Anticancer evaluation of a novel dithiocarbamate hybrid as the tubulin polymerization inhibitor
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Novel quinoline-dithiocarbamate hybrids were synthesized and designed by the molecular hybridization strategy. All these derivatives were evaluated for their antiproliferative activity against three selected cancer cell lines (MGC-803, HepG-2 and PC-3). Among them, compound 10c displayed the best antiproliferative activity against PC-3 cells with an IC50 value of 0.43 μM. Celluar mechanisms investigated that compound 10c could inhibit the migration against PC-3 cells by regulation the expression levels of E-cadherin and N-cadherin. Compound 10c induced morphological changes of PC-3 cells and regulated apoptosis-related proteins (Bcl-2, Bax and Cleaved-Parp). In addition, compound 10c inhibited tubulin polymerization in vitro with an IC50 value of 4.02 μM. Importantly, compound 10c inhibited the growth of PC-3 cells in vivo with the low toxicity toward mice. These results suggested that compound 10c might be an antitumor agent with potential for treating prostate cancer.
KeywordsQuinoline-dithiocarbamate Prostate cancer Migration Tubulin polymerization Apoptosis-related proteins
So thanks the supports from The 4th affiliated hospital of CMU.
Jia Liu., Dongwei Xue., Xingwang Zhu., Liu Yu., Minghuan Mao and Yili Liu performed the design work and experiments. Jia Liu and Yili Liu witten the paper. All authors read and approved the final manuscript.
This work was supported by The 4th affiliated hospital of CMU.
Compliance with ethical standards
Conflict of interest
The authors declare that they have no conflict of interest.
This article does not contain any studies with human participants performed by any of the authors. All applicable guidelines for the care and use of animals were followed by the 4th affiliated hospital of CMU (Shenyang, China).
Informed consent was obtained from all individual participants included in the study.
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