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Synthesis and cytotoxicity evaluation of naphthalimide derived N-mustards.

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.

SUBMITTER: Lou Q

PROVIDER: S-EPMC6271267 | biostudies-literature | 2014 Jun

REPOSITORIES: biostudies-literature

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Synthesis and cytotoxicity evaluation of naphthalimide derived N-mustards.

Lou Qinghua Q Ji Liyan L Zhong Wenhe W Li Shasha S Yu Siwang S Li Zhongjun Z Meng Xiangbao X

Molecules (Basel, Switzerland) 20140625 7

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 th ...[more]

PMID: 24968335

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