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Items: 1 to 50 of 164

1.

Design, synthesis and biological assessment of novel N-substituted 3-(phthalimidin-2-yl)-2,6-dioxopiperidines and 3-substituted 2,6-dioxopiperidines for TNF-α inhibitory activity.

Luo W, Yu QS, Salcedo I, Holloway HW, Lahiri DK, Brossi A, Tweedie D, Greig NH.

Bioorg Med Chem. 2011 Jul 1;19(13):3965-72. doi: 10.1016/j.bmc.2011.05.029. Epub 2011 May 23.

2.

Preparation and Characterization of Tetrabenazine Enantiomers against Vesicular Monoamine Transporter 2.

Yu QS, Luo W, Deschamps J, Holloway HW, Kopajtic T, Katz JL, Brossi A, Greig NH.

ACS Med Chem Lett. 2010 Mar 31;1(3):105-109.

3.

Long-acting anticholinesterases for myasthenia gravis: synthesis and activities of quaternary phenylcarbamates of neostigmine, pyridostigmine and physostigmine.

Yu QS, Holloway HW, Luo W, Lahiri DK, Brossi A, Greig NH.

Bioorg Med Chem. 2010 Jul 1;18(13):4687-93. doi: 10.1016/j.bmc.2010.05.022. Epub 2010 May 12.

4.

Antitumor agents 273. Design and synthesis of N-alkyl-thiocolchicinoids as potential antitumor agents.

Kozaka T, Nakagawa-Goto K, Shi Q, Lai CY, Hamel E, Bastow KF, Brossi A, Lee KH.

Bioorg Med Chem Lett. 2010 Jul 15;20(14):4091-4. doi: 10.1016/j.bmcl.2010.05.081. Epub 2010 May 24.

5.

Antitumor agents. 272. Structure-activity relationships and in vivo selective anti-breast cancer activity of novel neo-tanshinlactone analogues.

Dong Y, Shi Q, Pai HC, Peng CY, Pan SL, Teng CM, Nakagawa-Goto K, Yu D, Liu YN, Wu PC, Bastow KF, Morris-Natschke SL, Brossi A, Lang JY, Hsu JL, Hung MC, Lee EY, Lee KH.

J Med Chem. 2010 Mar 11;53(5):2299-308. doi: 10.1021/jm1000858.

6.

Antitumor agents 270. Novel substituted 6-phenyl-4H-furo[3,2-c]pyran-4-one derivatives as potent and highly selective anti-breast cancer agents.

Dong Y, Shi Q, Nakagawa-Goto K, Wu PC, Morris-Natschke SL, Brossi A, Bastow KF, Lang JY, Hung MC, Lee KH.

Bioorg Med Chem. 2010 Jan 15;18(2):803-8. doi: 10.1016/j.bmc.2009.11.049. Epub 2009 Dec 2.

7.

A cellular model of inflammation for identifying TNF-alpha synthesis inhibitors.

Tweedie D, Luo W, Short RG, Brossi A, Holloway HW, Li Y, Yu QS, Greig NH.

J Neurosci Methods. 2009 Oct 15;183(2):182-7. doi: 10.1016/j.jneumeth.2009.06.034. Epub 2009 Jul 5.

8.

GLP-1 receptor stimulation preserves primary cortical and dopaminergic neurons in cellular and rodent models of stroke and Parkinsonism.

Li Y, Perry T, Kindy MS, Harvey BK, Tweedie D, Holloway HW, Powers K, Shen H, Egan JM, Sambamurti K, Brossi A, Lahiri DK, Mattson MP, Hoffer BJ, Wang Y, Greig NH.

Proc Natl Acad Sci U S A. 2009 Jan 27;106(4):1285-90. doi: 10.1073/pnas.0806720106. Epub 2009 Jan 21.

9.

Antitumor agents 253. Design, synthesis, and antitumor evaluation of novel 9-substituted phenanthrene-based tylophorine derivatives as potential anticancer agents.

