R. Steensma

发表

Piperazine-based CCR5 antagonists as HIV-1 inhibitors. I: 2(S)-methyl piperazine as a key pharmacophore element.

S. Mccombie, J. Tagat, J. Liu, 2001, Bioorganic & medicinal chemistry letters.

Piperazine-based CCR5 antagonists as HIV-1 inhibitors. III: synthesis, antiviral and pharmacokinetic profiles of symmetrical heteroaryl carboxamides.

B. Neustadt, M. Endres, A. Palani, 2003, Bioorganic & medicinal chemistry letters.

Inhibition of the development of collagen-induced arthritis in rhesus monkeys by a small molecular weight antagonist of CCR5.

S. Narula, E. Remarque, B. Hart, 2005, Arthritis and rheumatism.

Structure of the coat protein in fd filamentous bacteriophage particles determined by solid-state NMR spectroscopy

Sungjoon Kim, Jiqing Jiang, Jonathan S. Melnick, 2007 .

Fragment-based discovery of JAK-2 inhibitors.

M. Wilson, P. Sprengeler, S. Antonysamy, 2008, Bioorganic & medicinal chemistry letters.

Ternary complex of human RORγ ligand‐binding domain, inverse agonist and SMRT peptide shows a unique mechanism of corepressor recruitment

R. Babine, Shin‐ichi Hirashima, Makoto Shiozaki, 2017, Genes to cells : devoted to molecular & cellular mechanisms.

Piperazine-based CCR5 antagonists as HIV-1 inhibitors. II. Discovery of 1-[(2,4-dimethyl-3-pyridinyl)carbonyl]-4- methyl-4-[3(S)-methyl-4-[1(S)-[4-(trifluoromethyl)phenyl]ethyl]-1-piperazinyl]- piperidine N1-oxide (Sch-350634), an orally bioavailable, potent CCR5 antagonist.

B. Neustadt, K. Cox, M. Murray, 2001, Journal of medicinal chemistry.

Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK

Peter G. Schultz, Yi Liu, Jiqing Jiang, 2007, Proceedings of the National Academy of Sciences.

Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2

Sungjoon Kim, Nanxin Li, M. Warmuth, 2013, Journal of medicinal chemistry.

Piperazine-based CCR5 antagonists as HIV-1 inhibitors. IV. Discovery of 1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]- 4-[4-[2-methoxy-1(R)-4-(trifluoromethyl)phenyl]ethyl-3(S)-methyl-1-piperazinyl]- 4-methylpiperidine (Sch-417690/Sch-D), a potent, highly selective, and orally bioavailable CCR5 antagonis

J. Lachowicz, K. Cox, G. Varty, 2004, Journal of medicinal chemistry.

SAR Exploration Guided by LE and Fsp(3): Discovery of a Selective and Orally Efficacious RORγ Inhibitor.

R. Babine, Shin‐ichi Hirashima, Hiromasa Hashimoto, 2016, ACS medicinal chemistry letters.