Design, Synthesis and Activity Study of Aminopeptidase N Targeted AHPA Derivatives
News Apr 26, 2012
A series of (2RS,3S)-3-amino- 2-hydroxy-4-phenyl-butanoic acids (AHPA) derivatives (MA0-MA7) were synthesized. The in vitro aminopeptidase N (APN) enzyme and cell proliferation assay of target compounds were investigated. The results showed that most compounds displayed potent inhibitory activities against APN, compound MA0 showed even better inhibitory effects than bestatin on both enzyme activity and HL60 cell proliferation. The FlexX docking result showed the mode of binding between MA0 and APN.
This study was published online in Drug Discoveries and Therapeutics and is free to access.
Researchers Develop Novel ‘One-pot’ Approach to Conjugated Tetraenes SynthesisNews
TUAT researchers have achieved the new synthetic route of conjugated tetraenes from inexpensive and easily available 1,3-butadiene and substituted acetylenes by a one-pot approach under mild conditions. Conjugated tetraenes are important key substructures in biologically active natural products such as vitamins, and anti-mycotic drugs.READ MORE
Cancer Fighting Compound Activated by Substance Found in Stinging NettlesNews
Researchers have developed a new line of attack against cancer: an organic-osmium compound, which is triggered using a non-toxic dose of sodium formate, a natural product found in many organisms, including nettles and ants.READ MORE