Wei L, Shi Q, Bastow KF, Brossi A, Morris-Natschke SL, Nakagawa-Goto K, Wu TS, Pan SL, Teng CM, Lee KH.

J Med Chem. 2007 Jul 26;50(15):3674-80. Epub 2007 Jun 22.

PMID:
17585747
10.

Antitumor agents 252. Application of validated QSAR models to database mining: discovery of novel tylophorine derivatives as potential anticancer agents.

Zhang S, Wei L, Bastow K, Zheng W, Brossi A, Lee KH, Tropsha A.

J Comput Aided Mol Des. 2007 Jan-Mar;21(1-3):97-112. Epub 2007 Mar 6.

11.

Neurine, an acetylcholine autolysis product, elevates secreted amyloid-beta protein precursor and amyloid-beta peptide levels, and lowers neuronal cell viability in culture: a role in Alzheimer's disease?

Tweedie D, Brossi A, Chen D, Ge YW, Bailey J, Yu QS, Kamal MA, Sambamurti K, Lahiri DK, Greig NH.

J Alzheimers Dis. 2006 Sep;10(1):9-16.

PMID:
16988475
12.

Antitumor agents 251: synthesis, cytotoxic evaluation, and structure-activity relationship studies of phenanthrene-based tylophorine derivatives (PBTs) as a new class of antitumor agents.

Wei L, Brossi A, Kendall R, Bastow KF, Morris-Natschke SL, Shi Q, Lee KH.

Bioorg Med Chem. 2006 Oct 1;14(19):6560-9. Epub 2006 Jun 30.

PMID:
16809043
13.

Identification of novel small molecule inhibitors of amyloid precursor protein synthesis as a route to lower Alzheimer's disease amyloid-beta peptide.

Utsuki T, Yu QS, Davidson D, Chen D, Holloway HW, Brossi A, Sambamurti K, Lahiri DK, Greig NH, Giordano T.

J Pharmacol Exp Ther. 2006 Aug;318(2):855-62. Epub 2006 May 11.

PMID:
16690718
14.

Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine.

Luo W, Yu QS, Kulkarni SS, Parrish DA, Holloway HW, Tweedie D, Shafferman A, Lahiri DK, Brossi A, Greig NH.

J Med Chem. 2006 Apr 6;49(7):2174-85.

15.

Selective butyrylcholinesterase inhibition elevates brain acetylcholine, augments learning and lowers Alzheimer beta-amyloid peptide in rodent.

Greig NH, Utsuki T, Ingram DK, Wang Y, Pepeu G, Scali C, Yu QS, Mamczarz J, Holloway HW, Giordano T, Chen D, Furukawa K, Sambamurti K, Brossi A, Lahiri DK.

Proc Natl Acad Sci U S A. 2005 Nov 22;102(47):17213-8. Epub 2005 Nov 7.

17.

An overview of phenserine tartrate, a novel acetylcholinesterase inhibitor for the treatment of Alzheimer's disease.

Greig NH, Sambamurti K, Yu QS, Brossi A, Bruinsma GB, Lahiri DK.

Curr Alzheimer Res. 2005 Jul;2(3):281-90. Review.

PMID:
15974893
18.

Novel anticholinesterases based on the molecular skeletons of furobenzofuran and methanobenzodioxepine.

Luo W, Yu QS, Zhan M, Parrish D, Deschamps JR, Kulkarni SS, Holloway HW, Alley GM, Lahiri DK, Brossi A, Greig NH.

J Med Chem. 2005 Feb 24;48(4):986-94.

PMID:
15715468
19.

Antitumor agents. Part 236: Synthesis of water-soluble colchicine derivatives.

Nakagawa-Goto K, Chen CX, Hamel E, Wu CC, Bastow KF, Brossi A, Lee KH.

Bioorg Med Chem Lett. 2005 Jan 3;15(1):235-8.

PMID:
15582446
20.
21.

Thalidomide-based TNF-alpha inhibitors for neurodegenerative diseases.

Greig NH, Giordano T, Zhu X, Yu QS, Perry TA, Holloway HW, Brossi A, Rogers JT, Sambamurti K, Lahiri DK.

