-
1
-
-
0025805633
-
Identification of the hepatocyte growth factor receptor as the c-met proto-oncogene product
-
(a) Bottaro, D. P.; Rubin, J. S.; Faletto, D. L.; Chan, A. M.; Kmiecik, T. E.; Vande Woude, G. F.; Aaronson, S. A. Identification of the hepatocyte growth factor receptor as the c-met proto-oncogene product. Science 1991, 251, 802-804.
-
(1991)
Science
, vol.251
, pp. 802-804
-
-
Bottaro, D.P.1
Rubin, J.S.2
Faletto, D.L.3
Chan, A.M.4
Kmiecik, T.E.5
Vande Woude, G.F.6
Aaronson, S.A.7
-
2
-
-
0025771101
-
Scatter factor and hepatocyte growth factor are indistinguishable ligands for the MET receptor
-
(b) Naldini, L.; Weidner, K. M.; Vigna, E.; Gaudino, G.; Bardelli, A.; Ponzetto, C.; Narsimhan, R. P.; Hartmann, G.; Zarnegar, R.; Michalopoulos, G. K. Scatter factor and hepatocyte growth factor are indistinguishable ligands for the MET receptor. EMBO J. 1991, 10, 2867-2878.
-
(1991)
EMBO J
, vol.10
, pp. 2867-2878
-
-
Naldini, L.1
Weidner, K.M.2
Vigna, E.3
Gaudino, G.4
Bardelli, A.5
Ponzetto, C.6
Narsimhan, R.P.7
Hartmann, G.8
Zarnegar, R.9
Michalopoulos, G.K.10
-
3
-
-
33847390775
-
c-Met and hepatocyte growth factor: Potential as novel targets in cancer therapy
-
(a) Sattler, M.; Salgia, R. c-Met and hepatocyte growth factor: potential as novel targets in cancer therapy. Curr. Oncol. Rep. 2007, 9, 102-108.
-
(2007)
Curr. Oncol. Rep
, vol.9
, pp. 102-108
-
-
Sattler, M.1
Salgia, R.2
-
4
-
-
33749367676
-
The Met pathway: Master switch and drug target in cancer progression
-
(b) Mazzone, M.; Comoglio, P. M. The Met pathway: master switch and drug target in cancer progression. FASEB J. 2006, 20, 1611-1621.
-
(2006)
FASEB J
, vol.20
, pp. 1611-1621
-
-
Mazzone, M.1
Comoglio, P.M.2
-
5
-
-
0036551486
-
Scatter-factor and semaphorin receptors: Cell signaling for invasive growth
-
(c) Trusolino, L.; Comoglio, P. M. Scatter-factor and semaphorin receptors: cell signaling for invasive growth. Nat. Rev. Cancer 2002, 2, 289-300.
-
(2002)
Nat. Rev. Cancer
, vol.2
, pp. 289-300
-
-
Trusolino, L.1
Comoglio, P.M.2
-
6
-
-
33947104149
-
One pill, many uses
-
(a) Jarvis, L. M. One pill, many uses. Chem. Eng. News 2007, 85, 15-23.
-
(2007)
Chem. Eng. News
, vol.85
, pp. 15-23
-
-
Jarvis, L.M.1
-
7
-
-
19544389146
-
c-Met as a target for human cancer and characterization of inhibitors for therapeutic intervention
-
(b) Christensen, J.; Burrows, J.; Salgia, R. c-Met as a target for human cancer and characterization of inhibitors for therapeutic intervention. Cancer Lett 2005, 225, 1-25.
-
(2005)
Cancer Lett
, vol.225
, pp. 1-25
-
-
Christensen, J.1
Burrows, J.2
Salgia, R.3
-
8
-
-
33845299864
-
HGF- and c-Met-targeted drugs: Hopes, challenges and their future in cancer therapy
-
(c) Dussault, I.; Kaplan-Lefko, P.; Jun, T.; Coxon, A.; Burgess, T. L. HGF- and c-Met-targeted drugs: hopes, challenges and their future in cancer therapy. Drugs Future 2006, 31, 819-825.
-
(2006)
Drugs Future
, vol.31
, pp. 819-825
-
-
Dussault, I.1
Kaplan-Lefko, P.2
Jun, T.3
Coxon, A.4
Burgess, T.L.5
-
9
-
-
34248681295
-
Review of clinical trials: Agents targeting c-Met
-
(d) Abidoye, O.; Murukurthy, N.; Salgia, R. Review of clinical trials: agents targeting c-Met. Rev. Recent Clin. Trials 2007, 2, 143-147.
