scholarly journals Cu(II) Propionyl-Thiazole Thiosemicarbazone Complexes: Crystal Structure, Inhibition of Human Topoisomerase IIα, and Activity against Breast Cancer Cells

2018 ◽  
Vol 08 (02) ◽  
pp. 30-46 ◽  
Author(s):  
Edward C. Lisic ◽  
Victoria G. Rand ◽  
Lana Ngo ◽  
Patrick Kent ◽  
Jeffrey Rice ◽  
...  
2015 ◽  
Vol 19 (10) ◽  
pp. 1107-1113 ◽  
Author(s):  
Qiong Yu ◽  
Wei-Xia Xu ◽  
Ya-Hong Yao ◽  
Zeng-Qi Zhang ◽  
Shu Sun ◽  
...  

One novel porphyrin 5,10,15-tris(phenyl)-20-[4-(2-(2-methyl-5-nitro-imidazolyl)ethoxyl)phenyl] porphyrin and its zinc(II) metalloporphyrin were synthesized and characterized by IR, UV-vis, 1H NMR, MS and elemental analysis. The single crystal structure of zinc(II) porphyrin shows that the Zn(II) ion is coordinated with four nitrogen atoms of porphyrin ring and one oxygen atom of ethanol from axial, forming a five-coordinated square pyramidal geometry. Their cytotoxicity and photodynamic activity against breast cancer cells were studied. The results indicate that both of the porphyrins display high phototoxicity to the breast cancer cells with the negligible dark toxicity. In addition, the photodynamic activity of zinc(II) porphyrin was obviously higher than that of the free porphyrin.


2016 ◽  
Vol 06 (02) ◽  
pp. 146-154 ◽  
Author(s):  
Jennifer D. Conner ◽  
Wathsala Medawala ◽  
Madison T. Stephens ◽  
William H. Morris ◽  
Joseph E. Deweese ◽  
...  

1999 ◽  
Vol 55 (9) ◽  
pp. 1516-1523 ◽  
Author(s):  
Elaine R. Podell ◽  
Daniel J. Harrington ◽  
Dylan J. Taatjes ◽  
Tad H. Koch

Epidoxorubicin and daunorubicin are proposed to be cytotoxic to tumor cells by catalyzing production of formaldehyde through redox cycling and using the formaldehyde for covalent attachment to DNA at G bases. The crystal structure of epidoxorubicin covalently bound to a d(CGCGCG) oligomer was determined to 1.6 Å resolution. The structure reveals slightly distorted B-form DNA bearing two molecules of epidoxorubicin symmetrically intercalated at the termini, with each covalently attached from its N3′ to N2 of a G base via a CH2 group from the formaldehyde. The structure is analogous to daunorubicin covalently bound to d(CGCGCG) determined previously, except for additional hydrogen bonding from the epimeric O4′ to O2 of a C base. The role of drug–DNA covalent bonding in cells was investigated with synthetic epidoxorubicin–formaldehyde conjugate (Epidoxoform) and synthetic daunorubicin–formaldehyde conjugate (Daunoform). Uptake and location of drug fluorophore in doxorubicin-resistant human breast-cancer cells (MCF-7/ADR cells) was observed by fluorescence microscopy and flow cytometry. The fluorophore of Daunoform appeared more rapidly in cells and was released more rapidly from cells than the fluorophore of Epidoxoform over a 3 h exposure period. The fluorophore appeared predominantly in the nucleus of cells treated with both conjugates. The difference in uptake is explained in terms of the slower rate of hydrolysis of Epidoxoform to the species reactive with DNA and a proposed slower release from DNA based upon the crystal structures.


2005 ◽  
Vol 44 (3) ◽  
pp. 240-247 ◽  
Author(s):  
Takeshi Asano ◽  
Eugenie S. Kleinerman ◽  
Leonard A. Zwelling ◽  
Zhichao Zhou ◽  
Yoshitaka Fukunaga

2017 ◽  
Vol 46 (12) ◽  
pp. 3833-3847 ◽  
Author(s):  
Angela Sîrbu ◽  
Oleg Palamarciuc ◽  
Maria V. Babak ◽  
Jia Min Lim ◽  
Kateryna Ohui ◽  
...  

The synthesis, characterisation and mode of action of water-soluble copper(ii)–TSC complexes are reported.


2009 ◽  
Vol 69 (3) ◽  
pp. 948-957 ◽  
Author(s):  
V. Ashutosh Rao ◽  
Sarah R. Klein ◽  
Keli K. Agama ◽  
Eriko Toyoda ◽  
Noritaka Adachi ◽  
...  

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