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Molecules 2014, 19(7), 8803-8819; https://doi.org/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.
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Received: 21 May 2014 / Revised: 10 June 2014 / Accepted: 17 June 2014 / Published: 25 June 2014
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Abstract

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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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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