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Items: 1 to 20 of 101

1.

The development of HKI-272 and related compounds for the treatment of cancer.

Wissner A, Mansour TS.

Arch Pharm (Weinheim). 2008 Aug;341(8):465-77. doi: 10.1002/ardp.200800009. Review.

PMID:
18493974
2.

Optimization of 6,7-disubstituted-4-(arylamino)quinoline-3-carbonitriles as orally active, irreversible inhibitors of human epidermal growth factor receptor-2 kinase activity.

Tsou HR, Overbeek-Klumpers EG, Hallett WA, Reich MF, Floyd MB, Johnson BD, Michalak RS, Nilakantan R, Discafani C, Golas J, Rabindran SK, Shen R, Shi X, Wang YF, Upeslacis J, Wissner A.

J Med Chem. 2005 Feb 24;48(4):1107-31.

PMID:
15715478
3.

Synthesis and structure-activity relationships of 6,7-disubstituted 4-anilinoquinoline-3-carbonitriles. The design of an orally active, irreversible inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) and the human epidermal growth factor receptor-2 (HER-2).

Wissner A, Overbeek E, Reich MF, Floyd MB, Johnson BD, Mamuya N, Rosfjord EC, Discafani C, Davis R, Shi X, Rabindran SK, Gruber BC, Ye F, Hallett WA, Nilakantan R, Shen R, Wang YF, Greenberger LM, Tsou HR.

J Med Chem. 2003 Jan 2;46(1):49-63.

PMID:
12502359
4.

Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase.

Rabindran SK, Discafani CM, Rosfjord EC, Baxter M, Floyd MB, Golas J, Hallett WA, Johnson BD, Nilakantan R, Overbeek E, Reich MF, Shen R, Shi X, Tsou HR, Wang YF, Wissner A.

Cancer Res. 2004 Jun 1;64(11):3958-65.

5.

Neratinib: an oral, irreversible dual EGFR/HER2 inhibitor for breast and non-small cell lung cancer.

Bose P, Ozer H.

Expert Opin Investig Drugs. 2009 Nov;18(11):1735-51. doi: 10.1517/13543780903305428. Review.

PMID:
19780706
6.

HKI-272 in non small cell lung cancer.

Wong KK.

Clin Cancer Res. 2007 Aug 1;13(15 Pt 2):s4593-6. Review.

7.

6-Substituted-4-(3-bromophenylamino)quinazolines as putative irreversible inhibitors of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor (HER-2) tyrosine kinases with enhanced antitumor activity.

Tsou HR, Mamuya N, Johnson BD, Reich MF, Gruber BC, Ye F, Nilakantan R, Shen R, Discafani C, DeBlanc R, Davis R, Koehn FE, Greenberger LM, Wang YF, Wissner A.

J Med Chem. 2001 Aug 16;44(17):2719-34.

PMID:
11495584
8.

The major lung cancer-derived mutants of ERBB2 are oncogenic and are associated with sensitivity to the irreversible EGFR/ERBB2 inhibitor HKI-272.

Minami Y, Shimamura T, Shah K, LaFramboise T, Glatt KA, Liniker E, Borgman CL, Haringsma HJ, Feng W, Weir BA, Lowell AM, Lee JC, Wolf J, Shapiro GI, Wong KK, Meyerson M, Thomas RK.

Oncogene. 2007 Jul 26;26(34):5023-7. Epub 2007 Feb 19.

PMID:
17311002
9.

Dual inhibition of ErbB1 (EGFR/HER1) and ErbB2 (HER2/neu).

Reid A, Vidal L, Shaw H, de Bono J.

Eur J Cancer. 2007 Feb;43(3):481-9. Epub 2007 Jan 8. Review.

PMID:
17208435
10.

4-Anilino-6,7-dialkoxyquinoline-3-carbonitrile inhibitors of epidermal growth factor receptor kinase and their bioisosteric relationship to the 4-anilino-6,7-dialkoxyquinazoline inhibitors.

Wissner A, Berger DM, Boschelli DH, Floyd MB Jr, Greenberger LM, Gruber BC, Johnson BD, Mamuya N, Nilakantan R, Reich MF, Shen R, Tsou HR, Upeslacis E, Wang YF, Wu B, Ye F, Zhang N.

J Med Chem. 2000 Aug 24;43(17):3244-56.

