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Publikationer i urvalet

39 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 2022-08-08

An overview on Estrogen receptors signaling and its ligands in breast cancer.

Khan MZI, Uzair M, Nazli A, Chen JZ.

Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2022.114658

Bibliografisk träff 2017-05-30

Combating breast cancer with non-steroidal aromatase inhibitors (NSAIs): Understanding the chemico-biological interactions through comparative SAR/QSAR study.

Adhikari N, Amin SA, Saha A, Jha T.

Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2017.05.041

Bibliografisk träff 2016-01-19

Recent Progress in the Discovery of Next Generation Inhibitors of Aromatase from the Structure-Function Perspective.

Ghosh D, Lo J, Egbuta C.

J Med Chem · research support, non-u.s. gov't; research-article; review; journal article; research support, n.i.h., extramural · DOI 10.1021/acs.jmedchem.5b01281

Bibliografisk träff 2015-10-02

Discovery of 4-Aryl-5,6,7,8-tetrahydroisoquinolines as Potent, Selective, and Orally Active Aldosterone Synthase (CYP11B2) Inhibitors: In Vivo Evaluation in Rodents and Cynomolgus Monkeys.

Martin RE, Aebi JD, Hornsperger B, Krebs HJ, Kuhn B, Kuglstatter A, Alker AM, Märki HP, Müller S, Burger D, Ottaviani G, Riboulet W, Verry P, Tan X, Amrein K, Mayweg AV.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.5b00851

Bibliografisk träff 2015-07-17

Discovery of Triazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.

Hoyt SB, Petrilli W, London C, Liang GB, Tata J, Hu Q, Yin L, van Koppen CJ, Hartmann RW, Struthers M, Wisniewski T, Ren N, Bopp C, Sok A, Cai TQ, Stribling S, Pai LY, Ma X, Metzger J, Verras A, McMasters D, Chen Q, Tung E, Tang W, Salituro G, Buist N, Clemas J, Zhou G, Gibson J, Maxwell CA, Lassman M, McLaughlin T, Castro-Perez J, Szeto D, Forrest G, Hajdu R, Rosenbach M, Xiong Y.

ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/acsmedchemlett.5b00048

Bibliografisk träff 2015-04-07

Discovery of Benzimidazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.

Hoyt SB, Park MK, London C, Xiong Y, Tata J, Bennett DJ, Cooke A, Cai J, Carswell E, Robinson J, MacLean J, Brown L, Belshaw S, Clarkson TR, Liu K, Liang GB, Struthers M, Cully D, Wisniewski T, Ren N, Bopp C, Sok A, Cai TQ, Stribling S, Pai LY, Ma X, Metzger J, Verras A, McMasters D, Chen Q, Tung E, Tang W, Salituro G, Buist N, Kuethe J, Rivera N, Clemas J, Zhou G, Gibson J, Maxwell CA, Lassman M, McLaughlin T, Castro-Perez J, Szeto D, Forrest G, Hajdu R, Rosenbach M, Ali A.

ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/acsmedchemlett.5b00054

Bibliografisk träff 2015-03-03

Novel pyridyl substituted 4,5-dihydro-[1,2,4]triazolo[4,3-a]quinolines as potent and selective aldosterone synthase inhibitors with improved in vitro metabolic stability.

Hu Q, Yin L, Ali A, Cooke AJ, Bennett J, Ratcliffe P, Lo MM, Metzger E, Hoyt S, Hartmann RW.

J Med Chem · journal article · DOI 10.1021/acs.jmedchem.5b00079

Bibliografisk träff 2014-12-13

Heteroatom insertion into 3,4-dihydro-1H-quinolin-2-ones leads to potent and selective inhibitors of human and rat aldosterone synthase.

Grombein CM, Hu Q, Rau S, Zimmer C, Hartmann RW.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2014.12.022

Bibliografisk träff 2014-10-12

1-Phenylsulfinyl-3-(pyridin-3-yl)naphthalen-2-ols: a new class of potent and selective aldosterone synthase inhibitors.

Grombein CM, Hu Q, Heim R, Rau S, Zimmer C, Hartmann RW.

Eur J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.ejmech.2014.10.027

Bibliografisk träff 2014-06-05

Novel pyridyl- or isoquinolinyl-substituted indolines and indoles as potent and selective aldosterone synthase inhibitors.

Yin L, Hu Q, Emmerich J, Lo MM, Metzger E, Ali A, Hartmann RW.

J Med Chem · journal article · DOI 10.1021/jm500140c

Bibliografisk träff 2014-01-24

Aldosterone synthase inhibitors as promising treatments for mineralocorticoid dependent cardiovascular and renal diseases.

Hu Q, Yin L, Hartmann RW.

J Med Chem · journal article · DOI 10.1021/jm401430e

Bibliografisk träff 2013-07-29

Highly potent and selective nonsteroidal dual inhibitors of CYP17/CYP11B2 for the treatment of prostate cancer to reduce risks of cardiovascular diseases.

Pinto-Bazurco Mendieta MA, Hu Q, Engel M, Hartmann RW.

J Med Chem · journal article · DOI 10.1021/jm400484p

Bibliografisk träff 2013-02-12

Modulation of cytochromes P450 with xanthone-based molecules: from aromatase to aldosterone synthase and steroid 11β-hydroxylase inhibition.

