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Items: 1 to 50 of 598

1.

Design, synthesis and biological evaluation of 2-alkoxycarbonyl-3-anilinoindoles as a new class of potent inhibitors of tubulin polymerization.

Romagnoli R, Prencipe F, Oliva P, Kimatrai Salvador M, Brancale A, Ferla S, Hamel E, Viola G, Bortolozzi R, Persoons L, Balzarini J, Liekens S, Schols D.

Bioorg Chem. 2020 Feb 18;97:103665. doi: 10.1016/j.bioorg.2020.103665. [Epub ahead of print]

PMID:
32086053
2.

The Past, Present, And Possible Future Of Public Opinion On The ACA.

Brodie M, Hamel EC, Kirzinger A, Altman DE.

Health Aff (Millwood). 2020 Feb 19:101377hlthaff201901420. doi: 10.1377/hlthaff.2019.01420. [Epub ahead of print]

PMID:
32073909
3.

S-(4-Methoxyphenyl)-4-methoxybenzenesulfonothioate as a Promising Lead Compound for the Development of a Renal Carcinoma Agent.

Nantes CI, Pereira ID, Bai R, Hamel E, Burnett JC, de Oliveira RJ, de F C Matos M, Beatriz A, Yonekawa MKA, Perdomo RT, de Lima DP, Bogo D, Dos A Dos Santos E.

ChemMedChem. 2019 Dec 13. doi: 10.1002/cmdc.201900566. [Epub ahead of print]

PMID:
31834975
4.

Interaction of diazonamide A with tubulin.

Bai R, Cruz-Monserrate Z, Fenical W, Pettit GR, Hamel E.

Arch Biochem Biophys. 2020 Feb 15;680:108217. doi: 10.1016/j.abb.2019.108217. Epub 2019 Dec 9.

PMID:
31830440
5.

Proceedings from the Albert Charitable Trust Inaugural Workshop on white matter and cognition in aging.

Sorond FA, Whitehead S, Arai K, Arnold D, Carmichael ST, De Carli C, Duering M, Fornage M, Flores-Obando RE, Graff-Radford J, Hamel E, Hess DC, Ihara M, Jensen MK, Markus HS, Montagne A, Rosenberg G, Shih AY, Smith EE, Thiel A, Tse KH, Wilcock D, Barone F.

Geroscience. 2020 Feb;42(1):81-96. doi: 10.1007/s11357-019-00141-8. Epub 2019 Dec 6. Review.

PMID:
31811528
6.

Structure-activity relationship studies and in vitro and in vivo anticancer activity of novel 3-aroyl-1,4-diarylpyrroles against solid tumors and hematological malignancies.

Puxeddu M, Shen H, Bai R, Coluccia A, Nalli M, Mazzoccoli C, Da Pozzo E, Cavallini C, Martini C, Orlando V, Biagioni S, Mazzoni C, Coluccia AML, Hamel E, Liu T, Silvestri R, La Regina G.

Eur J Med Chem. 2020 Jan 1;185:111828. doi: 10.1016/j.ejmech.2019.111828. Epub 2019 Nov 2.

PMID:
31727471
7.

Memory and cerebrovascular deficits recovered following angiotensin IV intervention in a mouse model of Alzheimer's disease.

Royea J, Martinot P, Hamel E.

Neurobiol Dis. 2020 Feb;134:104644. doi: 10.1016/j.nbd.2019.104644. Epub 2019 Oct 24.

8.

Comparative benefits of simvastatin and exercise in a mouse model of vascular cognitive impairment and dementia.

Trigiani LJ, Royea J, Tong XK, Hamel E.

FASEB J. 2019 Dec;33(12):13280-13293. doi: 10.1096/fj.201901002R. Epub 2019 Sep 26.

9.

Synthesis and biological evaluation of structurally diverse α-conformationally restricted chalcones and related analogues.

Maguire CJ, Carlson GJ, Ford JW, Strecker TE, Hamel E, Trawick ML, Pinney KG.

Medchemcomm. 2019 Jun 4;10(8):1445-1456. doi: 10.1039/c9md00127a. eCollection 2019 Aug 1.

PMID:
31534659
10.

