route to spirocycles Tetrahedron Lett. 52 2011 4204 4206
-
(2011)
Tetrahedron Lett.
, vol.52
, pp. 4204-4206
-
-
Kang, F.-A.1
Sui, Z.2
-
6
-
-
36749025633
-
Pyrrolidinyl-spirooxindole natural products as inspirations for the development of potential therapeutic agents
-
C.V. Galliford K.A. Scheidt Pyrrolidinyl-spirooxindole natural products as inspirations for the development of potential therapeutic agents Angew. Chem. Int. Ed. 46 2007 8748 8758
-
(2007)
Angew. Chem. Int. Ed.
, vol.46
, pp. 8748-8758
-
-
Galliford, C.V.1
Scheidt, K.A.2
-
7
-
-
84903246603
-
Spirooxindoles: Promising scaffolds for anticancer agents
-
B. Yu D.-Q. Yu H.-M. Liu Spirooxindoles: promising scaffolds for anticancer agents Eur. J. Med. Chem. 2015
-
(2015)
Eur. J. Med. Chem.
-
-
Yu, B.1
Yu, D.-Q.2
Liu, H.-M.3
-
8
-
-
84920814085
-
The discovery of polo-like kinase 4 inhibitors: Identification of (1 R,2 S)-2-(3-((E)-4-(((cis)-2,6-dimethylmorpholino)methyl)styryl)-1 H-indazol-6-yl)-5g 2-methoxyspiro[cyclopropane-1,3g 2-indolin]-2g 2-one (CFI-400945) as a potent, orally active antitumor agent
-
P.B. Sampson Y. Liu B. Forrest G. Cumming S.-W. Li N.K. Patel L. Edwards R. Laufer M. Feher F. Ban D.E. Awrey G. Mao O. Plotnikova R. Hodgson I. Beletskaya J.M. Mason X. Luo V. Nadeem X. Wei R. Kiarash B. Madeira P. Huang T.W. Mak G. Pan H.W. Pauls The discovery of polo-like kinase 4 inhibitors: identification of (1 R,2 S)-2-(3-((E)-4-(((cis)-2,6-dimethylmorpholino)methyl)styryl)-1 H-indazol-6-yl)-5g2-methoxyspiro[cyclopropane-1,3g2-indolin]-2g 2-one (CFI-400945) as a potent, orally active antitumor agent J. Med. Chem. 58 2015 147 169
-
(2015)
J. Med. Chem.
, vol.58
, pp. 147-169
-
-
Sampson, P.B.1
Liu, Y.2
Forrest, B.3
Cumming, G.4
Li, S.-W.5
Patel, N.K.6
Edwards, L.7
Laufer, R.8
Feher, M.9
Ban, F.10
Awrey, D.E.11
Mao, G.12
Plotnikova, O.13
Hodgson, R.14
Beletskaya, I.15
Mason, J.M.16
Luo, X.17
Nadeem, V.18
Wei, X.19
Kiarash, R.20
Madeira, B.21
Huang, P.22
Mak, T.W.23
Pan, G.24
Pauls, H.W.25
more..
-
9
-
-
0032535244
-
Polo-like kinases: A team that plays throughout mitosis
-
D.M. Glover I.M. Hagan Á.A.M. Tavares Polo-like kinases: a team that plays throughout mitosis Genes. Dev. 12 1998 3777 3787
-
(1998)
Genes. Dev.
