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Items: 42

1.

Discovery of CRBN E3 Ligase Modulator CC-92480 for the Treatment of Relapsed and Refractory Multiple Myeloma.

Hansen JD, Correa M, Nagy MA, Alexander M, Plantevin V, Grant V, Whitefield B, Huang D, Kercher T, Harris R, Narla RK, Leisten J, Tang Y, Moghaddam M, Ebinger K, Piccotti J, Havens CG, Cathers B, Carmichael J, Daniel T, Vessey R, Hamann LG, Leftheris K, Mendy D, Baculi F, LeBrun LA, Khambatta G, Lopez-Girona A.

J Med Chem. 2020 Mar 19. doi: 10.1021/acs.jmedchem.9b01928. [Epub ahead of print]

PMID:
32130004
2.

Synthetic Lethal Strategy Identifies a Potent and Selective TTK and CLK1/2 Inhibitor for Treatment of Triple-Negative Breast Cancer with a Compromised G1-S Checkpoint.

Zhu D, Xu S, Deyanat-Yazdi G, Peng SX, Barnes LA, Narla RK, Tran T, Mikolon D, Ning Y, Shi T, Jiang N, Raymon HK, Riggs JR, Boylan JF.

Mol Cancer Ther. 2018 Aug;17(8):1727-1738. doi: 10.1158/1535-7163.MCT-17-1084. Epub 2018 Jun 4.

3.

The Discovery of a Dual TTK Protein Kinase/CDC2-Like Kinase (CLK2) Inhibitor for the Treatment of Triple Negative Breast Cancer Initiated from a Phenotypic Screen.

Riggs JR, Nagy M, Elsner J, Erdman P, Cashion D, Robinson D, Harris R, Huang D, Tehrani L, Deyanat-Yazdi G, Narla RK, Peng X, Tran T, Barnes L, Miller T, Katz J, Tang Y, Chen M, Moghaddam MF, Bahmanyar S, Pagarigan B, Delker S, LeBrun L, Chamberlain PP, Calabrese A, Canan SS, Leftheris K, Zhu D, Boylan JF.

J Med Chem. 2017 Nov 9;60(21):8989-9002. doi: 10.1021/acs.jmedchem.7b01223. Epub 2017 Oct 27.

PMID:
28991472
4.

Pomalidomide in combination with dexamethasone results in synergistic anti-tumour responses in pre-clinical models of lenalidomide-resistant multiple myeloma.

Rychak E, Mendy D, Shi T, Ning Y, Leisten J, Lu L, Miller K, Narla RK, Orlowski RZ, Raymon HK, Bjorklund CC, Thakurta A, Gandhi AK, Cathers BE, Chopra R, Daniel TO, Lopez-Girona A.

Br J Haematol. 2016 Mar;172(6):889-901. doi: 10.1111/bjh.13905. Epub 2016 Feb 23.

PMID:
26914976
5.

Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115.

Mortensen DS, Perrin-Ninkovic SM, Shevlin G, Elsner J, Zhao J, Whitefield B, Tehrani L, Sapienza J, Riggs JR, Parnes JS, Papa P, Packard G, Lee BG, Harris R, Correa M, Bahmanyar S, Richardson SJ, Peng SX, Leisten J, Khambatta G, Hickman M, Gamez JC, Bisonette RR, Apuy J, Cathers BE, Canan SS, Moghaddam MF, Raymon HK, Worland P, Narla RK, Fultz KE, Sankar S.

J Med Chem. 2015 Jul 23;58(14):5599-608. doi: 10.1021/acs.jmedchem.5b00627. Epub 2015 Jul 8.

PMID:
26102506
6.

Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.

Mortensen DS, Perrin-Ninkovic SM, Shevlin G, Zhao J, Packard G, Bahmanyar S, Correa M, Elsner J, Harris R, Lee BG, Papa P, Parnes JS, Riggs JR, Sapienza J, Tehrani L, Whitefield B, Apuy J, Bisonette RR, Gamez JC, Hickman M, Khambatta G, Leisten J, Peng SX, Richardson SJ, Cathers BE, Canan SS, Moghaddam MF, Raymon HK, Worland P, Narla RK, Fultz KE, Sankar S.

J Med Chem. 2015 Jul 9;58(13):5323-33. doi: 10.1021/acs.jmedchem.5b00626. Epub 2015 Jun 26.

PMID:
26083478
7.

CC-122, a pleiotropic pathway modifier, mimics an interferon response and has antitumor activity in DLBCL.