Design, synthesis and biological evaluation of novel vicinal diaryl-substituted 1H-Pyrazole analogues of combretastatin A-4 as highly potent tubulin polymerization inhibitors.

Romagnoli R, Oliva P, Salvador MK, Camacho ME, Padroni C, Brancale A, Ferla S, Hamel E, Ronca R, Grillo E, Bortolozzi R, Rruga F, Mariotto E, Viola G.

Eur J Med Chem. 2019 Nov 1;181:111577. doi: 10.1016/j.ejmech.2019.111577. Epub 2019 Aug 1.

PMID:
31400707
11.

Evaluating the effects of fluorine on biological properties and metabolic stability of some antitubulin 3-substituted 7-phenyl-pyrroloquinolinones.

Bortolozzi R, Carta D, Prà MD, Antoniazzi G, Mattiuzzo E, Sturlese M, Di Paolo V, Calderan L, Moro S, Hamel E, Quintieri L, Ronca R, Viola G, Ferlin MG.

Eur J Med Chem. 2019 Sep 15;178:297-314. doi: 10.1016/j.ejmech.2019.05.092. Epub 2019 Jun 3.

PMID:
31195171
12.

Synthesis and biological evaluation of indole-2-carbohydrazides and thiazolidinyl-indole-2-carboxamides as potent tubulin polymerization inhibitors.

Kazan F, Yagci ZB, Bai R, Ozkirimli E, Hamel E, Ozkirimli S.

Comput Biol Chem. 2019 Jun;80:512-523. doi: 10.1016/j.compbiolchem.2019.05.002. Epub 2019 May 11.

PMID:
31185422
13.

Structure Guided Design, Synthesis, and Biological Evaluation of Novel Benzosuberene Analogues as Inhibitors of Tubulin Polymerization.

Niu H, Strecker TE, Gerberich JL, Campbell JW 3rd, Saha D, Mondal D, Hamel E, Chaplin DJ, Mason RP, Trawick ML, Pinney KG.

J Med Chem. 2019 Jun 13;62(11):5594-5615. doi: 10.1021/acs.jmedchem.9b00551. Epub 2019 May 24.

PMID:
31059248
14.

Design, Synthesis and in vitro Anti-Cancer evaluation of Novel Derivatives of 2-(2-Methyl-1,5-diaryl-1H-pyrrol-3-yl)-2-oxo-N-(pyridin-3-yl)acetamide.

Moghadam ES, Saravani F, Hamel E, Shahsavari Z, Alipour M, Hosseinkhani S, Ostad S, Amini M.

Med Chem. 2019 Apr 25. doi: 10.2174/1573406415666190425153717. [Epub ahead of print]

PMID:
31032753
15.

Antiproliferative Aspidosperma-Type Monoterpenoid Indole Alkaloids from Bousigonia mekongensis Inhibit Tubulin Polymerization.

Zhang Y, Goto M, Oda A, Hsu PL, Guo LL, Fu YH, Morris-Natschke SL, Hamel E, Lee KH, Hao XJ.

Molecules. 2019 Mar 31;24(7). pii: E1256. doi: 10.3390/molecules24071256.

16.

Synthesis and anti-breast cancer activity of novel indibulin related diarylpyrrole derivatives.

Saeedian Moghadam E, Hamel E, Shahsavari Z, Amini M.

Daru. 2019 Jun;27(1):179-189. doi: 10.1007/s40199-019-00260-9. Epub 2019 Mar 20.

17.

Synthesis, in vitro and in vivo biological evaluation of substituted 3-(5-imidazo[2,1-b]thiazolylmethylene)-2-indolinones as new potent anticancer agents.

Morigi R, Locatelli A, Leoni A, Rambaldi M, Bortolozzi R, Mattiuzzo E, Ronca R, Maccarinelli F, Hamel E, Bai R, Brancale A, Viola G.

Eur J Med Chem. 2019 Mar 15;166:514-530. doi: 10.1016/j.ejmech.2019.01.049. Epub 2019 Jan 26.

PMID:
30784885
18.

Tetrahydroisoquinoline Sulfamates as Potent Microtubule Disruptors: Synthesis, Antiproliferative and Antitubulin Activity of Dichlorobenzyl-Based Derivatives, and a Tubulin Cocrystal Structure.

