2. Academic Validation
  3. A sub-milligram-synthesis protocol for in vitro screening of HDAC11 inhibitors

A sub-milligram-synthesis protocol for in vitro screening of HDAC11 inhibitors

  • Bioorg Med Chem Lett. 2016 May 15;26(10):2434-2437. doi: 10.1016/j.bmcl.2016.03.116.
Yinping Tian 1,  Jin Jin 1,  Congying Wang 1,  Wenhui Lv 1,  Xuewei Li 1,  Xiaona Che 1,  Yanchao Gong 1,  Yanjun Li 1,  Quanli Li 1,  Jingli Hou 2,  Peng G Wang 3,  Jie Shen 4
Affiliations

Affiliations

  • 1 State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300071, People's Republic of China.
  • 2 Tianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics, School of Pharmacy, Tianjin Medical University, Tianjin 300070, People's Republic of China.
  • 3 State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300071, People's Republic of China. Electronic address: pwang@nankai.edu.cn.
  • 4 State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300071, People's Republic of China. Electronic address: jieshen@nankai.edu.cn.
PMID: 27055940 DOI: 10.1016/j.bmcl.2016.03.116
Abstract

This work demonstrated the high efficiency of a sub-milligram-synthesis based medicinal chemistry method. Totally 72 compounds, consisting a tri-substituted pyrrolidine core, were prepared. Around 0.1mg of each compound was solid-phase synthesized. Based on the additive property of UV absorptions of unconjugated chromophores of a molecule, these compounds were quantified by UV measurement. A hit, whose IC50 value was 1.2μM in HDAC11 inhibition assays, highlights the applicability of the approach reported here in future optimization works.

Keywords

HDAC11; Solid phase synthesis; Sub-milligram-synthesis; UV quantification; Unconjugated chromophore.

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