Journal ArticleDOI
The cytotoxicity of 2-formyl and 2-acetyl-(6-picolyl)-4N-substituted thiosemicarbazones and their copper(II) complexes.
M. C. Miller,Kenneth F. Bastow,Christa N. Stineman,John R. Vance,Sun C. Song,Douglas X. West,Iris H. Hall +6 more
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TLDR
2‐Acetyl‐(6‐picolyl)‐4N‐substituted thiosemicarbazones and their copper(II) complexes were shown to be potent antineoplastic and cytotoxic agents against murine and human cultured cells and were as active against solid tumor growth as clinically useful agents.Abstract:
1-Acetyl-(6-picolyl)- 4 N-substituted thiosemicarbazones and their copper(II) complexes were shown to be potent antineoplastic and cytotoxic agents against murine and human cultured cells. Numerous derivatives were as active against solid tumor growth as clinically useful agents.The agents inhibited L 1210 DNA and RNA syntheses with inhibition of key regulatory enzyme activities of the purine pathway as well as nucleoside kinase activities. d[NTP] pools were reduced and DNA strand scission occurred. These agents were DNA topoisomerase II inhibitors with lower IC 50 values than that of VP-16. However, they did not cause L 1210 DNA protein linked breaks and actually protected against those breaks afforded by VP-16. The agents were not synergistic with VP-16 in reducing cell growth or DNA synthesis although they did reduce growth of L 1210 cells in agar suspended media.read more
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Advances in copper complexes as anticancer agents.
Carlo Santini,Maura Pellei,Valentina Gandin,Marina Porchia,Francesco Tisato,Cristina Marzano +5 more
Journal ArticleDOI
Role of metalation in the topoisomerase IIα inhibition and antiproliferation activity of a series of α-heterocyclic-N4-substituted thiosemicarbazones and their Cu(II) complexes.
TL;DR: The topoisomerase-IIα inhibition and antiproliferative activity of α-heterocyclic thiosemicarbazones and their corresponding copper(II) complexes have been investigated and copper complexes were shown to inhibit the proliferation of breast cancer cells expressing high levels of the enzyme.
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The cytotoxicity and mechanisms of 1,2-naphthoquinone thiosemicarbazone and its metal derivatives against MCF-7 human breast cancer cells.
Junnan Chen,Yue-Wern Huang,Guanshu Liu,Zahra Afrasiabi,Ekkehard Sinn,Subhash Padhye,Yinfa Ma +6 more
TL;DR: Investigation of the antitumor functions and mechanisms of 1,2-naphthoquinone-2-thiosemicarbazone and its metal complexes against MCF-7 human breast cancer cells revealed that these complexes are effective antitumors chemicals in inhibiting MCf-7 cell growth, with Ni-NQTS being the most effective among the complexes studied.
Journal ArticleDOI
Copper Complexes as Anticancer Agents Targeting Topoisomerases I and II.
TL;DR: New emerging treatment aspects are depicted to encourage the expansion of this family of highly active anticancer drugs and to expend their use in clinical trials and future cancer therapy.
Journal ArticleDOI
Interactions of the pyridine-2-carboxaldehyde isonicotinoyl hydrazone class of chelators with iron and DNA: implications for toxicity in the treatment of iron overload disease.
TL;DR: Under extreme conditions seen in the DNA-strand break assay, weak DNA-binding may potentiate the redox activity of the PCIH analogues, and these results support the potential of these chelators for the treatment of Fe overload.