-
(2007)
Rev. Recent Clin. Trials
, vol.2
, pp. 143-147
-
-
Abidoye, O.1
Murukurthy, N.2
Salgia, R.3
-
10
-
-
0141481285
-
A novel small molecule met inhibitor induces apoptosis in cells transformed by the oncogenic TPR-MET tyrosine kinase
-
(a) Sattler, M.; Pride, Y. B.; Ma, P.; Gramlich, J. L.; Chu, S. C.; Quinnan, L. A.; Shirazian, S.; Liang, C.; Podar, K.; Christensen, J. G.; Salgia, R. A novel small molecule met inhibitor induces apoptosis in cells transformed by the oncogenic TPR-MET tyrosine kinase. Cancer Res. 2003, 63, 5462-5469.
-
(2003)
Cancer Res
, vol.63
, pp. 5462-5469
-
-
Sattler, M.1
Pride, Y.B.2
Ma, P.3
Gramlich, J.L.4
Chu, S.C.5
Quinnan, L.A.6
Shirazian, S.7
Liang, C.8
Podar, K.9
Christensen, J.G.10
Salgia, R.11
-
11
-
-
10744228765
-
-
Christensen, J. G.; Schreck, R.; Burrows., J.; Kuruganti, P.; Chan, E.; Le, P.; Chen, J.; Wang, X.; Ruslim, L.; Blake, R.; Lipson, K. E.; Ramphal, J.; Do S Cui, J. J.; Cherrington, J. M.; Mendel, D. B. A selective small molecule inhibitor of c-Met kinase inhibits c-Met-dependent phenotypes in vitro and exhibits cytoreductive antitumor activity in vivo. Cancer Res. 2003, 63, 7345-7355.
-
(b) Christensen, J. G.; Schreck, R.; Burrows., J.; Kuruganti, P.; Chan, E.; Le, P.; Chen, J.; Wang, X.; Ruslim, L.; Blake, R.; Lipson, K. E.; Ramphal, J.; Do S Cui, J. J.; Cherrington, J. M.; Mendel, D. B. A selective small molecule inhibitor of c-Met kinase inhibits c-Met-dependent phenotypes in vitro and exhibits cytoreductive antitumor activity in vivo. Cancer Res. 2003, 63, 7345-7355.
-
-
-
-
12
-
-
34249324494
-
An orally available small-molecule inhibitor of c-Met, PF-2341066, exhibits cytoreductive antitumor efficacy through antiproliferative and antiangiogenic mechanisms
-
Zou, H. Y.; Li, Q.; Lee. J. H.; Arango, M. E.; McDonnell, S. R.; Yamazaki, S.; Koudriakova, T. B.; Alton, G.; Cui, J. J.; Kung, P. P.; Nambu, M. D.; Los, G.; Bender, S. L.; Mroczkowski, B.; Christensen, J. G. An orally available small-molecule inhibitor of c-Met, PF-2341066, exhibits cytoreductive antitumor efficacy through antiproliferative and antiangiogenic mechanisms. Cancer Res. 2007, 67, 4408-4417.
-
(2007)
Cancer Res
, vol.67
, pp. 4408-4417
-
-
Zou, H.Y.1
Li, Q.2
Lee, J.H.3
Arango, M.E.4
McDonnell, S.R.5
Yamazaki, S.6
Koudriakova, T.B.7
Alton, G.8
Cui, J.J.9
Kung, P.P.10
Nambu, M.D.11
Los, G.12
Bender, S.L.13
Mroczkowski, B.14
Christensen, J.G.15
-
13
-
-
46849122987
-
Discovery of AMG 458: An Orally Bioavailable, Selective c-Met Inhibitor
-
For a preliminary discussion on the aspect of structural based design leading to 17, see the following:, Presented at the, San Diego, CA, April 12-16
-
For a preliminary discussion on the aspect of structural based design leading to 17, see the following: Choquette, D.; Liu, L. ; Kim, T.-S.; Norman, M. H.; Siegmund, A.; Xi, N.; Bellon, S. F.; Kaplan-Lefko, P.; Lee, M.; Lin, J.; Rex, K.; Teffera, Y.; Dussault, I.; Harmange, J. C. Discovery of AMG 458: An Orally Bioavailable, Selective c-Met Inhibitor. Presented at the AACR Annual Meeting, San Diego, CA, April 12-16, 2008.
-
(2008)
AACR Annual Meeting
-
-
Choquette, D.1
Liu, L.2
Kim, T.-S.3
Norman, M.H.4
Siegmund, A.5
Xi, N.6
Bellon, S.F.7
Kaplan-Lefko, P.8
Lee, M.9
Lin, J.10
Rex, K.11
Teffera, Y.12
Dussault, I.13
Harmange, J.C.14
-
14
-
-
84946565545
-
-
The discovery and detailed SAR studies of 1 will be reported in a separate publication, to be submitted
-
(a) The discovery and detailed SAR studies of 1 will be reported in a separate publication. J. Med. Chem., to be submitted.