PMID:
10966743
11.

Antitumor activity of a dual epidermal growth factor receptor and ErbB2 kinase inhibitor MP-412 (AV-412) in mouse xenograft models.

Suzuki T, Fujii A, Ohya J, Nakamura H, Fujita F, Koike M, Fujita M.

Cancer Sci. 2009 Aug;100(8):1526-31. doi: 10.1111/j.1349-7006.2009.01197.x. Epub 2009 May 13.

12.

A phase I study with neratinib (HKI-272), an irreversible pan ErbB receptor tyrosine kinase inhibitor, in patients with solid tumors.

Wong KK, Fracasso PM, Bukowski RM, Lynch TJ, Munster PN, Shapiro GI, Jänne PA, Eder JP, Naughton MJ, Ellis MJ, Jones SF, Mekhail T, Zacharchuk C, Vermette J, Abbas R, Quinn S, Powell C, Burris HA.

Clin Cancer Res. 2009 Apr 1;15(7):2552-8. doi: 10.1158/1078-0432.CCR-08-1978. Epub 2009 Mar 24.

13.

Synthesis and antitumor evaluation of novel 5-substituted-4-hydroxy-8-nitroquinazolines as EGFR signaling-targeted inhibitors.

Jin Y, Li HY, Lin LP, Tan J, Ding J, Luo X, Long YQ.

Bioorg Med Chem. 2005 Oct 1;13(19):5613-22.

PMID:
15993078
14.

Discovery of novel small-molecule inhibitors of human epidermal growth factor receptor-2: combined ligand and target-based approach.

Gundla R, Kazemi R, Sanam R, Muttineni R, Sarma JA, Dayam R, Neamati N.

J Med Chem. 2008 Jun 26;51(12):3367-77. doi: 10.1021/jm7013875.

PMID:
18500794
15.

Targeting EGFR and HER-2 receptor tyrosine kinases for cancer drug discovery and development.

Kamath S, Buolamwini JK.

Med Res Rev. 2006 Sep;26(5):569-94. Review.

PMID:
16788977
16.

Novel pyrrolo[2,1-f][1,2,4]triazin-4-amines: Dual inhibitors of EGFR and HER2 protein tyrosine kinases.

Fink BE, Norris D, Mastalerz H, Chen P, Goyal B, Zhao Y, Kim SH, Vite GD, Lee FY, Zhang H, Oppenheimer S, Tokarski JS, Wong TW, Gavai AV.

Bioorg Med Chem Lett. 2011 Jan 15;21(2):781-5. doi: 10.1016/j.bmcl.2010.11.100. Epub 2010 Nov 30.

PMID:
21177105
17.

Second-generation epidermal growth factor tyrosine kinase inhibitors in non-small cell lung cancer.

Mukherji D, Spicer J.

Expert Opin Investig Drugs. 2009 Mar;18(3):293-301. doi: 10.1517/13543780902762843 . Review.

PMID:
19243280
18.

Design, synthesis and in vitro antitumor activity of 4-aminoquinoline and 4-aminoquinazoline derivatives targeting EGFR tyrosine kinase.

Abouzid K, Shouman S.

Bioorg Med Chem. 2008 Aug 15;16(16):7543-51. doi: 10.1016/j.bmc.2008.07.038. Epub 2008 Jul 20.

PMID:
18678492
19.

Design, synthesis and biological evaluation of thiazolidinone derivatives as potential EGFR and HER-2 kinase inhibitors.

Lv PC, Zhou CF, Chen J, Liu PG, Wang KR, Mao WJ, Li HQ, Yang Y, Xiong J, Zhu HL.

Bioorg Med Chem. 2010 Jan 1;18(1):314-9. doi: 10.1016/j.bmc.2009.10.051. Epub 2009 Oct 30.

PMID:
19914835
20.

Irreversible inhibition of epidermal growth factor receptor activity by 3-aminopropanamides.

Carmi C, Galvani E, Vacondio F, Rivara S, Lodola A, Russo S, Aiello S, Bordi F, Costantino G, Cavazzoni A, Alfieri RR, Ardizzoni A, Petronini PG, Mor M.

J Med Chem. 2012 Mar 8;55(5):2251-64. doi: 10.1021/jm201507x. Epub 2012 Feb 17.

PMID:
22280453

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