Dohle W, Prota AE, Menchon G, Hamel E, Steinmetz MO, Potter BVL.

ACS Omega. 2019 Jan 31;4(1):755-764. doi: 10.1021/acsomega.8b02879. Epub 2019 Jan 9.

19.

Spatial memory formation requires netrin-1 expression by neurons in the adult mammalian brain.

Wong EW, Glasgow SD, Trigiani LJ, Chitsaz D, Rymar V, Sadikot A, Ruthazer ES, Hamel E, Kennedy TE.

Learn Mem. 2019 Feb 15;26(3):77-83. doi: 10.1101/lm.049072.118. Print 2019 Mar.

PMID:
30770464
20.

How reliable is cerebral blood flow to map changes in neuronal activity?

Lecrux C, Bourourou M, Hamel E.

Auton Neurosci. 2019 Mar;217:71-79. doi: 10.1016/j.autneu.2019.01.005. Epub 2019 Jan 29. Review.

PMID:
30744905
21.
22.

Vascular dysfunction-The disregarded partner of Alzheimer's disease.

Sweeney MD, Montagne A, Sagare AP, Nation DA, Schneider LS, Chui HC, Harrington MG, Pa J, Law M, Wang DJJ, Jacobs RE, Doubal FN, Ramirez J, Black SE, Nedergaard M, Benveniste H, Dichgans M, Iadecola C, Love S, Bath PM, Markus HS, Salman RA, Allan SM, Quinn TJ, Kalaria RN, Werring DJ, Carare RO, Touyz RM, Williams SCR, Moskowitz MA, Katusic ZS, Lutz SE, Lazarov O, Minshall RD, Rehman J, Davis TP, Wellington CL, González HM, Yuan C, Lockhart SN, Hughes TM, Chen CLH, Sachdev P, O'Brien JT, Skoog I, Pantoni L, Gustafson DR, Biessels GJ, Wallin A, Smith EE, Mok V, Wong A, Passmore P, Barkof F, Muller M, Breteler MMB, Román GC, Hamel E, Seshadri S, Gottesman RF, van Buchem MA, Arvanitakis Z, Schneider JA, Drewes LR, Hachinski V, Finch CE, Toga AW, Wardlaw JM, Zlokovic BV.

Alzheimers Dement. 2019 Jan;15(1):158-167. doi: 10.1016/j.jalz.2018.07.222.

23.

Design, Synthesis, and Biological Evaluation of 6-Substituted Thieno[3,2- d]pyrimidine Analogues as Dual Epidermal Growth Factor Receptor Kinase and Microtubule Inhibitors.

Romagnoli R, Prencipe F, Oliva P, Baraldi S, Baraldi PG, Schiaffino Ortega S, Chayah M, Kimatrai Salvador M, Lopez-Cara LC, Brancale A, Ferla S, Hamel E, Ronca R, Bortolozzi R, Mariotto E, Mattiuzzo E, Viola G.

J Med Chem. 2019 Feb 14;62(3):1274-1290. doi: 10.1021/acs.jmedchem.8b01391. Epub 2019 Jan 18.

PMID:
30633509
24.

Synthesis of dihydronaphthalene analogues inspired by combretastatin A-4 and their biological evaluation as anticancer agents.

Maguire CJ, Chen Z, Mocharla VP, Sriram M, Strecker TE, Hamel E, Zhou H, Lopez R, Wang Y, Mason RP, Chaplin DJ, Trawick ML, Pinney KG.

Medchemcomm. 2018 Aug 24;9(10):1649-1662. doi: 10.1039/c8md00322j. eCollection 2018 Oct 1.

25.

Development and internal validation of the multivariable CIPHER (Collaborative Integrated Pregnancy High-dependency Estimate of Risk) clinical risk prediction model.