-
J. Med. Chem
-
-
-
15
-
-
46849096820
-
-
For the synthesis and nomenclature of the pyrazolone piece leading to 4 and 5, see ref 10 and ref 16 therein
-
(b) For the synthesis and nomenclature of the pyrazolone piece leading to 4 and 5, see ref 10 (and ref 16 therein).
-
-
-
-
16
-
-
33751413349
-
A review of the latest clinical compounds to inhibit VEGF in pathological angiogenesis
-
(a) Baka, S.; Clamp, A. R.; Jayson, G. C. A review of the latest clinical compounds to inhibit VEGF in pathological angiogenesis. Expert Opin. Ther. Targets 2006, 10, 867-876.
-
(2006)
Expert Opin. Ther. Targets
, vol.10
, pp. 867-876
-
-
Baka, S.1
Clamp, A.R.2
Jayson, G.C.3
-
17
-
-
28444476260
-
Angiogenic inhibitors: A new therapeutic strategy in oncology
-
(b) Gasparini, G.; Longo, R.; Toi, M.; Ferrara, N. Angiogenic inhibitors: a new therapeutic strategy in oncology. Nat. Clin. Pract. Oncol. 2005, 2, 562-577.
-
(2005)
Nat. Clin. Pract. Oncol
, vol.2
, pp. 562-577
-
-
Gasparini, G.1
Longo, R.2
Toi, M.3
Ferrara, N.4
-
18
-
-
46849099300
-
-
Other strategies to address the issue of ketone formation such as protecting the OH group as methyl ether, or introducing alkyl groups flanking the OH group, were less successful
-
Other strategies to address the issue of ketone formation such as protecting the OH group as methyl ether, or introducing alkyl groups flanking the OH group, were less successful.
-
-
-
-
19
-
-
42949126801
-
Selective μ-hydroxyethylation at the N-1 position of a pyrazolone: Synthesis of benzyl 1-(μ-hydroxyethyl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H- pyrazole-4-carboxylate
-
Siegmund, A.; Retz, D.; Xi, N.; Dominguez, C.; Bürli, R.; Liu, L. Selective μ-hydroxyethylation at the N-1 position of a pyrazolone: synthesis of benzyl 1-(μ-hydroxyethyl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H- pyrazole-4-carboxylate. Synlett. 2008, 1005-1008.
-
(2008)
Synlett
, pp. 1005-1008
-
-
Siegmund, A.1
Retz, D.2
Xi, N.3
Dominguez, C.4
Bürli, R.5
Liu, L.6
-
20
-
-
84993911722
-
4-Alkoxycarbonyl, 4-alkylthiocarbonyl and 5-alkoxycarbonyloxy derivatives of 1-substituted-3-methylpyrazol-5-ones
-
Lopez, R.; Leon, G.; Oliva, A. 4-Alkoxycarbonyl, 4-alkylthiocarbonyl and 5-alkoxycarbonyloxy derivatives of 1-substituted-3-methylpyrazol-5-ones. J. Heterocycl. Chem. 1995, 32, 1377-1379.
-
(1995)
J. Heterocycl. Chem
, vol.32
, pp. 1377-1379
-
-
Lopez, R.1
Leon, G.2
Oliva, A.3
-
21
-
-
84872622570
-
Synthesis of some chloromethoxyquinolines
-
Lauer, W. M.; Arnold, R. T.; Tiffany, B.; Tinker, J. Synthesis of some chloromethoxyquinolines. J. Am. Chem. Soc. 1946, 68, 1268-1269.
-
(1946)
J. Am. Chem. Soc
, vol.68
, pp. 1268-1269
-
-
Lauer, W.M.1
Arnold, R.T.2
Tiffany, B.3
Tinker, J.4
-
22
-
-
0020325715
-
Metabolic activation and drug toxicity
-
Nelson, S. D. Metabolic activation and drug toxicity. J. Med. Chem. 1982, 25, 753-765.
-
(1982)
J. Med. Chem
, vol.25
, pp. 753-765
-
-
Nelson, S.D.1
-
24
-
-
33644872197
-
Structural characterization of autoinhibited c-Met kinase produced by coexpression in bacteria with phosphatase
-
Wang, W.; Marimuthu, A.; Tsai, J.; Kumar, A.; Krupka, H. I.; Zhang, C.; Powell, B.; Suzuki, Y.; Nguyen, H.; Tabrizizad, M.; Luu, C.; West, B. L. Structural characterization of autoinhibited c-Met kinase produced by coexpression in bacteria with phosphatase. Proc. Natl. Acad. Sci. U.S.A. 2006, 103, 3563-3568.