Hagner PR, Man HW, Fontanillo C, Wang M, Couto S, Breider M, Bjorklund C, Havens CG, Lu G, Rychak E, Raymon H, Narla RK, Barnes L, Khambatta G, Chiu H, Kosek J, Kang J, Amantangelo MD, Waldman M, Lopez-Girona A, Cai T, Pourdehnad M, Trotter M, Daniel TO, Schafer PH, Klippel A, Thakurta A, Chopra R, Gandhi AK.

Blood. 2015 Aug 6;126(6):779-89. doi: 10.1182/blood-2015-02-628669. Epub 2015 May 22.

8.

CC-223, a Potent and Selective Inhibitor of mTOR Kinase: In Vitro and In Vivo Characterization.

Mortensen DS, Fultz KE, Xu S, Xu W, Packard G, Khambatta G, Gamez JC, Leisten J, Zhao J, Apuy J, Ghoreishi K, Hickman M, Narla RK, Bissonette R, Richardson S, Peng SX, Perrin-Ninkovic S, Tran T, Shi T, Yang WQ, Tong Z, Cathers BE, Moghaddam MF, Canan SS, Worland P, Sankar S, Raymon HK.

Mol Cancer Ther. 2015 Jun;14(6):1295-305. doi: 10.1158/1535-7163.MCT-14-1052. Epub 2015 Apr 8.

9.

Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.

Mortensen DS, Sapienza J, Lee BG, Perrin-Ninkovic SM, Harris R, Shevlin G, Parnes JS, Whitefield B, Hickman M, Khambatta G, Bisonette RR, Peng S, Gamez JC, Leisten J, Narla RK, Fultz KE, Sankar S.

Bioorg Med Chem Lett. 2013 Mar 15;23(6):1588-91. doi: 10.1016/j.bmcl.2013.01.110. Epub 2013 Jan 30.

PMID:
23414803
10.

1,1-Diarylalkenes as anticancer agents: dual inhibitors of tubulin polymerization and phosphodiesterase 4.

Ruchelman AL, Man HW, Chen R, Liu W, Lu L, Cedzik D, Zhang L, Leisten J, Collette A, Narla RK, Raymon HK, Muller GW.

Bioorg Med Chem. 2011 Nov 1;19(21):6356-74. doi: 10.1016/j.bmc.2011.08.068. Epub 2011 Sep 5.

PMID:
21955454
11.

The synthetic compound CC-5079 is a potent inhibitor of tubulin polymerization and tumor necrosis factor-alpha production with antitumor activity.

Zhang LH, Wu L, Raymon HK, Chen RS, Corral L, Shirley MA, Narla RK, Gamez J, Muller GW, Stirling DI, Bartlett JB, Schafer PH, Payvandi F.

Cancer Res. 2006 Jan 15;66(2):951-9.

12.

Phenylarsonic acid compounds with broad-spectrum and potent cytotoxic activity against human cancer cells.

Uckun FM, D'Cruz OJ, Liu XP, Narla RK.

Arzneimittelforschung. 2003;53(6):428-39.

PMID:
12872614
13.

Organic phenyl arsonic acid compounds with potent antileukemic activity.

Liu XP, Narla RK, Uckun FM.

Bioorg Med Chem Lett. 2003 Feb 10;13(3):581-3.

PMID:
12565976
14.

Structure-based design of novel anticancer agents.

Uckun FM, Sudbeck EA, Mao C, Ghosh S, Liu XP, Vassilev AO, Navara CS, Narla RK.

Curr Cancer Drug Targets. 2001 May;1(1):59-71. Review.

PMID:
12188892
15.

Spongistatins as tubulin targeting agents.

Uckun FM, Mao C, Jan ST, Huang H, Vassilev AO, Navara CS, Narla RK.

Curr Pharm Des. 2001 Sep;7(13):1291-6. Review.

PMID:
11472268
16.
18.

X-ray structure, solution properties, and biological activity profile of vanadocene(IV) acetylacetonate complex,.

Ghosh P, Ghosh S, Navara C, Narla RK, Benyumov A, Uckun FM.

J Inorg Biochem. 2001 Apr;84(3-4):241-53.

PMID:
11374587
19.

Vanadocenes as potent anti-proliferative agents disrupting mitotic spindle formation in cancer cells.

Navara CS, Benyumov A, Vassilev A, Narla RK, Ghosh P, Uckun FM.

Anticancer Drugs. 2001 Apr;12(4):369-76.

PMID:
11335794
20.
21.

SPIKET and COBRA compounds as novel tubulin modulators with potent anticancer activity.

Uckun FM, Mao C, Jan ST, Huang H, Vassilev AO, Sudbeck EA, Navara CS, Narla RK.