Payne BA, Ryan H, Bone J, Magee LA, Aarvold AB, Mark Ansermino J, Bhutta ZA, Bowen M, Guilherme Cecatti J, Chazotte C, Crozier T, de Pont AJM, Demirkiran O, Duan T, Kallen M, Ganzevoort W, Geary M, Goffman D, Hutcheon JA, Joseph KS, Lapinsky SE, Lataifeh I, Li J, Liskonova S, Hamel EM, McAuliffe FM, O'Herlihy C, Mol BWJ, Seaward PGR, Tadros R, Togal T, Qureshi R, Vivian Ukah U, Vasquez D, Wallace E, Yong P, Zhou V, Walley KR, von Dadelszen P; CIPHER Group.

Crit Care. 2018 Oct 30;22(1):278. doi: 10.1186/s13054-018-2215-6.

26.

Pleiotropic Benefits of the Angiotensin Receptor Blocker Candesartan in a Mouse Model of Alzheimer Disease.

Trigiani LJ, Royea J, Lacalle-Aurioles M, Tong XK, Hamel E.

Hypertension. 2018 Nov;72(5):1217-1226. doi: 10.1161/HYPERTENSIONAHA.118.11775.

PMID:
30354809
27.

Sterically induced conformational restriction: Discovery and preclinical evaluation of novel pyrrolo[3,2-d]pyrimidines as microtubule targeting agents.

Pavana RK, Shah K, Gentile T, Dybdal-Hargreaves NF, Risinger AL, Mooberry SL, Hamel E, Gangjee A.

Bioorg Med Chem. 2018 Nov 1;26(20):5470-5478. doi: 10.1016/j.bmc.2018.09.025. Epub 2018 Sep 21.

28.

Modified carbazoles destabilize microtubules and kill glioblastoma multiform cells.

Diaz P, Horne E, Xu C, Hamel E, Wagenbach M, Petrov RR, Uhlenbruck B, Haas B, Hothi P, Wordeman L, Gussio R, Stella N.

Eur J Med Chem. 2018 Nov 5;159:74-89. doi: 10.1016/j.ejmech.2018.09.026. Epub 2018 Sep 11.

29.

Design, synthesis, in vitro antiproliferative activity and apoptosis-inducing studies of 1-(3',4',5'-trimethoxyphenyl)-3-(2'-alkoxycarbonylindolyl)-2-propen-1-one derivatives obtained by a molecular hybridisation approach.

Preti D, Romagnoli R, Rondanin R, Cacciari B, Hamel E, Balzarini J, Liekens S, Schols D, Estévez-Sarmiento F, Quintana J, Estévez F.

J Enzyme Inhib Med Chem. 2018 Dec;33(1):1225-1238. doi: 10.1080/14756366.2018.1493473.

30.

Design, synthesis and preclinical evaluation of 5-methyl-N4-aryl-furo[2,3-d]pyrimidines as single agents with combination chemotherapy potential.

Devambatla RKV, Choudhary S, Ihnat M, Hamel E, Mooberry SL, Gangjee A.

Bioorg Med Chem Lett. 2018 Oct 1;28(18):3085-3093. doi: 10.1016/j.bmcl.2018.07.039. Epub 2018 Jul 27.

PMID:
30098869
31.

3-Aryl/Heteroaryl-5-amino-1-(3',4',5'-trimethoxybenzoyl)-1,2,4-triazoles as antimicrotubule agents. Design, synthesis, antiproliferative activity and inhibition of tubulin polymerization.

Romagnoli R, Prencipe F, Oliva P, Baraldi S, Baraldi PG, Brancale A, Ferla S, Hamel E, Bortolozzi R, Viola G.

Bioorg Chem. 2018 Oct;80:361-374. doi: 10.1016/j.bioorg.2018.06.037. Epub 2018 Jun 30.

PMID:
29986184
32.

Brain Perfusion and Astrocytes.

Cauli B, Hamel E.

Trends Neurosci. 2018 Jul;41(7):409-413. doi: 10.1016/j.tins.2018.04.010.

PMID:
29933772
33.

New 6- and 7-heterocyclyl-1H-indole derivatives as potent tubulin assembly and cancer cell growth inhibitors.

La Regina G, Bai R, Coluccia A, Naccarato V, Famiglini V, Nalli M, Masci D, Verrico A, Rovella P, Mazzoccoli C, Da Pozzo E, Cavallini C, Martini C, Vultaggio S, Dondio G, Varasi M, Mercurio C, Hamel E, Lavia P, Silvestri R.