Acta Neurobiol Exp (Wars). 2004;64(1):1-9.

22.

Antitumor agents. Part 235: Novel 4'-ester etoposide analogues as potent DNA topoisomerase II inhibitors with improved therapeutic potential.

Xiao Z, Vance JR, Bastow KF, Brossi A, Wang HK, Lee KH.

Bioorg Med Chem. 2004 Jun 15;12(12):3363-9.

PMID:
15158805
23.

Thiothalidomides: novel isosteric analogues of thalidomide with enhanced TNF-alpha inhibitory activity.

Zhu X, Giordano T, Yu QS, Holloway HW, Perry TA, Lahiri DK, Brossi A, Greig NH.

J Med Chem. 2003 Nov 20;46(24):5222-9.

PMID:
14613324
24.

Antitumor agents. Part 226: synthesis and cytotoxicity of 2-phenyl-4-quinolone acetic acids and their esters.

Xia Y, Yang ZY, Xia P, Bastow KF, Nakanishi Y, Nampoothiri P, Hamel E, Brossi A, Lee KH.

Bioorg Med Chem Lett. 2003 Sep 1;13(17):2891-3.

PMID:
14611851
25.

Anti-HIV agents. Part 55: 3'R,4'R-Di-(O)-(-)-camphanoyl-2',2'-dimethyldihydropyrano[2,3-f]chromone (DCP), a novel anti-HIV agent.

Yu D, Brossi A, Kilgore N, Wild C, Allaway G, Lee KH.

Bioorg Med Chem Lett. 2003 May 5;13(9):1575-6.

PMID:
12699758
26.

Antitumor agents. Part 215: antitubulin effects of cytotoxic B-ring modified allocolchicinoids.

Han S, Hamel E, Bastow KF, McPhail AT, Brossi A, Lee KH.

Bioorg Med Chem Lett. 2002 Oct 21;12(20):2851-3.

PMID:
12270161
27.

Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines.

Yu QS, Zhu X, Holloway HW, Whittaker NF, Brossi A, Greig NH.

J Med Chem. 2002 Aug 15;45(17):3684-91.

PMID:
12166941
28.

Antitumor agents. Part 209: Pheophorbide-a derivatives as photo-Independent cytotoxic agents.

Wongsinkongman P, Brossi A, Wang HK, Bastow KF, Lee KH.

Bioorg Med Chem. 2002 Mar;10(3):583-91.

PMID:
11814846
29.

Methyl analogues of the experimental Alzheimer drug phenserine: synthesis and structure/activity relationships for acetyl- and butyrylcholinesterase inhibitory action.

Yu Q, Holloway HW, Flippen-Anderson JL, Hoffman B, Brossi A, Greig NH.

J Med Chem. 2001 Nov 22;44(24):4062-71.

PMID:
11708910
30.

Phenserine regulates translation of beta -amyloid precursor protein mRNA by a putative interleukin-1 responsive element, a target for drug development.

Shaw KT, Utsuki T, Rogers J, Yu QS, Sambamurti K, Brossi A, Ge YW, Lahiri DK, Greig NH.

Proc Natl Acad Sci U S A. 2001 Jun 19;98(13):7605-10. Epub 2001 Jun 12.

31.

The experimental Alzheimer drug phenserine: preclinical pharmacokinetics and pharmacodynamics.

Greig NH, De Micheli E, Holloway HW, Yu QS, Utsuki T, Perry TA, Brossi A, Ingram DK, Deutsch J, Lahiri DK, Soncrant TT.

Acta Neurol Scand Suppl. 2000;176:74-84.

PMID:
11261809
32.
33.

Anti-AIDS agents part 41: synthesis and anti-HIV activity of 3',4'-di-o-(-)-camphanoyl-(+)-cis-khellactone (DCK) lactam analogues.

Yang ZY, Xia Y, Xia P, Brossi A, Cosentino LM, Lee KH.