, vol.12
, pp. 3777-3787
-
-
Glover, D.M.1
Hagan, I.M.2
Tavares Á., A.M.3
-
10
-
-
13244284602
-
Structure and function of polo-like kinases
-
D.M. Lowery D. Lim M.B. Yaffe Structure and function of polo-like kinases Oncogene 24 2005 248 259
-
(2005)
Oncogene
, vol.24
, pp. 248-259
-
-
Lowery, D.M.1
Lim, D.2
Yaffe, M.B.3
-
11
-
-
68049112546
-
Polo-like kinase (PLK) inhibitors in preclinical and early clinical development in oncology
-
P. Schöffski Polo-like kinase (PLK) inhibitors in preclinical and early clinical development in oncology Oncologist 14 2009 559 570
-
(2009)
Oncologist
, vol.14
, pp. 559-570
-
-
Schöffski, P.1
-
12
-
-
34548058372
-
Pharmacological and functional comparison of the polo-like kinase family:ginsight into inhibitor and substrate specificity
-
E.F. Johnson K.D. Stewart K.W. Woods V.L. Giranda Y. Luo Pharmacological and functional comparison of the polo-like kinase family:ginsight into inhibitor and substrate specificity Biochemistry 46 2007 9551 9563
-
(2007)
Biochemistry
, vol.46
, pp. 9551-9563
-
-
Johnson, E.F.1
Stewart, K.D.2
Woods, K.W.3
Giranda, V.L.4
Luo, Y.5
-
13
-
-
17144393305
-
Progress in the discovery of polo-like kinase inhibitors
-
C. McInnes M. Mezna P.M. Fischer Progress in the discovery of polo-like kinase inhibitors Curr. Top. Med. Chem. 5 2005 181 197
-
(2005)
Curr. Top. Med. Chem.
, vol.5
, pp. 181-197
-
-
McInnes, C.1
Mezna, M.2
Fischer, P.M.3
-
14
-
-
78649476052
-
Shared and separate functions of polo-like kinases and aurora kinases in cancer
-
S.M. Lens E.E. Voest R.H. Medema Shared and separate functions of polo-like kinases and aurora kinases in cancer Nat. Rev. Cancer 10 2010 825 841
-
(2010)
Nat. Rev. Cancer
, vol.10
, pp. 825-841
-
-
Lens, S.M.1
Voest, E.E.2
Medema, R.H.3
-
15
-
-
34249076619
-
Structure of the catalytic domain of human polo-like kinase 1
-
M. Kothe D. Kohls S. Low R. Coli A.C. Cheng S.L. Jacques T.L. Johnson C. Lewis C. Loh J. Nonomiya A.L. Sheils K.A. Verdries T.A. Wynn C. Kuhn Y.-H. Ding Structure of the catalytic domain of human polo-like kinase 1 Biochemistry 46 2007 5960 5971
-
(2007)
Biochemistry
, vol.46
, pp. 5960-5971
-
-
Kothe, M.1
Kohls, D.2
Low, S.3
Coli, R.4
Cheng, A.C.5
Jacques, S.L.6
Johnson, T.L.7
Lewis, C.8
Loh, C.9
Nonomiya, J.10
Sheils, A.L.11
Verdries, K.A.12
Wynn, T.A.13
Kuhn, C.14
Ding, Y.-H.15
-
16
-
-
84920828640
-
A new class of peptidomimetics targeting the polo-box domain of Polo-like kinase 1
-
M. Ahn Y.-H. Han J.-E. Park S. Kim W.C. Lee S.J. Lee P. Gunasekaran C. Cheong S.Y. Shin H.-Y. Kim E.K. Ryu R.N. Murugan N.-H. Kim J.K. Bang A new class of peptidomimetics targeting the polo-box domain of Polo-like kinase 1 J. Med. Chem. 58 2015 294 304
-
(2015)
