Parallel synthesis and antileishmanial activity of ether-linked phospholipids.
The synthesis and antileishmanial activity of 18 edelfosine analogues are described. Compounds were obtained in parallel combining solid phase and solution phase synthesis. The most active analogue is characterized by the octadecyl group in position 2 of the glycerol chain. Considering that this substitution determines the loss of antitumor activity, a different mechanism of antileishmanial action can be hypothesized.
Coghi
Paolo
P
Istituto di Chimica Farmaceutica e Tossicologica Pietro Pratesi, Università degli Studi di Milano, Via G. Mangiagalli 25, 20133 Milano, Italy.
Vaiana
Nadia
N
Pezzano
Maria G
MG
Rizzi
Luca
L
Kaiser
Marcel
M
Brun
Reto
R
Romeo
Sergio
S
D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D002845:Chromatography / Q000379:methods; D015195:Drug Design; D004987:Ethers; D005990:Glycerol / Q000737:chemistry; D006801:Humans; D020128:Inhibitory Concentration 50; D007893:Leishmania donovani / Q000187:drug effects; D009682:Magnetic Resonance Spectroscopy; D008956:Models, Chemical; D010743:Phospholipids / Q000737:chemistry*; D011108:Polymers / Q000737:chemistry
D000970:Antineoplastic Agents; D000981:Antiprotozoal Agents; D004987:Ethers; D010743:Phospholipids; D011108:Polymers; D005990:Glycerol