Synthesis and cytotoxic activities of 2-alkyl-2,3-dihydro-1H-2,6,9-triazacyclopenta[b]anthracene-5,10-diones.
A series of 2-alkyl-2,3-dihydro-1H-2,6,9-triazacyclopenta[b]anthracene-5,10-diones (4a-f) were synthesized and their in vitro cytotoxic activities were evaluated against six human cancer cell lines (HCT15, SK-OV-3, A549, SNB19, MCF7 and MCF7/ADR). A number of compounds including 4c and 4d showed 2-180 times more potent cytotoxic activity than doxorubicin against all human cancer cell lines tested. Furthermore, these compounds retained considerable cytotoxic activity against the doxorubicin-resistant cell line MCF7/ADR, implying their therapeutic potential to treat doxorubicin-resistant tumors.
Kwak
Jae-Hwan
JH
College of Pharmacy, Chungbuk National University, Cheongju 361-763, Korea.
Namgoong
Kwon
K
Jung
Jae-Kyung
JK
Cho
Jungsook
J
Kim
Hwan-Mook
HM
Park
Sung-Gyu
SG
Yoo
Yeong-Ah
YA
Kwon
Joo-Hee
JH
Lee
Heesoon
H
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D011719:Pyrazines / Q000138:chemical synthesis* / Q000494:pharmacology*; D011809:Quinones / Q000138:chemical synthesis* / Q000494:pharmacology*; D012235:Rhodamines; D013055:Spectrophotometry, Infrared; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D011719:Pyrazines; D011809:Quinones; D012235:Rhodamines; C022027:lissamine rhodamine B