Synthesis of 2-methyl N10-substituted acridones as selective inhibitors of multidrug resistance (MDR) associated protein in cancer cells.
A series of N10-substituted-2-methyl acridone derivatives are synthesized and are examined for its ability to reverse P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in breast cancer cell lines MCF-7 and MCF-7/Adr. The structural requirement of in-vitro anti-cancer and reversal of drug resistance are studied. The results showed that compound 16 with four carbon spacer exhibited promising in-vitro anti-cancer and reversal of drug resistance in comparison to the other analogues.
Mayur
Y C
YC
Department of Medical Oncology, Cancer Center Amsterdam, VU Medical Center, Amsterdam, The Netherlands. mayuryc@rediffmail.com
Ahmad
Osman
O
Prasad
V V S Rajendra
VV
Purohit
M N
MN
Srinivasulu
N
N
Kumar
S M Shanta
SM
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000378:metabolism; D054831:Acridones / Q000138:chemical synthesis / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D001943:Breast Neoplasms / Q000378:metabolism / Q000473:pathology; D045744:Cell Line, Tumor / Q000187:drug effects / Q000473:pathology; D019008:Drug Resistance, Neoplasm; D006801:Humans; D008956:Models, Chemical; D027425:ATP-Binding Cassette, Sub-Family C Proteins / Q000037:antagonists & inhibitors*
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D054831:Acridones; D000970:Antineoplastic Agents; D027425:ATP-Binding Cassette, Sub-Family C Proteins