TY - JOUR
T1 - Aza-analogs of dibenzo[c,h]cinnoline
T2 - Triazachrysenes as potent topoisomerase I-targeting anticancer agents
AU - Singh, Sudhir K.
AU - Ruchelman, Alexander L.
AU - Zhou, Nai
AU - Li, Tsai Kun
AU - Liu, Angela
AU - Liu, Leroy F.
AU - LaVoie, Edmond J.
PY - 2003
Y1 - 2003
N2 - 2,3-Dimethoxy-8,9-methylenedioxydibenzo[c,h]cinnoline 1 exhibits greater topoisomerase I (TOP1)-targeting activity and cytotoxicity than its benzo[i]phenanthridine analog. 1,5,6-, 5,6,11-, and 5,6,12-Triazachrysene analogs were prepared to determine the influence of further aza-substitution on TOP1-targeting activity and cytotoxicity. The data reinforce the structure-activity relationships previously observed and indicate that a nitrogen heteroatom can be tolerated at the 11- or 12-position without adversely affecting the TOP1-targeting activity or cytotoxicity of 1.
AB - 2,3-Dimethoxy-8,9-methylenedioxydibenzo[c,h]cinnoline 1 exhibits greater topoisomerase I (TOP1)-targeting activity and cytotoxicity than its benzo[i]phenanthridine analog. 1,5,6-, 5,6,11-, and 5,6,12-Triazachrysene analogs were prepared to determine the influence of further aza-substitution on TOP1-targeting activity and cytotoxicity. The data reinforce the structure-activity relationships previously observed and indicate that a nitrogen heteroatom can be tolerated at the 11- or 12-position without adversely affecting the TOP1-targeting activity or cytotoxicity of 1.
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M3 - Article
AN - SCOPUS:0242523648
SN - 1054-2523
VL - 12
SP - 1
EP - 12
JO - Medicinal Chemistry Research
JF - Medicinal Chemistry Research
IS - 1
ER -