J. Med. Chem.
, vol.58
, pp. 294-304
-
-
Ahn, M.1
Han, Y.-H.2
Park, J.-E.3
Kim, S.4
Lee, W.C.5
Lee, S.J.6
Gunasekaran, P.7
Cheong, C.8
Shin, S.Y.9
Kim, H.-Y.10
Ryu, E.K.11
Murugan, R.N.12
Kim, N.-H.13
Bang, J.K.14
-
17
-
-
84862967638
-
Discovery of a potent and orally bioavailable benzolactam-derived inhibitor of polo-like kinase 1 (MLN0905)
-
M.O. Duffey T.J. Vos R. Adams J. Alley J. Anthony C. Barrett I. Bharathan D. Bowman N.J. Bump R. Chau C. Cullis D.L. Driscoll A. Elder N. Forsyth J. Frazer J. Guo L. Guo M.L. Hyer D. Janowick B. Kulkarni S.-J. Lai K. Lasky G. Li J. Li D. Liao J. Little B. Peng M.G. Qian D.J. Reynolds M. Rezaei M.P. Scott T.B. Sells V. Shinde Q.J. Shi M.D. Sintchak F. Soucy K.T. Sprott S.G. Stroud M. Nestor I. Visiers G. Weatherhead Y. Ye N. D'Amore Discovery of a potent and orally bioavailable benzolactam-derived inhibitor of polo-like kinase 1 (MLN0905) J. Med. Chem. 55 2011 197 208
-
(2011)
J. Med. Chem.
, vol.55
, pp. 197-208
-
-
Duffey, M.O.1
Vos, T.J.2
Adams, R.3
Alley, J.4
Anthony, J.5
Barrett, C.6
Bharathan, I.7
Bowman, D.8
Bump, N.J.9
Chau, R.10
Cullis, C.11
Driscoll, D.L.12
Elder, A.13
Forsyth, N.14
Frazer, J.15
Guo, J.16
Guo, L.17
Hyer, M.L.18
Janowick, D.19
Kulkarni, B.20
Lai, S.-J.21
Lasky, K.22
Li, G.23
Li, J.24
Liao, D.25
Little, J.26
Peng, B.27
Qian, M.G.28
Reynolds, D.J.29
Rezaei, M.30
Scott, M.P.31
Sells, T.B.32
Shinde, V.33
Shi, Q.J.34
Sintchak, M.D.35
Soucy, F.36
Sprott, K.T.37
Stroud, S.G.38
Nestor, M.39
Visiers, I.40
Weatherhead, G.41
Ye, Y.42
D'Amore, N.43
more..
-
19
-
-
77951027070
-
Plk4 is required for cytokinesis and maintenance of chromosomal stability
-
C.O. Rosario M.A. Ko Y.Z. Haffani R.A. Gladdy J. Paderova A. Pollett J.A. Squire J.W. Dennis C.J. Swallow Plk4 is required for cytokinesis and maintenance of chromosomal stability Proc. Natl. Acad. Sci. USA. 107 2010 6888 6893
-
(2010)
Proc. Natl. Acad. Sci. USA.
, vol.107
, pp. 6888-6893
-
-
Rosario, C.O.1
Ko, M.A.2
Haffani, Y.Z.3
Gladdy, R.A.4
Paderova, J.5
Pollett, A.6
Squire, J.A.7
Dennis, J.W.8
Swallow, C.J.9
-
21
-
-
77957154311
-
Polo-like kinase 4: The odd one out of the family
-
J. Sillibourne M. Bornens Polo-like kinase 4: the odd one out of the family Cell. Div. 5 2010 25 33
-
(2010)
Cell. Div.
, vol.5
, pp. 25-33
-
-
Sillibourne, J.1
Bornens, M.2
-
22
-
-
29044431521
-
SAK/PLK4 is required for centriole duplication and flagella development
-
M. Bettencourt-Dias A. Rodrigues-Martins L. Carpenter M. Riparbelli L. Lehmann M. Gatt N. Carmo F. Balloux G. Callaini D. Glover SAK/PLK4 is required for centriole duplication and flagella development Curr. Biol. 15 2005 2199 2207
-
(2005)
Curr. Biol.
