当前位置： SCI文献检索 > BIOORGANIC & MEDICINAL CHEMISTRY期刊下所有文献 > Antiproliferative and apoptosis-inducing activities of novel naphthalimide-cyclam conjugates through dual topoisomerase (topo) I/II inhibition.

Antiproliferative and apoptosis-inducing activities of novel naphthalimide-cyclam conjugates through dual topoisomerase (topo) I/II inhibition.

Abstract：

:A novel series of naphthalimide-cyclam conjugates were designed and synthesized. Among them, compounds 4c, 4d, 8c and 8d which bearing long lipophilic alkyl chains, displayed comparable or more potent cytotoxic activities against human tumor cell lines than amonafide. Furthermore, the four compounds were proved to possess strong inhibition against both topoisomerase I and II. The representative compound 8c exhibited moderate DNA intercalation activity. Molecular modeling studies identified the possible interaction of compound 8c with the molecular target by forming topoisomerase/DNA/drug ternary complex. Finally, derivatives with long lipophilic alkyl chains could efficiently induce apoptosis.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Tan S,Sun D,Lyu J,Sun X,Wu F,Li Q,Yang Y,Liu J,Wang X,Chen Z,Li H,Qian X,Xu Y

doi

10.1016/j.bmc.2015.07.011

subject

Has Abstract

pub_date

2015-09-01 00:00:00

pages

5672-80

issue

17

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(15)00578-7

journal_volume

23

pub_type

杂志文章

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