Browse by Journal Title

2023

Structure-based design of xanthine-imidazopyridines and -imidazothiazoles as highly potent and in vivo efficacious tryptophan hydroxylase inhibitors.
Specker, E. and Wesolowski, R. and Schütz, A. and Matthes, S. and Mallow, K. and Wasinska-Kalwa, M. and Winkler, L. and Oder, A. and Alenina, N. and Pleimes, D. and von Kries, J.P. and Heinemann, U. and Bader, M. and Nazaré, M.
Journal of Medicinal Chemistry 66 (21): 14866-14896. 9 November 2023

Leveraging ligand affinity and properties: discovery of novel benzamide-type cereblon binders for the design of PROTACs.
Steinebach, C. and Bricelj, A. and Murgai, A. and Sosič, I. and Bischof, L. and Ng, Y.L.D. and Heim, C. and Maiwald, S. and Proj, M. and Voget, R. and Feller, F. and Košmrlj, J. and Sapozhnikova, V. and Schmidt, A. and Zuleeg, M.R. and Lemnitzer, P. and Mertins, P. and Hansen, F.K. and Gütschow, M. and Krönke, J. and Hartmann, M.D.
Journal of Medicinal Chemistry 66 (21): 14513-14543. 9 November 2023

2022

Structure-based design of xanthine-benzimidazole derivatives as novel and potent tryptophan hydroxylase inhibitors.
Specker, E. and Matthes, S. and Wesolowski, R. and Schütz, A. and Grohmann, M. and Alenina, N. and Pleimes, D. and Mallow, K. and Neuenschwander, M. and Gogolin, A. and Weise, M. and Pfeifer, J. and Ziebart, N. and Heinemann, U. and von Kries, J.P. and Nazaré, M. and Bader, M.
Journal of Medicinal Chemistry 65 (16): 11126-11149. 25 August 2022

Rational design of highly potent, selective, and bioavailable SGK1 protein kinase inhibitors for the treatment of osteoarthritis.
Halland, N. and Schmidt, F. and Weiss, T. and Li, Z. and Czech, J. and Saas, J. and Ding-Pfennigdorff, D. and Dreyer, M.K. and Strübing, C. and Nazare, M.
Journal of Medicinal Chemistry 65 (2): 1567-1584. 27 January 2022

2021

Development of a 1,2,4-triazole-based lead tankyrase inhibitor: part II.
Leenders, R.G.G. and Brinch, S.A. and Sowa, S.T. and Amundsen-Isaksen, E. and Galera-Prat, A. and Murthy, S. and Aertssen, S. and Smits, J.N. and Nieczypor, P. and Damen, E. and Wegert, A. and Nazaré, M. and Lehtiö, L. and Waaler, J. and Krauss, S.
Journal of Medicinal Chemistry 64 (24): 17936-17949. 23 December 2021

Enhanced properties of a benzimidazole benzylpyrazole lysine demethylase inhibitor: mechanism-of-action, binding site analysis, and activity in cellular models of prostate cancer.
Carter, D.M. and Specker, E. and Malecki, P.H. and Przygodda, J. and Dudaniec, K. and Weiss, M.S. and Heinemann, U. and Nazaré, M. and Gohlke, U.
Journal of Medicinal Chemistry 64 (19): 14266-14282. 14 October 2021

A versatile sub-nanomolar fluorescent ligand enables NanoBRET binding studies and single-molecule microscopy at the histamine H(3) receptor.
Rosier, N. and Grätz, L. and Schihada, H. and Möller, J. and Işbilir, A. and Humphrys, L.J. and Nagl, M. and Seibel, U. and Lohse, M.J. and Pockes, S.
Journal of Medicinal Chemistry 64 (15): 11695-11708. 12 August 2021

2020

From pyrazolones to azaindoles: evolution of active-site SHP2 inhibitors based on scaffold hopping and bioisosteric replacement.
Mostinski, Y. and Heynen, G.J.J.E. and López-Alberca, M.P. and Paul, J. and Miksche, S. and Radetzki, S. and Schaller, D. and Shanina, E. and Seyffarth, C. and Kolomeets, Y. and Ziebart, N. and de Schryver, J. and Oestreich, S. and Neuenschwander, M. and Roske, Y. and Heinemann, U. and Rademacher, C. and Volkamer, A. and von Kries, J.P. and Birchmeier, W. and Nazaré, M.
Journal of Medicinal Chemistry 63 (23): 14780-14804. 10 December 2020

Preclinical lead optimization of a 1,2,4-triazole based tankyrase inhibitor.
Waaler, J. and Leenders, R. and Sowa, S.T. and Alam Brinch, S. and Lycke, M. and Nieczypor, P. and Aertssen, S. and Murthy, S. and Galera-Prat, A. and Damen, E. and Wegert, A. and Nazare, M. and Lehtiö, L. and Krauss, S.
Journal of Medicinal Chemistry 63 (13): 6834-6846. 9 July 2020

2019

Development of robust 17(R),18(S)-epoxyeicosatetraenoic acid (17,18-EEQ) analogues as potential clinical antiarrhythmic agents.
Adebesin, A.M. and Wesser, T. and Vijaykumar, J. and Konkel, A. and Paudyal, M. and Lossie, J. and Zhu, C. and Westphal, C. and Puli, N. and Fischer, R. and Schunck, W.H. and Falck, J.
Journal of Medicinal Chemistry 62 (22): 10124-10143. 27 November 2019