, vol.15
, pp. 2199-2207
-
-
Bettencourt-Dias, M.1
Rodrigues-Martins, A.2
Carpenter, L.3
Riparbelli, M.4
Lehmann, L.5
Gatt, M.6
Carmo, N.7
Balloux, F.8
Callaini, G.9
Glover, D.10
-
23
-
-
84881425734
-
The discovery of PLK4 inhibitors: (E)-3-((1 H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents
-
R. Laufer B. Forrest S.-W. Li Y. Liu P. Sampson L. Edwards Y. Lang D.E. Awrey G. Mao O. Plotnikova G. Leung R. Hodgson I. Beletskaya J.M. Mason X. Luo X. Wei Y. Yao M. Feher F. Ban R. Kiarash E. Green T.W. Mak G. Pan H.W. Pauls The discovery of PLK4 inhibitors: (E)-3-((1 H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents J. Med. Chem. 56 2013 6069 6087
-
(2013)
J. Med. Chem.
, vol.56
, pp. 6069-6087
-
-
Laufer, R.1
Forrest, B.2
Li, S.-W.3
Liu, Y.4
Sampson, P.5
Edwards, L.6
Lang, Y.7
Awrey, D.E.8
Mao, G.9
Plotnikova, O.10
Leung, G.11
Hodgson, R.12
Beletskaya, I.13
Mason, J.M.14
Luo, X.15
Wei, X.16
Yao, Y.17
Feher, M.18
Ban, F.19
Kiarash, R.20
Green, E.21
Mak, T.W.22
Pan, G.23
Pauls, H.W.24
more..
-
24
-
-
84986880911
-
Cancer: PLK4 inhibitor shows potent antitumour activity
-
A. Flemming Cancer: PLK4 inhibitor shows potent antitumour activity Nat. Rev. Drug. Discov. 13 2014 654
-
(2014)
Nat. Rev. Drug. Discov.
, vol.13
, pp. 654
-
-
Flemming, A.1
-
25
-
-
84905709109
-
Functional characterization of CFI-400945, a Polo-like kinase 4 inhibitor, as a potential anticancer agent
-
Jacqueline M. Mason Dan C.-C. Lin X. Wei Y. Che Y. Yao R. Kiarash David W. Cescon Graham C. Fletcher Donald E. Awrey Mark R. Bray G. Pan Tak W. Mak Functional characterization of CFI-400945, a Polo-like kinase 4 inhibitor, as a potential anticancer agent Cancer Cell. 26 2014 163 176
-
(2014)
Cancer Cell.
, vol.26
, pp. 163-176
-
-
Mason, J.M.1
Lin, D.C.-C.2
Wei, X.3
Che, Y.4
Yao, Y.5
Kiarash, R.6
Cescon, D.W.7
Fletcher, G.C.8
Awrey, D.E.9
Bray, M.R.10
Pan, G.11
Mak, T.W.12
-
26
-
-
80155186763
-
The protein phosphatase 2A regulatory subunit twins stabilizes Plk4 to induce centriole amplification
-
C.W. Brownlee J.E. Klebba D.W. Buster G.C. Rogers The protein phosphatase 2A regulatory subunit twins stabilizes Plk4 to induce centriole amplification J. Cell. Biol. 195 2011 231 243
-
(2011)
J. Cell. Biol.
, vol.195
, pp. 231-243
-
-
Brownlee, C.W.1
Klebba, J.E.2
Buster, D.W.3
Rogers, G.C.4
-
27
-
-
79960990834
-
The SCF-FBXW5 E3-ubiquitin ligase is regulated by PLK4 and targets HsSAS-6 to control centrosome duplication
-
A. Puklowski Y. Homsi D. Keller M. May S. Chauhan U. Kossatz V. Grunwald S. Kubicka A. Pich M.P. Manns I. Hoffmann P. Gonczy N.P. Malek The SCF-FBXW5 E3-ubiquitin ligase is regulated by PLK4 and targets HsSAS-6 to control centrosome duplication Nat. Cell. Biol. 13 2011 1004 1009
-
(2011)
Nat. Cell. Biol.
