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Publikationer i urvalet

26 träffar

Bibliografisk träff 2024-01-13

Identification and evaluation of small-molecule inhibitors against the dNTPase SAMHD1 via a comprehensive screening funnel.

Zhang SM, Paulin CBJ, Shu H, Yagüe-Capilla M, Michel M, Marttila P, Ortis F, Bwanika HC, Dirks C, Venkatram RP, Wiita E, Jemth AS, Almlöf I, Loseva O, Hormann FM, Koolmeister T, Linde E, Lee S, Llona-Minguez S, Haraldsson M, Axelsson H, Strömberg K, Homan EJ, Scobie M, Lundbäck T, Helleday T, Rudd SG.

iScience · research-article; journal article · DOI 10.1016/j.isci.2024.108907

Bibliografisk träff 2023-07-19

A preclinical secondary pharmacology resource illuminates target-adverse drug reaction associations of marketed drugs.

Sutherland JJ, Yonchev D, Fekete A, Urban L.

Nat Commun · research support, non-u.s. gov't; research-article; journal article · DOI 10.1038/s41467-023-40064-9

Bibliografisk träff 2017-08-24

A prodrug design for improved oral absorption and reduced hepatic interaction.

Ahmed G, Elger W, Meece F, Nair HB, Schneider B, Wyrwa R, Nickisch K.

Bioorg Med Chem · journal article · DOI 10.1016/j.bmc.2017.08.027

Bibliografisk träff 2017-07-11

Structure-Based Approach To Identify 5-[4-Hydroxyphenyl]pyrrole-2-carbonitrile Derivatives as Potent and Tissue Selective Androgen Receptor Modulators.

Unwalla R, Mousseau JJ, Fadeyi OO, Choi C, Parris K, Hu B, Kenney T, Chippari S, McNally C, Vishwanathan K, Kilbourne E, Thompson C, Nagpal S, Wrobel J, Yudt M, Morris CA, Powell D, Gilbert AM, Chekler ELP.

J Med Chem · journal article · DOI 10.1021/acs.jmedchem.7b00373

Bibliografisk träff 2017-04-13

Synthesis and biological evaluation of novel selective androgen receptor modulators (SARMs) Part III: Discovery of 4-(5-oxopyrrolidine-1-yl)benzonitrile derivative 2f as a clinical candidate.

Aikawa K, Asano M, Ono K, Habuka N, Yano J, Wilson K, Fujita H, Kandori H, Hara T, Morimoto M, Santou T, Yamaoka M, Nakayama M, Hasuoka A.

Bioorg Med Chem · journal article · DOI 10.1016/j.bmc.2017.04.018

Bibliografisk träff 2014-08-26

3-alkoxy-pyrrolo[1,2-b]pyrazolines as selective androgen receptor modulators with ideal physicochemical properties for transdermal administration.

Ullrich T, Sasmal S, Boorgu V, Pasagadi S, Cheera S, Rajagopalan S, Bhumireddy A, Shashikumar D, Chelur S, Belliappa C, Pandit C, Krishnamurthy N, Mukherjee S, Ramanathan A, Ghadiyaram C, Ramachandra M, Santos PG, Lagu B, Bock MG, Perrone MH, Weiler S, Keller H.

J Med Chem · journal article · DOI 10.1021/jm5009049

Bibliografisk träff 2014-03-10

1-(2-Hydroxy-2-methyl-3-phenoxypropanoyl)indoline-4-carbonitrile derivatives as potent and tissue selective androgen receptor modulators.

Piatnitski Chekler EL, Unwalla R, Khan TA, Tangirala RS, Johnson M, St Andre M, Anderson JT, Kenney T, Chiparri S, McNally C, Kilbourne E, Thompson C, Nagpal S, Weber G, Schelling S, Owens J, Morris CA, Powell D, Verhoest PR, Gilbert AM.

J Med Chem · journal article · DOI 10.1021/jm401625b

Bibliografisk träff 2013-04-09

Structure-based identification of OATP1B1/3 inhibitors.

De Bruyn T, van Westen GJ, Ijzerman AP, Stieger B, de Witte P, Augustijns PF, Annaert PP.

Mol Pharmacol · research support, non-u.s. gov't; journal article · DOI 10.1124/mol.112.084152

Bibliografisk träff 2012-09-25

Discovery of diarylhydantoins as new selective androgen receptor modulators.

Nique F, Hebbe S, Peixoto C, Annoot D, Lefrançois JM, Duval E, Michoux L, Triballeau N, Lemoullec JM, Mollat P, Thauvin M, Prangé T, Minet D, Clément-Lacroix P, Robin-Jagerschmidt C, Fleury D, Guédin D, Deprez P.

J Med Chem · journal article · DOI 10.1021/jm300249m

Bibliografisk träff 2012-09-25

Identification of a 4-(hydroxymethyl)diarylhydantoin as a selective androgen receptor modulator.

Nique F, Hebbe S, Triballeau N, Peixoto C, Lefrançois JM, Jary H, Alvey L, Manioc M, Housseman C, Klaassen H, Van Beeck K, Guédin D, Namour F, Minet D, Van der Aar E, Feyen J, Fletcher S, Blanqué R, Robin-Jagerschmidt C, Deprez P.

J Med Chem · journal article · DOI 10.1021/jm300281x

Bibliografisk träff 2010-01-01

Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.

Fourches D, Barnes JC, Day NC, Bradley P, Reed JZ, Tropsha A.

