Tuesday January 16th 2018

New quinolone- and 1,8-naphthyridine-3-carboxamides as selective CB2 receptor agonists with anticancer and immuno-modulatory activity.

In this study, we synthesized and tested a series of new quinoline-2(1H)-one- and 4-hydroxy-2-oxo-1,2-dihydro-1,8-naphthyridine derivatives characterized by a 4-methylcyclohexylamido substituent in position 3 of the heterocyclic nucleus with high CB2 receptor affinity and selectivity. Two compounds showing the best binding and selectivity profile behaved as a full agonist and a partial agonist at the CB2 receptor and induced a concentration-dependent decrease of cell viability on LNCaP, a prostatic cancer cell line expressing CB2 receptor. Moreover considering that the CB2 receptor is mainly expressed in cells and organs of the immune system, the same compounds were studied for their potential immune-modulatory and anti-inflammatory effects in activated lymphocytes isolated from healthy co…

View the original here:  

New quinolone- and 1,8-naphthyridine-3-carboxamides as selective CB2 receptor agonists with anticancer and immuno-modulatory activity.

Leave a Comment

More from category

FDA Denies Health Claim for Vitamin D to Prevent MS FDA Denies Health Claim for Vitamin D to Prevent MS
FDA Denies Health Claim for Vitamin D to Prevent MS FDA Denies Health Claim for Vitamin D to Prevent MS

The FDA responded to a petition, saying that after reviewing the evidence, there is no basis for the claim that vitamin [Read More]

Effects of sport climbing on multiple sclerosis – Steimer J, Weissert R.
Effects of sport climbing on multiple sclerosis – Steimer J, Weissert R.

Multiple sclerosis (MS) is an autoimmune and neurodegenerative disease of the central nervous system (CNS) with [Read More]

Researchers use novel PET tracer to assess myelin damage in mouse models of MS
Researchers use novel PET tracer to assess myelin damage in mouse models of MS

The loss or damage of myelin, a cellular sheath that surrounds and insulates nerves, is the hallmark of the [Read More]

MS Drug Ocrelizumab (Ocrevus) Approved in Europe MS Drug Ocrelizumab (Ocrevus) Approved in Europe
MS Drug Ocrelizumab (Ocrevus) Approved in Europe MS Drug Ocrelizumab (Ocrevus) Approved in Europe

The European Commission clears the anti-CD20 monoclonal antibody for adults with relapsing multiple sclerosis and early [Read More]

New PET radiotracer offers insight into multiple sclerosis
New PET radiotracer offers insight into multiple sclerosis

Combining PET scans with a novel radiotracer could help researchers track damage...Read more on AuntMinnie.comRelated [Read More]