Gobbi S, Hu Q, Negri M, Zimmer C, Belluti F, Rampa A, Hartmann RW, Bisi A.

J Med Chem · journal article · DOI 10.1021/jm301844q

Bibliografisk träff 2013-01-03

Tetrahydropyrroloquinolinone type dual inhibitors of aromatase/aldosterone synthase as a novel strategy for breast cancer patients with elevated cardiovascular risks.

Yin L, Hu Q, Hartmann RW.

J Med Chem · journal article · DOI 10.1021/jm301408t

Bibliografisk träff 2012-08-03

Selective dual inhibitors of CYP19 and CYP11B2: targeting cardiovascular diseases hiding in the shadow of breast cancer.

Hu Q, Yin L, Hartmann RW.

J Med Chem · journal article · DOI 10.1021/jm3004637

Bibliografisk träff 2012-07-12

Novel imidazol-1-ylmethyl substituted 1,2,5,6-tetrahydropyrrolo[3,2,1-ij]quinolin-4-ones as potent and selective CYP11B1 inhibitors for the treatment of Cushing's syndrome.

Yin L, Lucas S, Maurer F, Kazmaier U, Hu Q, Hartmann RW.

J Med Chem · journal article · DOI 10.1021/jm3003872

Bibliografisk träff 2012-02-11

Optimization of the aromatase inhibitory activities of pyridylthiazole analogues of resveratrol.

Mayhoub AS, Marler L, Kondratyuk TP, Park EJ, Pezzuto JM, Cushman M.

Bioorg Med Chem · journal article · DOI 10.1016/j.bmc.2012.01.047

Bibliografisk träff 2011-03-08

Fine-tuning the selectivity of aldosterone synthase inhibitors: structure-activity and structure-selectivity insights from studies of heteroaryl substituted 1,2,5,6-tetrahydropyrrolo[3,2,1-ij]quinolin-4-one derivatives.

Lucas S, Negri M, Heim R, Zimmer C, Hartmann RW.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm101470k

Bibliografisk träff 2011-02-22

Design, synthesis, and biological evaluation of imidazolyl derivatives of 4,7-disubstituted coumarins as aromatase inhibitors selective over 17-α-hydroxylase/C17-20 lyase.

Stefanachi A, Favia AD, Nicolotti O, Leonetti F, Pisani L, Catto M, Zimmer C, Hartmann RW, Carotti A.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm101120u

Bibliografisk träff 2010-11-12

N-(Pyridin-3-yl)benzamides as selective inhibitors of human aldosterone synthase (CYP11B2).

Zimmer C, Hafner M, Zender M, Ammann D, Hartmann RW, Vock CA.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2010.11.040

Bibliografisk träff 2010-07-01

Novel highly potent and selective nonsteroidal aromatase inhibitors: synthesis, biological evaluation and structure-activity relationships investigation.

Gobbi S, Zimmer C, Belluti F, Rampa A, Hartmann RW, Recanatini M, Bisi A.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm100319h

Bibliografisk träff 2010-04-08

Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).

Muftuoglu Y, Mustata G.

Bioorg Med Chem Lett · research support, u.s. gov't, non-p.h.s.; journal article · DOI 10.1016/j.bmcl.2010.03.113

Bibliografisk träff 2008-12-01

In vivo active aldosterone synthase inhibitors with improved selectivity: lead optimization providing a series of pyridine substituted 3,4-dihydro-1H-quinolin-2-one derivatives.

Lucas S, Heim R, Ries C, Schewe KE, Birk B, Hartmann RW.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm800888q

Bibliografisk träff 2008-09-03

Novel aldosterone synthase inhibitors with extended carbocyclic skeleton by a combined ligand-based and structure-based drug design approach.

Lucas S, Heim R, Negri M, Antes I, Ries C, Schewe KE, Bisi A, Gobbi S, Hartmann RW.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm800683c

Bibliografisk träff 2008-08-26

CYP19 (aromatase): exploring the scaffold flexibility for novel selective inhibitors.

Castellano S, Stefancich G, Ragno R, Schewe K, Santoriello M, Caroli A, Hartmann RW, Sbardella G.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2008.08.046

Bibliografisk träff 2008-08-01

Overcoming undesirable CYP1A2 inhibition of pyridylnaphthalene-type aldosterone synthase inhibitors: influence of heteroaryl derivatization on potency and selectivity.

Heim R, Lucas S, Grombein CM, Ries C, Schewe KE, Negri M, Müller-Vieira U, Birk B, Hartmann RW.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm800377h

Bibliografisk träff 2007-06-22

Imidazolylmethylbenzophenones as highly potent aromatase inhibitors.

Gobbi S, Cavalli A, Negri M, Schewe KE, Belluti F, Piazzi L, Hartmann RW, Recanatini M, Bisi A.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm0702938

Bibliografisk träff 2006-07-01

Lead optimization providing a series of flavone derivatives as potent nonsteroidal inhibitors of the cytochrome P450 aromatase enzyme.

Gobbi S, Cavalli A, Rampa A, Belluti F, Piazzi L, Paluszcak A, Hartmann RW, Recanatini M, Bisi A.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm060186y