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Molecules 2014, 19(7), 8803-8819; doi:10.3390/molecules19078803

Synthesis and Cytotoxicity Evaluation of Naphthalimide Derived N-Mustards

State Key Laboratory of Natural and Biomimetic Drugs, Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China
These authors contributed equally to this work.
Authors to whom correspondence should be addressed.
Received: 21 May 2014 / Revised: 10 June 2014 / Accepted: 17 June 2014 / Published: 25 June 2014
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A series of N-mustards, which was conjugated to mono- or bis-naphthalimides with a flexible amine link, were synthesized and evaluated for cytotoxicity against five cancer cell lines (HCT-116, PC-3, U87 MG, Hep G2 and SK-OV-3). Several compounds displayed better activities than the control compound amonafide. Further evaluations by fluorescence spectroscopy studies and DNA-interstrand cross-linking assays revealed that the derivatives showed both alkylating and intercalating properties. Among the derivatives, the bis-naphthalimide N-mustard derivative 11b was found to exhibit the highest cytotoxic activity and DNA cross-linking ability. Both 11b and 7b induce HCT-116 cell apoptosis by S phase arrest. View Full-Text
Keywords: cytotoxicity; DNA alkylating agent; DNA intercalator; synthesis; N-mustard; naphthalimide cytotoxicity; DNA alkylating agent; DNA intercalator; synthesis; N-mustard; naphthalimide

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MDPI and ACS Style

Lou, Q.; Ji, L.; Zhong, W.; Li, S.; Yu, S.; Li, Z.; Meng, X. Synthesis and Cytotoxicity Evaluation of Naphthalimide Derived N-Mustards. Molecules 2014, 19, 8803-8819.

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