期刊
CHEMISTRYSELECT
卷 2, 期 16, 页码 4382-4391出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/slct.201700701
关键词
Anticancer; Density-functional theory; Dithiocarbamate; Metallomacrocyclic; Sulfone
资金
- CSIR, New Delhi, India [01/2733/13/EMR-II]
- UGC, New Delhi, India
Interesting biological profile of dapsone (dap) has encouraged us to derivatize it further into a novel series of diamines 4,4'-bis(2-(alkylamino) acetamido) diphenylsulfone L-1-L-3 and their ensuing metallomacrocyclic complexes of the type [M-2-(2)-bis-{(S-2,S-S2CN(R)CH2CONHC6H4)(2)SO2}] {R=Cy, M=Ni-II 1a, Cu-II 1b, Zn-II 1c; R=Pr-i, M=Ni-II 2a, Cu-II 2b, Zn-II 2c; R=Bu-n, M=Ni-II 3a, Cu-II 3b, Zn-II 3c}. These compounds were characterized by standard spectroscopic methods. A DFT level calculation has been performed on selected compounds. In vitro anticancer activity against Hep G2 (hepatoma) and C6 (Glioblastoma) cell lines suggests specificity of these compounds for cancer cells over normal liver cells. Interestingly, complex 2c holding zinc(II) and N-Pr-i substituents shows nearly 3 fold better cytotoxic activity against both Hep G2 (8.47 +/- 0.016 g/mL) and C6 (4.3 +/- 0.019 g/mL) cell lines, compared to the reference drug Cisplatin. The morphological changes and moderate to heavy DNA laddering clearly demonstrate the induction of apoptotic cell death, required for major chemical therapeutic implications.
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