Eur J Med Chem. 2018 May 25;152:283-297. doi: 10.1016/j.ejmech.2018.04.042. Epub 2018 Apr 25.

PMID:
29730191
34.

Structure based drug design and in vitro metabolism study: Discovery of N-(4-methylthiophenyl)-N,2-dimethyl-cyclopenta[d]pyrimidine as a potent microtubule targeting agent.

Xiang W, Choudhary S, Hamel E, Mooberry SL, Gangjee A.

Bioorg Med Chem. 2018 May 15;26(9):2437-2451. doi: 10.1016/j.bmc.2018.04.010. Epub 2018 Apr 4.

35.

Outcome of tacrolimus and vedolizumab after corticosteroid and anti-TNF failure in paediatric severe colitis.

Hamel B, Wu M, Hamel EO, Bass DM, Park KT.

BMJ Open Gastroenterol. 2018 Feb 14;5(1):e000195. doi: 10.1136/bmjgast-2017-000195. eCollection 2018.

36.

Transforming growth factor-β1 induces cerebrovascular dysfunction and astrogliosis through angiotensin II type 1 receptor-mediated signaling pathways.

Ongali B, Nicolakakis N, Tong XK, Lecrux C, Imboden H, Hamel E.

Can J Physiol Pharmacol. 2018 May;96(5):527-534. doi: 10.1139/cjpp-2017-0640. Epub 2018 Mar 5.

PMID:
29505736
37.

Quinazolinone-Based Anticancer Agents: Synthesis, Antiproliferative SAR, Antitubulin Activity, and Tubulin Co-crystal Structure.

Dohle W, Jourdan FL, Menchon G, Prota AE, Foster PA, Mannion P, Hamel E, Thomas MP, Kasprzyk PG, Ferrandis E, Steinmetz MO, Leese MP, Potter BVL.

J Med Chem. 2018 Feb 8;61(3):1031-1044. doi: 10.1021/acs.jmedchem.7b01474. Epub 2018 Jan 8.

PMID:
29227648
38.

2-Alkoxycarbonyl-3-arylamino-5-substituted thiophenes as a novel class of antimicrotubule agents: Design, synthesis, cell growth and tubulin polymerization inhibition.

Romagnoli R, Kimatrai Salvador M, Schiaffino Ortega S, Baraldi PG, Oliva P, Baraldi S, Lopez-Cara LC, Brancale A, Ferla S, Hamel E, Balzarini J, Liekens S, Mattiuzzo E, Basso G, Viola G.

Eur J Med Chem. 2018 Jan 1;143:683-698. doi: 10.1016/j.ejmech.2017.11.096.

39.

Targeting tubulin polymerization by novel 7-aryl-pyrroloquinolinones: Synthesis, biological activity and SARs.

Bortolozzi R, Mattiuzzo E, Dal Pra M, Sturlese M, Moro S, Hamel E, Carta D, Viola G, Ferlin MG.

Eur J Med Chem. 2018 Jan 1;143:244-258. doi: 10.1016/j.ejmech.2017.11.038. Epub 2017 Nov 20.

40.

In Vivo and Mechanistic Studies on Antitumor Lead 7-Methoxy-4-(2-methylquinazolin-4-yl)-3,4-dihydroquinoxalin-2(1H)-one and Its Modification as a Novel Class of Tubulin-Binding Tumor-Vascular Disrupting Agents.

Cui MT, Jiang L, Goto M, Hsu PL, Li L, Zhang Q, Wei L, Yuan SJ, Hamel E, Morris-Natschke SL, Lee KH, Xie L.

J Med Chem. 2017 Jul 13;60(13):5586-5598. doi: 10.1021/acs.jmedchem.7b00273. Epub 2017 Jun 27.

41.

An endothelial link between the benefits of physical exercise in dementia.

Trigiani LJ, Hamel E.

J Cereb Blood Flow Metab. 2017 Aug;37(8):2649-2664. doi: 10.1177/0271678X17714655. Epub 2017 Jun 15. Review.

42.

Design, synthesis, and structure-activity relationships of pyrimido[4,5-b]indole-4-amines as microtubule depolymerizing agents that are effective against multidrug resistant cells.