Chem Res Toxicol · research-article; research support, u.s. gov't, non-p.h.s.; journal article; research support, n.i.h., extramural · DOI 10.1021/tx900326k

Bibliografisk träff 2009-06-01

Nonsteroidal selective androgen receptor modulators (SARMs): dissociating the anabolic and androgenic activities of the androgen receptor for therapeutic benefit.

Mohler ML, Bohl CE, Jones A, Coss CC, Narayanan R, He Y, Hwang DJ, Dalton JT, Miller DD.

J Med Chem · review; journal article · DOI 10.1021/jm900280m

Bibliografisk träff 2007-07-18

Design, synthesis, and in vivo SAR of a novel series of pyrazolines as potent selective androgen receptor modulators.

Zhang X, Li X, Allan GF, Sbriscia T, Linton O, Lundeen SG, Sui Z.

J Med Chem · journal article · DOI 10.1021/jm0613976

Bibliografisk träff 2007-06-07

Discovery of potent and muscle selective androgen receptor modulators through scaffold modifications.

Li JJ, Sutton JC, Nirschl A, Zou Y, Wang H, Sun C, Pi Z, Johnson R, Krystek SR, Seethala R, Golla R, Sleph PG, Beehler BC, Grover GJ, Fura A, Vyas VP, Li CY, Gougoutas JZ, Galella MA, Zahler R, Ostrowski J, Hamann LG.

J Med Chem · journal article · DOI 10.1021/jm070312d

Bibliografisk träff 2007-06-06

Synthesis and SAR of tetrahydropyrrolo[1,2-b][1,2,5]thiadiazol-2(3H)-one 1,1-dioxide analogues as highly potent selective androgen receptor modulators.

Manfredi MC, Bi Y, Nirschl AA, Sutton JC, Seethala R, Golla R, Beehler BC, Sleph PG, Grover GJ, Ostrowski J, Hamann LG.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2007.06.007

Bibliografisk träff 2006-12-01

Discovery of potent, orally-active, and muscle-selective androgen receptor modulators based on an N-aryl-hydroxybicyclohydantoin scaffold.

Sun C, Robl JA, Wang TC, Huang Y, Kuhns JE, Lupisella JA, Beehler BC, Golla R, Sleph PG, Seethala R, Fura A, Krystek SR, An Y, Malley MF, Sack JS, Salvati ME, Grover GJ, Ostrowski J, Hamann LG.

J Med Chem · journal article · DOI 10.1021/jm061101w

Bibliografisk träff 2006-10-17

Serendipitous discovery of novel imidazolopyrazole scaffold as selective androgen receptor modulators.

Zhang X, Li X, Allan GF, Sbriscia T, Linton O, Lundeen SG, Sui Z.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2006.10.035

Bibliografisk träff 2006-09-07

Synthesis and SAR of novel hydantoin derivatives as selective androgen receptor modulators.

Zhang X, Allan GF, Sbriscia T, Linton O, Lundeen SG, Sui Z.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2006.08.084

Bibliografisk träff 2005-09-01

Impact of induced fit on ligand binding to the androgen receptor: a multidimensional QSAR study to predict endocrine-disrupting effects of environmental chemicals.

Lill MA, Winiger F, Vedani A, Ernst B.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm050403f

Bibliografisk träff 2004-12-01

Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.

Matthews EJ, Kruhlak NL, Weaver JL, Benz RD, Contrera JF.

Curr Drug Discov Technol · journal article · DOI 10.2174/1570163043334794

Bibliografisk träff 2004-10-01

Design and synthesis of aryl diphenolic azoles as potent and selective estrogen receptor-beta ligands.

Malamas MS, Manas ES, McDevitt RE, Gunawan I, Xu ZB, Collini MD, Miller CP, Dinh T, Henderson RA, Keith JC, Harris HA.

J Med Chem · journal article · DOI 10.1021/jm049719y

Bibliografisk träff 2003-06-01

Three dimensional pharmacophore modeling of human CYP17 inhibitors. Potential agents for prostate cancer therapy.

Clement OO, Freeman CM, Hartmann RW, Handratta VD, Vasaitis TS, Brodie AM, Njar VC.

J Med Chem · research support, u.s. gov't, p.h.s.; research support, non-u.s. gov't; journal article · DOI 10.1021/jm020576u

Bibliografisk träff 2002-08-01

Synthesis and evaluation of 2'-substituted 4-(4'-carboxy- or 4'-carboxymethylbenzylidene)-N-acylpiperidines: highly potent and in vivo active steroid 5alpha-reductase type 2 inhibitors.

Picard F, Barassin S, Mokhtarian A, Hartmann RW.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm0208471

Bibliografisk träff 1991-09-01

New aromatase inhibitors. Synthesis and biological activity of pyridyl-substituted tetralone derivatives.

Bayer H, Batzl C, Hartmann RW, Mannschreck A.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm00113a004

Bibliografisk träff 1985-12-01

Antiandrogenic activity of a series of des-A-steroid derivatives.

Morales-Alanis H, Brienne MJ, Jacques J, Bouton MM, Nédélec L, Torelli V, Tournemine C.

J Med Chem · comparative study; journal article · DOI 10.1021/jm00150a009

Bibliografisk träff 1979-10-01

Syntheses and biological activities of 7 beta-methyl steroids.

Chiu WH, Wolff ME.

J Med Chem · research support, u.s. gov't, p.h.s.; journal article · DOI 10.1021/jm00196a020