
Dalton Transactions p. 5932 - 5940 (2013)
Update date:2022-08-04
Topics:
Liu, Shenggui
Cao, Wenqiang
Yu, Lianling
Zheng, Wenjie
Li, Linlin
Fan, Cundong
Chen, Tianfeng
In the present study, two zinc(ii) complexes containing bis-benzimidazole derivatives, Zn(bpbp)Cl2 (1) and [Zn(bpbp)2](ClO 4)2·CH3CH2OH·H 2O (2) (bpbp = 2,6-bis(1-phenyl-1H-benzo[d]imidazol-2-yl)pyridine), have been designed, synthesized and evaluated for their in vitro anticancer activities. The underlying molecular mechanisms through which they caused the cancer cell death were also elucidated. The complexes were identified as potent antiproliferative agents against a panel of five human cancer cell lines by comparing with cisplatin. Complex 2 demonstrated dose-dependent growth inhibition on MCF-7 human breast carcinoma cells with IC50 at 2.9 μM. Despite this potency, the complexes possessed great selectivity between human cancer cells and normal cells. Induction of apoptosis in MCF-7 cells by complex 2 was evidenced by accumulation of sub-G1 cell population, DNA fragmentation and nuclear condensation. Further investigation on intracellular mechanisms revealed that complex 2 was able to induce p53-dependent apoptosis in cancer cells by triggering DNA damage. On the basis of this evidence, we suggest that Zn(ii) complexes containing bis-benzimidazole derivatives may be candidates for further evaluation as chemotherapeutic agents for human cancers.
SHIJIAZHUANG AGERUO-BIOTECH CO.LTD
Contact:+86-130-2866-6699
Address:Huaian east Road 158
Wuhan Hanye Chemical New Material Co.,Ltd
Contact:+86-27-85308141
Address:LiuDian, Panlongcheng Economic Development Zone, HuangPi district, Wuhan, Hubei 430311 P.R.China
PharmaResources(Kaiyuan)CO,.Ltd
Contact:+86-21-50720028
Address:No.3, Beihuan Road, Economic Development District, Kaiyuan City, Tieling City, Liaoning Province, China 112300
website:http://www.NEM.COM.CN
Contact:+86-393-4411771
Address:The west section of shengli Road,Puyang,Henan Province,China
Hangzhou LINGEBA Technology Co., Ltd.
Contact:+0086-571-87389059
Address:Office 1-913,NewYouth Plaza, GongShu Area, HangZhou,ZheJiang,P.R.China
Doi:10.1021/om400143u
(2013)Doi:10.1021/ja4086808
(2014)Doi:10.1016/0022-328X(94)88003-4
(1994)Doi:10.1016/j.bmcl.2013.12.090
(2014)Doi:10.1021/jo00086a028
(1994)Doi:10.1016/0040-4039(94)88189-8
(1994)