Abstract:
:A series of novel naphthalimide derivatives with 4-[4-(3,3-diphenylallyl)piperazin-1-yl]benzoic acid as side chain were designed and synthesized. Their antitumor activities were evaluated against a variety of cancer cell lines in vitro. Preliminary results showed that most of the derivatives had cytotoxic activity comparable with that of amonafide, with IC₅₀ values of 10⁻⁶-10⁻⁵ M. Interestingly, compound 12e had the unique antitumor activity against MCF-7 among the cancer cell lines tested. More importantly, flow cytometric analysis indicated that compared with amonafide, the target compounds could effectively induce G₂/M arrest and progress to apoptosis in HL-60 cells after double staining with annexin V-FITC and propidium iodide. The present work provided a novel class of naphthalimide-based derivatives with potential apoptosis-inducing and improved antitumor activity for further optimization.
journal_name
Chem Biol Drug Desjournal_title
Chemical biology & drug designauthors
Wu A,Mei P,Xu Y,Qian Xdoi
10.1111/j.1747-0285.2011.01232.xsubject
Has Abstractpub_date
2011-12-01 00:00:00pages
941-7issue
6eissn
1747-0277issn
1747-0285journal_volume
78pub_type
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