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A novel quinoline, MT477: suppresses cell signaling through Ras molecular pathway, inhibits PKC activity, and demonstrates in vivo anti-tumor activity against human carcinoma cell lines.

Jasinski P, Welsh B, Galvez J, Land D, Zwolak P, Ghandi L, Terai K, Dudek AZ.

Invest New Drugs. 2008 Jun;26(3):223-32. Epub 2007 Oct 24.


Novel Ras pathway inhibitor induces apoptosis and growth inhibition of K-ras-mutated cancer cells in vitro and in vivo.

Jasinski P, Zwolak P, Terai K, Dudek AZ.

Transl Res. 2008 Nov;152(5):203-12. doi: 10.1016/j.trsl.2008.09.001. Epub 2008 Oct 11.


PKC-alpha inhibitor MT477 slows tumor growth with minimal toxicity in in vivo model of non-Ras-mutated cancer via induction of apoptosis.

Jasinski P, Zwolak P, Terai K, Borja-Cacho D, Dudek AZ.

Invest New Drugs. 2011 Feb;29(1):33-40. doi: 10.1007/s10637-009-9330-9. Epub 2009 Oct 1.


R115777 (Zarnestra)/Zoledronic acid (Zometa) cooperation on inhibition of prostate cancer proliferation is paralleled by Erk/Akt inactivation and reduced Bcl-2 and bad phosphorylation.

Caraglia M, Marra M, Leonetti C, Meo G, D'Alessandro AM, Baldi A, Santini D, Tonini G, Bertieri R, Zupi G, Budillon A, Abbruzzese A.

J Cell Physiol. 2007 May;211(2):533-43.


Voreloxin, formerly SNS-595, has potent activity against a broad panel of cancer cell lines and in vivo tumor models.

Hoch U, Lynch J, Sato Y, Kashimoto S, Kajikawa F, Furutani Y, Silverman JA.

Cancer Chemother Pharmacol. 2009 Jun;64(1):53-65. doi: 10.1007/s00280-008-0850-3. Epub 2008 Oct 19.


Rhein lysinate suppresses the growth of breast cancer cells and potentiates the inhibitory effect of Taxol in athymic mice.

Lin YJ, Zhen YS.

Anticancer Drugs. 2009 Jan;20(1):65-72. doi: 10.1097/CAD.0b013e3283182913.


P276-00, a novel cyclin-dependent inhibitor induces G1-G2 arrest, shows antitumor activity on cisplatin-resistant cells and significant in vivo efficacy in tumor models.

Joshi KS, Rathos MJ, Mahajan P, Wagh V, Shenoy S, Bhatia D, Chile S, Sivakumar M, Maier A, Fiebig HH, Sharma S.

Mol Cancer Ther. 2007 Mar;6(3):926-34.


Growth-inhibitory effects of human anti-insulin-like growth factor-I receptor antibody (A12) in an orthotopic nude mouse model of anaplastic thyroid carcinoma.

Wang Z, Chakravarty G, Kim S, Yazici YD, Younes MN, Jasser SA, Santillan AA, Bucana CD, El-Naggar AK, Myers JN.

Clin Cancer Res. 2006 Aug 1;12(15):4755-65.


Identification of 4-anilino-3-quinolinecarbonitrile inhibitors of mitogen-activated protein/extracellular signal-regulated kinase 1 kinase.

Mallon R, Feldberg L, Kim S, Collins K, Wojciechowicz D, Kohler C, Kovacs D, Discafani C, Zhang N, Wu B, Floyd B, Powell D, Berger D.

Mol Cancer Ther. 2004 Jun;3(6):755-62.


Antimyeloma activity of the orally bioavailable dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor NVP-BEZ235.

McMillin DW, Ooi M, Delmore J, Negri J, Hayden P, Mitsiades N, Jakubikova J, Maira SM, Garcia-Echeverria C, Schlossman R, Munshi NC, Richardson PG, Anderson KC, Mitsiades CS.

Cancer Res. 2009 Jul 15;69(14):5835-42. doi: 10.1158/0008-5472.CAN-08-4285. Epub 2009 Jul 7.