Devambatla RKV, Li W, Zaware N, Choudhary S, Hamel E, Mooberry SL, Gangjee A.

Bioorg Med Chem Lett. 2017 Aug 1;27(15):3423-3430. doi: 10.1016/j.bmcl.2017.05.085. Epub 2017 May 27.

43.

3-Aroyl-1,4-diarylpyrroles Inhibit Chronic Myeloid Leukemia Cell Growth through an Interaction with Tubulin.

La Regina G, Bai R, Coluccia A, Famiglini V, Passacantilli S, Naccarato V, Ortar G, Mazzoccoli C, Ruggieri V, Agriesti F, Piccoli C, Tataranni T, Nalli M, Brancale A, Vultaggio S, Mercurio C, Varasi M, Saponaro C, Sergio S, Maffia M, Coluccia AML, Hamel E, Silvestri R.

ACS Med Chem Lett. 2017 Apr 26;8(5):521-526. doi: 10.1021/acsmedchemlett.7b00022. eCollection 2017 May 11.

44.

12,13-Aziridinyl Epothilones. Stereoselective Synthesis of Trisubstituted Olefinic Bonds from Methyl Ketones and Heteroaromatic Phosphonates and Design, Synthesis, and Biological Evaluation of Potent Antitumor Agents.

Nicolaou KC, Rhoades D, Wang Y, Bai R, Hamel E, Aujay M, Sandoval J, Gavrilyuk J.

J Am Chem Soc. 2017 May 31;139(21):7318-7334. doi: 10.1021/jacs.7b02655. Epub 2017 May 17.

PMID:
28513142
45.

Angiotensin IV Receptors Mediate the Cognitive and Cerebrovascular Benefits of Losartan in a Mouse Model of Alzheimer's Disease.

Royea J, Zhang L, Tong XK, Hamel E.

J Neurosci. 2017 May 31;37(22):5562-5573. doi: 10.1523/JNEUROSCI.0329-17.2017. Epub 2017 May 5.

46.

Synthesis and Biological Evaluation of 2-Methyl-4,5-Disubstituted Oxazoles as a Novel Class of Highly Potent Antitubulin Agents.

Romagnoli R, Baraldi PG, Prencipe F, Oliva P, Baraldi S, Salvador MK, Lopez-Cara LC, Brancale A, Ferla S, Hamel E, Ronca R, Bortolozzi R, Mariotto E, Porcù E, Basso G, Viola G.

Sci Rep. 2017 Apr 13;7:46356. doi: 10.1038/srep46356.

47.

Synthesis of two fluorescent GTPγS molecules and their biological relevance.

Trans DJ, Bai R, Addison JB, Liu R, Hamel E, Coleman MA, Henderson PT.

Nucleosides Nucleotides Nucleic Acids. 2017 Jun 3;36(6):379-391. doi: 10.1080/15257770.2016.1231320. Epub 2017 Mar 10.

48.

Caspase vinyl sulfone small molecule inhibitors prevent axonal degeneration in human neurons and reverse cognitive impairment in Caspase-6-overexpressing mice.

Pakavathkumar P, Noël A, Lecrux C, Tubeleviciute-Aydin A, Hamel E, Ahlfors JE, LeBlanc AC.

Mol Neurodegener. 2017 Feb 28;12(1):22. doi: 10.1186/s13024-017-0166-z.

49.

Synthesis and Biological Evaluation of Benzocyclooctene-based and Indene-based Anticancer Agents that Function as Inhibitors of Tubulin Polymerization.

Herdman CA, Strecker TE, Tanpure RP, Chen Z, Winters A, Gerberich J, Liu L, Hamel E, Mason RP, Chaplin DJ, Trawick ML, Pinney KG.

Medchemcomm. 2016 Dec 1;7(12):2418-2427. doi: 10.1039/C6MD00459H. Epub 2016 Sep 22.

50.

Amyloid-β Oligomers Interact with Neurexin and Diminish Neurexin-mediated Excitatory Presynaptic Organization.

Naito Y, Tanabe Y, Lee AK, Hamel E, Takahashi H.

Sci Rep. 2017 Feb 13;7:42548. doi: 10.1038/srep42548.

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