Optimization of pyrazole inhibitors of Coactivator Associated Arginine Methyltransferase 1 (CARM1)

Tram Huynh, Zhong Chen, Suhong Pang, Jieping Geng, Tiziano Bandiera, Simona Bindi, Paola Vianello, Fulvia Roletto, Sandrine Thieffine, Arturo Galvani, Wayne Vaccaro, Michael A. Poss, George L. Trainor, Matthew V. Lorenzi, Marco Gottardis, Lata Jayaraman, Ashok V. Purandare

Research output: Contribution to journalArticle

62 Citations (Scopus)

Abstract

Design, synthesis, and SAR development led to the identification of the potent, novel, and selective pyrazole based inhibitor (7f) of Coactivator Associated Arginine Methyltransferase (CARM1).

Original languageEnglish
Pages (from-to)2924-2927
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume19
Issue number11
DOIs
Publication statusPublished - Jun 1 2009

Fingerprint

coactivator-associated arginine methyltransferase 1
human PRMT2 protein
pyrazole

Keywords

  • CARM1
  • Coactivator associated arginine methyltransferase 1
  • Methyltransferase
  • PRMT4
  • Pyrazole

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry
  • Molecular Medicine
  • Molecular Biology
  • Clinical Biochemistry
  • Biochemistry

Cite this

Optimization of pyrazole inhibitors of Coactivator Associated Arginine Methyltransferase 1 (CARM1). / Huynh, Tram; Chen, Zhong; Pang, Suhong; Geng, Jieping; Bandiera, Tiziano; Bindi, Simona; Vianello, Paola; Roletto, Fulvia; Thieffine, Sandrine; Galvani, Arturo; Vaccaro, Wayne; Poss, Michael A.; Trainor, George L.; Lorenzi, Matthew V.; Gottardis, Marco; Jayaraman, Lata; Purandare, Ashok V.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 19, No. 11, 01.06.2009, p. 2924-2927.

Research output: Contribution to journalArticle

Huynh, T, Chen, Z, Pang, S, Geng, J, Bandiera, T, Bindi, S, Vianello, P, Roletto, F, Thieffine, S, Galvani, A, Vaccaro, W, Poss, MA, Trainor, GL, Lorenzi, MV, Gottardis, M, Jayaraman, L & Purandare, AV 2009, 'Optimization of pyrazole inhibitors of Coactivator Associated Arginine Methyltransferase 1 (CARM1)', Bioorganic and Medicinal Chemistry Letters, vol. 19, no. 11, pp. 2924-2927. https://doi.org/10.1016/j.bmcl.2009.04.075
Huynh, Tram ; Chen, Zhong ; Pang, Suhong ; Geng, Jieping ; Bandiera, Tiziano ; Bindi, Simona ; Vianello, Paola ; Roletto, Fulvia ; Thieffine, Sandrine ; Galvani, Arturo ; Vaccaro, Wayne ; Poss, Michael A. ; Trainor, George L. ; Lorenzi, Matthew V. ; Gottardis, Marco ; Jayaraman, Lata ; Purandare, Ashok V. / Optimization of pyrazole inhibitors of Coactivator Associated Arginine Methyltransferase 1 (CARM1). In: Bioorganic and Medicinal Chemistry Letters. 2009 ; Vol. 19, No. 11. pp. 2924-2927.
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