MT477 acts in tumor cells as an AURKA inhibitor and strongly induces NRF-2 signaling.

Jasinski P, Zwolak P, Terai K, Vogel RI, Borja-Cacho D, Dudek AZ.

Anticancer Res. 2011 Apr;31(4):1181-7.


Enzastaurin, a protein kinase C beta inhibitor, suppresses signaling through the ribosomal S6 kinase and bad pathways and induces apoptosis in human gastric cancer cells.

Lee KW, Kim SG, Kim HP, Kwon E, You J, Choi HJ, Park JH, Kang BC, Im SA, Kim TY, Kim WH, Bang YJ.

Cancer Res. 2008 Mar 15;68(6):1916-26. doi: 10.1158/0008-5472.CAN-07-3195.


FTY720 induced Bcl-associated and Fas-independent apoptosis in human renal cancer cells in vitro and significantly reduced in vivo tumor growth in mouse xenograft.

Ubai T, Azuma H, Kotake Y, Inamoto T, Takahara K, Ito Y, Kiyama S, Sakamoto T, Horie S, Muto S, Takahara S, Otsuki Y, Katsuoka Y.

Anticancer Res. 2007 Jan-Feb;27(1A):75-88.


Anticancer activity of litchi fruit pericarp extract against human breast cancer in vitro and in vivo.

Wang X, Yuan S, Wang J, Lin P, Liu G, Lu Y, Zhang J, Wang W, Wei Y.

Toxicol Appl Pharmacol. 2006 Sep 1;215(2):168-78. Epub 2006 Mar 23.


Huang-lian-jie-du-tang, a traditional Chinese medicine prescription, induces cell-cycle arrest and apoptosis in human liver cancer cells in vitro and in vivo.

Hsu YL, Kuo PL, Tzeng TF, Sung SC, Yen MH, Lin LT, Lin CC.

J Gastroenterol Hepatol. 2008 Jul;23(7 Pt 2):e290-9. doi: 10.1111/j.1440-1746.2008.05390.x. Epub 2008 Jun 3.


Resistance to mitogen-activated protein kinase kinase (MEK) inhibitors correlates with up-regulation of the MEK/extracellular signal-regulated kinase pathway in hepatocellular carcinoma cells.

Yip-Schneider MT, Klein PJ, Wentz SC, Zeni A, Menze A, Schmidt CM.

J Pharmacol Exp Ther. 2009 Jun;329(3):1063-70. doi: 10.1124/jpet.108.147306. Epub 2009 Mar 3.


Role of RAF/MEK/ERK pathway, p-STAT-3 and Mcl-1 in sorafenib activity in human pancreatic cancer cell lines.

Ulivi P, Arienti C, Amadori D, Fabbri F, Carloni S, Tesei A, Vannini I, Silvestrini R, Zoli W.

J Cell Physiol. 2009 Jul;220(1):214-21. doi: 10.1002/jcp.21753.


PWT-458, a novel pegylated-17-hydroxywortmannin, inhibits phosphatidylinositol 3-kinase signaling and suppresses growth of solid tumors.

Yu K, Lucas J, Zhu T, Zask A, Gaydos C, Toral-Barza L, Gu J, Li F, Chaudhary I, Cai P, Lotvin J, Petersen R, Ruppen M, Fawzi M, Ayral-Kaloustian S, Skotnicki J, Mansour T, Frost P, Gibbons J.

Cancer Biol Ther. 2005 May;4(5):538-45. Epub 2005 May 28.


7-Chloro-6-piperidin-1-yl-quinoline-5,8-dione (PT-262), a novel synthetic compound induces lung carcinoma cell death associated with inhibiting ERK and CDC2 phosphorylation via a p53-independent pathway.

Hsu TS, Chen C, Lee PT, Chiu SJ, Liu HF, Tsai CC, Chao JI.

Cancer Chemother Pharmacol. 2008 Oct;62(5):799-808. doi: 10.1007/s00280-007-0667-5. Epub 2008 Jan 10. Erratum in: Cancer Chemother Pharmacol. 2008 Oct;62(5):809.

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