AI Article Synopsis
- Researchers combined the tranylcypromine part from LSD1 inhibitors with a specific thienopyrimidine part from menin-MLL1 PPI inhibitors to create new chemical compounds for medicinal studies.
- Out of 15 new compounds developed, some showed very strong LSD1 activity and low activity against other MAO-A/B enzymes, alongside effective menin-MLL1 PPI inhibition and decent anti-cancer activity against MV4-11 cells.
- The effectiveness of the better compounds was verified through experiments that measured CD86 mRNA levels, confirming their engagement with LSD1 inside cells.
Article Abstract
Tranylcypromine moiety extracted from LSD1 inhibitors and 6-trifluoroethyl thienopyrimidine moiety from menin-MLL1 PPI inhibitors were merged to give new chemotypes for medicinal chemistry study. Among 15 new compounds prepared in this work, some exhibited nanomolar LSD1 activity and good selectivity over MAO-A/B, low micromolar menin-MLL1 PPI inhibitory activity, as well as submicromolar MV4-11 antiprofilative activities. Intracellular LSD1 engagement of compounds with higher enzymatic and antiproliferative activities was confirmed by CD86 mRNA up-regulation experiments.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2019.01.017 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Tranylcypromine and 6-trifluoroethyl thienopyrimidine hybrid as LSD1 inhibitor.
Bioorg Med Chem Lett
March 2019
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, PR China; University of Chinese Academy of Sciences, No. 19A Yuquan Road, Beijing 100049, PR China. Electronic address:
Article Synopsis
- Researchers combined the tranylcypromine part from LSD1 inhibitors with a specific thienopyrimidine part from menin-MLL1 PPI inhibitors to create new chemical compounds for medicinal studies.
- Out of 15 new compounds developed, some showed very strong LSD1 activity and low activity against other MAO-A/B enzymes, alongside effective menin-MLL1 PPI inhibition and decent anti-cancer activity against MV4-11 cells.
- The effectiveness of the better compounds was verified through experiments that measured CD86 mRNA levels, confirming their engagement with LSD1 inside cells.
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!