-
(2006)
Proc. Natl. Acad. Sci. U.S.A
, vol.103
, pp. 3563-3568
-
-
Wang, W.1
Marimuthu, A.2
Tsai, J.3
Kumar, A.4
Krupka, H.I.5
Zhang, C.6
Powell, B.7
Suzuki, Y.8
Nguyen, H.9
Tabrizizad, M.10
Luu, C.11
West, B.L.12
-
25
-
-
0344921400
-
-
50 = 8 nM). RON has also been implicated in human cancers. (a) Danilkovitch-Miagkova, A.; Duh, F. M.; Kuzmin, I.; Angeloni, D.; Liu, S. L.; Miller, A. D.; Lerman, M. I. Hyaluronidase-2 negatively regulates RON receptor tyrosine kinase and mediates transformation of epithelial cells by jaagsiekte sheep retrovirus. Proc. Natl. Acad. Sci. U.S.A. 2003, 100, 4580-4585.
-
50 = 8 nM). RON has also been implicated in human cancers. (a) Danilkovitch-Miagkova, A.; Duh, F. M.; Kuzmin, I.; Angeloni, D.; Liu, S. L.; Miller, A. D.; Lerman, M. I. Hyaluronidase-2 negatively regulates RON receptor tyrosine kinase and mediates transformation of epithelial cells by jaagsiekte sheep retrovirus. Proc. Natl. Acad. Sci. U.S.A. 2003, 100, 4580-4585.
-
-
-
-
26
-
-
46849122366
-
-
50, nM): LCK (730), FES (706), BLK (519), Lyn (506), FLT3 (391), BMX (363), FGR (328), Aurora1(280), CFMS (238), CSK (165), PDGF (120), ITK (62).
-
50, nM): LCK (730), FES (706), BLK (519), Lyn (506), FLT3 (391), BMX (363), FGR (328), Aurora1(280), CFMS (238), CSK (165), PDGF (120), ITK (62).
-
-
-
-
27
-
-
46849093963
-
-
-6 cm/s; Papp(B-A)/Papp(A-B): 0.8.
-
-6 cm/s; Papp(B-A)/Papp(A-B): 0.8.
-
-
-
-
28
-
-
0022472582
-
Mechanism of met oncogene activation
-
Park, M.; Dean, M.; Cooper, C. S.; Schmidt, M.; O'Brien, S. J.; Blaire, D. G.; Vande Woude, G. F. Mechanism of met oncogene activation. Cell 1986, 45, 895-904.
-
(1986)
Cell
, vol.45
, pp. 895-904
-
-
Park, M.1
Dean, M.2
Cooper, C.S.3
Schmidt, M.4
O'Brien, S.J.5
Blaire, D.G.6
Vande Woude, G.F.7
-
29
-
-
0030690583
-
Met and hepatocyte growth factor/scatter factor expression in human gliomas
-
(a) Koochekpour, S.; Jeffers, M.; Rulong, S.; Taylor, G.; Klineberg, E.; Hudson, E. A.; Resau, J. H.; Vande Woude, G. F. Met and hepatocyte growth factor/scatter factor expression in human gliomas. Cancer Res. 1997, 57, 5391-5398.
-
(1997)
Cancer Res
, vol.57
, pp. 5391-5398
-
-
Koochekpour, S.1
Jeffers, M.2
Rulong, S.3
Taylor, G.4
Klineberg, E.5
Hudson, E.A.6
Resau, J.H.7
Vande Woude, G.F.8
-
30
-
-
34547881522
-
Quantitative analysis of EGFRvIII cellular signaling networks reveals a combinatorial therapeutic strategy for glioblastoma
-
(b) Huang, P. H.; Mukasa, A.; Bonavia, R.; Flynn, R. A.: Brewer, Z. E.; Cavenee, W. K.; Furnari, F. B.; White, F. M. Quantitative analysis of EGFRvIII cellular signaling networks reveals a combinatorial therapeutic strategy for glioblastoma. Proc. Natl. Acad. Sci. U.S.A. 2007, 104, 12867-12872.
-
(2007)
Proc. Natl. Acad. Sci. U.S.A
, vol.104
, pp. 12867-12872
-
-
Huang, P.H.1
Mukasa, A.2
Bonavia, R.3
Flynn, R.A.4
Brewer, Z.E.5
Cavenee, W.K.6
Furnari, F.B.7
White, F.M.8
|