TY - JOUR
T1 - Antitumor agents 278. 4-Amino-2H-benzo[h]chromen-2-one (ABO) analogs as potent in vitro anti-cancer agents
AU - Dong, Yizhou
AU - Nakagawa-Goto, Kyoko
AU - Lai, Chin Yu
AU - Morris-Natschke, Susan L.
AU - Bastow, Kenneth F.
AU - Lee, Kuo Hsiung
PY - 2010/7/15
Y1 - 2010/7/15
N2 - 4-Amino-2H-benzo[h]chromen-2-one (ABO) analogs were designed, synthesized, and evaluated for cytotoxic activity. Among all 4-substituted ABO analogs, cyclohexyl (12), N-methoxy-N-methylacetamide (14), and various aromatic derivatives (15-25 and 27) exhibited promising cell growth inhibitory activity with ED 50 values of 0.01-5.8 μM against all tested tumor cell lines. The 4′-methoxyphenyl derivative (18) and 3′-methylphenyl derivative (24) showed the most potent antitumor activity against a broad range of cancer cell lines with ED 50 values of 0.01-76 μM. Preliminary SAR results indicated that substitutions on nitrogen are critical to the antitumor potency.
AB - 4-Amino-2H-benzo[h]chromen-2-one (ABO) analogs were designed, synthesized, and evaluated for cytotoxic activity. Among all 4-substituted ABO analogs, cyclohexyl (12), N-methoxy-N-methylacetamide (14), and various aromatic derivatives (15-25 and 27) exhibited promising cell growth inhibitory activity with ED 50 values of 0.01-5.8 μM against all tested tumor cell lines. The 4′-methoxyphenyl derivative (18) and 3′-methylphenyl derivative (24) showed the most potent antitumor activity against a broad range of cancer cell lines with ED 50 values of 0.01-76 μM. Preliminary SAR results indicated that substitutions on nitrogen are critical to the antitumor potency.
KW - 4-Amino-2H-benzo[h]chromen-2-one analogs (ABO)
KW - Cytotoxic activity
KW - Structure-activity relationships
UR - http://www.scopus.com/inward/record.url?scp=77953869126&partnerID=8YFLogxK
U2 - 10.1016/j.bmcl.2010.05.079
DO - 10.1016/j.bmcl.2010.05.079
M3 - Article
C2 - 20542429
AN - SCOPUS:77953869126
SN - 0960-894X
VL - 20
SP - 4085
EP - 4087
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 14
ER -