2017

Discovery of a novel series of tankyrase inhibitors by a hybridization approach.
Anumala, U.R. and Waaler, J. and Nkizinkiko, Y. and Ignatev, A. and Lazarow, K. and Lindemann, P. and Olsen, P.A. and Murthy, S. and Obaji, E. and Majouga, A.G. and Leonov, S. and von Kries, J.P. and Lehtiö, L. and Krauss, S. and Nazaré, M.
Journal of Medicinal Chemistry 60 (24): 10013-10025. 28 December 2017

2015

Ethyl 2-((4-chlorophenyl)amino)thiazole-4-carboxylate and derivatives are potent inducers of Oct3/4.
Cheng, X. and Yoshida, H. and Raoofi, D. and Saleh, S. and Alborzinia, H. and Wenke, F. and Goehring, A. and Reuter, S. and Mah, N. and Fuchs, H.R. and Andrade-Navarro, M.A. and Adjaye, J. and Gul, S. and Utikal, J. and Mrowka, R. and Woelfl, S.
Journal of Medicinal Chemistry 58 (1): 5742-5750. 13 August 2015

Identification of 2-[4-[(4-methoxyphenyl)methoxy]-phenyl]acetonitrile and derivatives as potent Oct3/4 inducers.
Cheng, X. and Dimou, E. and Alborzinia, H. and Wenke, F. and Goehring, A. and Reuter, S. and Mah, N. and Fuchs, H. and Andrade-Navarro, M.A. and Adjaye, J. and Gul, S. and Harms, C. and Utikal, J. and Klipp, E. and Mrowka, R. and Woelfl, S.
Journal of Medicinal Chemistry 58 (12): 4976-4983. 25 June 2015

2013

Structural characterization of amorfrutins bound to the peroxisome proliferator-activated receptor γ.
de Groot, J.C. and Weidner, C. and Krausze, J. and Kawamoto, K. and Schroeder, F.C. and Sauer, S. and Büssow, K.
Journal of Medicinal Chemistry 56 (4): 1535-1543. 28 February 2013

2011

17(R),18(S)-epoxyeicosatetraenoic acid, a potent eicosapentaenoic acid (EPA) derived regulator of cardiomyocyte contraction: structure-activity relationships and stable analogues.
Falck, J.R. and Wallukat, G. and Puli, N. and Goli, M. and Arnold, C. and Konkel, A. and Rothe, M. and Fischer, R. and Mueller, D.N. and Schunck, W.H.
Journal of Medicinal Chemistry 54 (12): 4109-4118. 23 June 2011

Elucidation of a structural basis for the inhibitor-driven, p62 (SQSTM1)-dependent intracellular redistribution of cAMP phosphodiesterase-4A4 (PDE4A4).
Day, J.P. and Lindsay, B. and Riddell, T. and Jiang, Z. and Allcock, R.W. and Abraham, A. and Sookup, S. and Christian, F. and Bogum, J. and Martin, E.K. and Rae, R.L. and Anthony, D. and Rosair, G.M. and Houslay, D.M. and Huston, E. and Baillie, G.S. and Klussmann, E. and Houslay, M.D. and Adams, D.R.
Journal of Medicinal Chemistry 54 (9): 3331-3347. 12 May 2011

2005

Synthesis and biological evaluation of spin-labeled alkylphospholipid analogs.
Mravljak, J. and Zeisig, R. and Pecar, S.
Journal of Medicinal Chemistry 48 (20): 6393-6399. 6 October 2005

Quinols as novel therapeutic agents. 2.(1) 4-(1-arylsulfonylindol-2-yl)-4-hydroxycyclohexa-2,5-dien-1-ones and related agents as potent and selective antitumor agents.
Berry, J.M. and Bradshaw, T.D. and Fichtner, I. and Ren, R. and Schwalbe, C.H. and Wells, G. and Chew, E.H. and Stevens, M.F. and Westwell, A.D.
Journal of Medicinal Chemistry 48 : 639-644. 27 January 2005

2004

PDBLIG: classification of small molecular protein binding in the Protein Data Bank.
Chalk, A.J. and Worth, C.L. and Overington, J.P. and Chan, A.W.E.
Journal of Medicinal Chemistry 47 (15): 3807-3816. 15 July 2004

2002

Probing the cysteine-34 position of endogenous serum albumin with thiol-binding doxorubicin derivatives. Improved efficacy of an acid-sensitive doxorubicin derivative with specific albumin-binding properties compared to that of the parent compound.
Kratz, F. and Warnecke, A. and Scheuermann, K. and Stockmar, C. and Schwab, J. and Lazar, P. and Drueckes, P. and Esser, N. and Drevs, J. and Rognan, D. and Bissantz, C. and Hinderling, C. and Folkers, G. and Fichtner, I. and Unger, C.
Journal of Medicinal Chemistry 45 (25): 5523-5533. 5 December 2002

1998

Newly synthesized L-enantiomers of 3'-fluoro-modified beta-2'- deoxyribonucleoside 5'-triphosphates inhibit hepatitis B DNA polymerases but not the five cellular DNA polymerases alpha, beta, gamma, delta and epsilon nor HIV-1 reverse transcriptase.
von Janta-Lipinski, M. and Costisella, B. and Ochs, H. and Huebscher, U. and Hafkemeyer, P. and Matthes, E.
Journal of Medicinal Chemistry 41 : 2040-2046. 1 January 1998

1996

Antitumor benzothiazoles. 3. Synthesis of 2-(4-aminophenyl)benzothiazoles and evaluation of their activities against breast cancer cell lines in vitro and in vivo.
Shi, D.F. and Bradshaw, T.D. and Wrigley, S. and McCall, C.J. and Lelieveld, P. and Fichtner, I. and Stevens, M.F.G.
Journal of Medicinal Chemistry 39 : 3375-3384. 1 January 1996