, vol.13
, pp. 1004-1009
-
-
Puklowski, A.1
Homsi, Y.2
Keller, D.3
May, M.4
Chauhan, S.5
Kossatz, U.6
Grunwald, V.7
Kubicka, S.8
Pich, A.9
Manns, M.P.10
Hoffmann, I.11
Gonczy, P.12
Malek, N.P.13
-
28
-
-
76149140089
-
Polo-like kinase 4 kinase activity limits centrosome overduplication by autoregulating its own stability
-
A. Holland W. Lan S. Niessen H. Hoover D. Cleveland Polo-like kinase 4 kinase activity limits centrosome overduplication by autoregulating its own stability J. Cell. Biol. 188 2010 191 198
-
(2010)
J. Cell. Biol.
, vol.188
, pp. 191-198
-
-
Holland, A.1
Lan, W.2
Niessen, S.3
Hoover, H.4
Cleveland, D.5
-
29
-
-
85042974880
-
-
For more information about clinical trials of CFI-400945 fumarate, please refer to the National Cancer Institute website.
-
For more information about clinical trials of CFI-400945 fumarate, please refer to the National Cancer Institute website (http://www.cancer.gov/drugdictionary?cdridCombining double low line754001).
-
-
-
-
30
-
-
84984910848
-
The discovery of Polo-like kinase 4 inhibitors: Design and optimization of spiro[cyclopropane-1,3g2[3 H[indol]-2g2(12 H)-ones as orally bioavailable antitumor agents
-
P.B. Sampson Y. Liu N.K. Patel M. Feher B. Forrest S.-W. Li L. Edwards R. Laufer Y. Lang F. Ban D.E. Awrey G. Mao O. Plotnikova G. Leung R. Hodgson J. Mason X. Wei R. Kiarash E. Green W. Qiu N.Y. Chirgadze T.W. Mak G. Pan H.W. Pauls The discovery of Polo-like kinase 4 inhibitors: design and optimization of spiro[cyclopropane-1,32[3 H[indol]-22(12 H)-ones as orally bioavailable antitumor agents J. Med. Chem. 58 2015 130 146
-
(2015)
J. Med. Chem.
, vol.58
, pp. 130-146
-
-
Sampson, P.B.1
Liu, Y.2
Patel, N.K.3
Feher, M.4
Forrest, B.5
Li, S.-W.6
Edwards, L.7
Laufer, R.8
Lang, Y.9
Ban, F.10
Awrey, D.E.11
Mao, G.12
Plotnikova, O.13
Leung, G.14
Hodgson, R.15
Mason, J.16
Wei, X.17
Kiarash, R.18
Green, E.19
Qiu, W.20
Chirgadze, N.Y.21
Mak, T.W.22
Pan, G.23
Pauls, H.W.24
more..
-
31
-
-
84862583428
-
Recent advances in the total synthesis of cyclopropane-containing natural products
-
D.Y.K. Chen R.H. Pouwer J.-A. Richard Recent advances in the total synthesis of cyclopropane-containing natural products Chem. Soc. Rev. 41 2012 4631 4642
-
(2012)
Chem. Soc. Rev.
, vol.41
, pp. 4631-4642
-
-
Chen, D.Y.K.1
Pouwer, R.H.2
Richard, J.-A.3
-
33
-
-
84905690496
-
Polo-like kinase 4 inhibition: A strategy for cancer therapy?
-
Andrew J. Holland Don W. Cleveland Polo-like kinase 4 inhibition: a strategy for cancer therapy? Cancer Cell. 26 2014 151 153
-
(2014)
Cancer Cell.
, vol.26
, pp. 151-153
-
-
Holland, A.J.1
Cleveland, D.W.2
-
34
-
-
33748331308
-
The mighty mouse: Genetically engineered mouse models in cancer drug development
-
N.E. Sharpless R.A. DePinho The mighty mouse: genetically engineered mouse models in cancer drug development Nat. Rev. Drug. Discov. 5 2006 741 754
-
(2006)
Nat. Rev. Drug. Discov.
, vol.5
, pp. 741-754
-
-
Sharpless, N.E.1
Depinho, R.A.2
|