Development of selective agents targeting serotonin 5HT1A receptors with subnanomolar activities based on a coumarin core.
Sign Up to like & getrecommendations! Published in 2017 at "MedChemComm"
DOI: 10.1039/c7md00281e
Abstract: A series of 18 new 5-[3-(4-aryl-1-piperazinyl)propoxy]coumarin derivatives from the corresponding bromoalkyl derivatives have been designed and synthesized by us using a microwave-assisted protocol. Radioligand binding assays of this series of compounds as well as a… read more here.
Keywords: targeting serotonin; development selective; 5ht1a receptors; serotonin 5ht1a ... See more keywords
Improving the Armamentarium of PI3K Inhibitors with Isoform-Selective Agents: A New Light in the Darkness.
Sign Up to like & getrecommendations! Published in 2017 at "Cancer discovery"
DOI: 10.1158/2159-8290.cd-17-0500
Abstract: Excitement and drug-development efforts aimed at targetable genetic aberrations in the PI3K/AKT/mTOR pathway have declined due to the limited clinical performance of these inhibitors as monotherapies. New, more isoform-selective treatments, such as taselisib, promise to… read more here.
Keywords: inhibitors isoform; armamentarium pi3k; improving armamentarium; isoform selective ... See more keywords