Synthesis and in Vitro cytotoxic activities of 2-alkyl-2,3-dihydro-1H-2,6-diazacyclopenta[b]anthracene-5,10-diones.
A series of 2-alkyl-2,3-dihydro-1H-2,6-diazacyclopenta[b]anthracene-5,10-diones (4a-f) was synthesized and their in vitro cytotoxic activities were evaluated against six human cancer cell lines (HCT15, SK-OV-3, SNB19, A549, MCF7 and MCF7/ADR). They all appeared to be less potent than doxorubicin against all doxorubicin sensitive human cancer cell lines tested. However, these compounds retained considerable cytotoxic activity against the doxorubicin-resistant cell line MCF7/ADR, implying their therapeutic potential to treat doxorubicin-resistant tumors. The most active compound 4c was equipotent with doxorubicin against HCT15 cell line.
Kwak
Jae-Hwan
JH
Chungbuk National University, Cheongju, Korea.
Namgoong
Kwon
K
Jung
Jae-Kyung
JK
Han
Sang-Bae
SB
Cho
Jungsook
J
Kim
Hwan-Mook
HM
Park
Song-Gyu
SG
Lee
Kiho
K
Kang
Jong Soon
JS
Lee
Heesoon
H
D000873:Anthracenes / Q000138:chemical synthesis* / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects*; D004317:Doxorubicin / Q000494:pharmacology; D019008:Drug Resistance, Neoplasm / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor / Q000379:methods; D006801:Humans; D015394:Molecular Structure; D021281:Quantitative Structure-Activity Relationship
D000873:Anthracenes; D000970:Antineoplastic Agents; D004317:Doxorubicin