Curr Opin Investig Drugs. 2000 Oct;1(2):252-6. Review.

PMID:
11249582
22.

Synthesis, X-ray structure, and anti-leukemic activity of oxovanadium(IV) complexes.

Dong Y, Narla RK, Sudbeck E, Uckun FM.

J Inorg Biochem. 2000 Mar;78(4):321-30.

PMID:
10857913
23.

A rationally designed anticancer drug targeting a unique binding cavity of tubulin.

Uckun FM, Mao C, Vassilev AO, Navara CS, Narla RK, Jan ST.

Bioorg Med Chem Lett. 2000 May 15;10(10):1015-8.

PMID:
10843205
24.

Bis(4,7-dimethyl-1,10-phenanthroline) sulfatooxovanadium(IV) as a novel apoptosis-inducing anticancer agent.

Narla RK, Dong Y, D'Cruz OJ, Navara C, Uckun FM.

Clin Cancer Res. 2000 Apr;6(4):1546-56.

25.

Apoptosis-inducing vanadocene compounds against human testicular cancer.

Ghosh P, D'Cruz OJ, Narla RK, Uckun FM.

Clin Cancer Res. 2000 Apr;6(4):1536-45.

26.

EGF-genistein inhibits neointimal hyperplasia after vascular injury in an experimental restenosis model.

Trieu VN, Narla RK, Myers DE, Uckun FM.

J Cardiovasc Pharmacol. 2000 Apr;35(4):595-605.

PMID:
10774791
27.

Structure-based design of potent inhibitors of EGF-receptor tyrosine kinase as anti-cancer agents.

Ghosh S, Narla RK, Zheng Y, Liu XP, Jun X, Mao C, Sudbeck EA, Uckun FM.

Anticancer Drug Des. 1999 Oct;14(5):403-10.

PMID:
10766295
28.

The S-alkyl chain length as a determinant of the anti-leukemic activity of cysteine chloromethyl ketone compounds.

Perrey DA, Scannell MP, Narla RK, Uckun FM.

Bioorg Med Chem Lett. 2000 Mar 20;10(6):551-2.

PMID:
10741551
29.

Cysteine chloromethyl and diazomethyl ketone derivatives with potent anti-leukemic activity.

Perrey DA, Narla RK, Uckun FM.

Bioorg Med Chem Lett. 2000 Mar 20;10(6):547-9.

PMID:
10741550
30.

Horizontal basal cell proliferation in the olfactory epithelium of transforming growth factor-alpha transgenic mice.

Getchell TV, Narla RK, Little S, Hyde JF, Getchell ML.

Cell Tissue Res. 2000 Feb;299(2):185-92.

PMID:
10741459
31.

Antioxidant function of phenethyl-5-bromo-pyridyl thiourea compounds with potent anti-HIV activity.

Dong Y, Venkatachalam TK, Narla RK, Trieu VN, Sudbeck EA, Uckun FM.

Bioorg Med Chem Lett. 2000 Jan 3;10(1):87-90.

PMID:
10636251
32.

Structure-based design of specific inhibitors of Janus kinase 3 as apoptosis-inducing antileukemic agents.

Sudbeck EA, Liu XP, Narla RK, Mahajan S, Ghosh S, Mao C, Uckun FM.

Clin Cancer Res. 1999 Jun;5(6):1569-82.

33.
34.
35.

Molecular genotoxicity profiles of apoptosis-inducing vanadocene complexes.

Aubrecht J, Narla RK, Ghosh P, Stanek J, Uckun FM.

Toxicol Appl Pharmacol. 1999 Feb 1;154(3):228-35.

PMID:
9931282
36.

Calphostin C triggers calcium-dependent apoptosis in human acute lymphoblastic leukemia cells.

Zhu DM, Narla RK, Fang WH, Chia NC, Uckun FM.

Clin Cancer Res. 1998 Dec;4(12):2967-76.

37.
39.
41.

In vivo toxicity, pharmacokinetics, and anticancer activity of Genistein linked to recombinant human epidermal growth factor.

Uckun FM, Narla RK, Zeren T, Yanishevski Y, Myers DE, Waurzyniak B, Ek O, Schneider E, Messinger Y, Chelstrom LM, Gunther R, Evans W.

Clin Cancer Res. 1998 May;4(5):1125-34.

42.

Cytotoxic activity of epidermal growth factor-genistein against breast cancer cells.

Uckun FM, Narla RK, Jun X, Zeren T, Venkatachalam T, Waddick KG, Rostostev A, Myers DE.

Clin Cancer Res. 1998 Apr;4(4):901-12.

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