Bioorg Med Chem Lett. 2000 May 15;10(10):1003-5.

PMID:
10843202
34.

Asymmetric solid-phase synthesis of (3'R,4'R)-di-O-cis-acyl 3-carboxyl khellactones.

Xia Y, Yang ZY, Brossi A, Lee KH.

Org Lett. 1999 Dec 30;1(13):2113-5.

PMID:
10836064
35.
36.

Synthesis of novel phenserine-based-selective inhibitors of butyrylcholinesterase for Alzheimer's disease.

Yu Q, Holloway HW, Utsuki T, Brossi A, Greig NH.

J Med Chem. 1999 May 20;42(10):1855-61.

PMID:
10346939
37.

Antitumor agents. Part 186: Synthesis and biological evaluation of demethylcolchiceinamide analogues as cytotoxic DNA topoisomerase II inhibitors.

Guan J, Zhu XK, Tachibana Y, Bastow KF, Brossi A, Hamel E, Lee KH.

Bioorg Med Chem. 1998 Nov;6(11):2127-31.

PMID:
9881102
38.

Antitumor agents. 185. Synthesis and biological evaluation of tridemethylthiocolchicine analogues as novel topoisomerase II inhibitors.

Guan J, Zhu XK, Tachibana Y, Bastow KF, Brossi A, Hamel E, Lee KH.

J Med Chem. 1998 May 21;41(11):1956-61.

PMID:
9599244
40.

Antitumor agents--CLXXV. Anti-tubulin action of (+)-thiocolchicine prepared by partial synthesis.

Shi Q, Verdier-Pinard P, Brossi A, Hamel E, Lee KH.

Bioorg Med Chem. 1997 Dec;5(12):2277-82.

PMID:
9459025
41.
42.

Antitumor agents. 172. Synthesis and biological evaluation of novel deacetamidothiocolchicin-7-ols and ester analogs as antitubulin agents.

Shi Q, Verdier-Pinard P, Brossi A, Hamel E, McPhail AT, Lee KH.

J Med Chem. 1997 Mar 14;40(6):961-6.

PMID:
9083485
43.

Identification of cysteine 354 of beta-tubulin as part of the binding site for the A ring of colchicine.

Bai R, Pei XF, Boyé O, Getahun Z, Grover S, Bekisz J, Nguyen NY, Brossi A, Hamel E.

J Biol Chem. 1996 May 24;271(21):12639-45.

44.

Maze learning in aged rats is enhanced by phenserine, a novel anticholinesterase.

Ikari H, Spangler EL, Greig NH, Pei XF, Brossi A, Speer D, Patel N, Ingram DK.

Neuroreport. 1995 Feb 15;6(3):481-4.

PMID:
7766848
45.

Phenserine and ring C hetero-analogues: drug candidates for the treatment of Alzheimer's disease.

Greig NH, Pei XF, Soncrant TT, Ingram DK, Brossi A.

Med Res Rev. 1995 Jan;15(1):3-31. Review. No abstract available.

PMID:
7898167
46.

Chiral drugs: synopsis.

Brossi A.

Med Res Rev. 1994 Nov;14(6):665-91. Review. No abstract available.

PMID:
7830418
47.

The nitrogen of the acetamido group of colchicine modulates P-glycoprotein-mediated multidrug resistance.

Tang-Wai DF, Brossi A, Arnold LD, Gros P.

Biochemistry. 1993 Jun 29;32(25):6470-6.

PMID:
8100149
48.

Effects of mescaline and some of its analogs on cholinergic neuromuscular transmission.

Ghansah E, Kopsombut P, Malleque MA, Brossi A.

Neuropharmacology. 1993 Feb;32(2):169-74.

PMID:
8383816
49.
50.

Chloroacetates of 2- and 3-demethylthiocolchicine: specific covalent interactions with tubulin with preferential labeling of the beta-subunit.

Grover S, Boyé O, Getahun Z, Brossi A, Hamel E.

Biochem Biophys Res Commun. 1992 Sep 30;187(3):1350-8.

PMID:
1417811

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