New potent P-glycoprotein inhibitors carrying a polycyclic scaffold.
New pentacyclic inhibitors of the P-glycoprotein carrying nitrogen-containing alkyl chains were synthesized and evaluated for MDR reverting activity on mouse lymphoma cells infected with pHa MDR1/A retrovirus. The activity of the compounds proved to be up to 5-fold higher than verapamil, used as reference compound.
Bisi
Alessandra
A
Department of Pharmaceutical Sciences, University of Bologna, Via Belmeloro 6, I-40126 Bologna, Italy. alessandra.bisi@unibo.it
Gobbi
Silvia
S
Rampa
Angela
A
Belluti
Federica
F
Piazzi
Lorna
L
Valenti
Piero
P
Gyemant
Nora
N
Molnár
Joseph
J
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000037:antagonists & inhibitors* / Q000235:genetics; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002461:Cell Line, Transformed; D045744:Cell Line, Tumor; D019008:Drug Resistance, Neoplasm / Q000187:drug effects*; D019450:Genes, MDR; D006576:Heterocyclic Compounds, 4 or More Rings / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051379:Mice; D012190:Retroviridae / Q000235:genetics
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D000970:Antineoplastic Agents; D006576:Heterocyclic Compounds, 4 or More Rings