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Design of new thiosemicarbazones and their Cu(II) and Pd(II) complexes as topoisomerase inhibitors

Grant number: 13/20156-5
Support type:Scholarships in Brazil - Post-Doctorate
Effective date (Start): February 01, 2014
Effective date (End): January 06, 2016
Field of knowledge:Physical Sciences and Mathematics - Chemistry - Inorganic Chemistry
Principal researcher:Adelino Vieira de Godoy Netto
Grantee:Fillipe Vieira Rocha
Home Institution: Instituto de Química (IQ). Universidade Estadual Paulista (UNESP). Campus de Araraquara. Araraquara , SP, Brazil


The main objective of this project is the design of new thiosemicarbazones and their Cu(II) and Pd(II) square planar complexes which act as inhibitors of DNA topoisomerase II ±. The interaction between the compounds and topoisomerase will be evaluated by agarose gel electrophoresis assay. The biological activity of the most promising compounds will be evaluated by MTT assays against the murine cells L929, LM3 and LP07 and apoptosis assays. To better understand the mechanism of action of these compounds against the target enzyme, molecular docking calculations could be performed. The thiosemicarbazones will be synthesized starting from suitable chalcones and thiossemicarbazides. The complexes will be obtained by the reactions of the appropriated metallic salt and the thiossemicarbazones, the tryphenilphosphine and halogens groups will act as co-ligands. The compounds will be characterized by elemental analysis, IR and NMR spectroscopies, ESI/MS mass spectrometry, thermogravimetry (TG) and single crystal X-ray diffraction methods.

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Scientific publications
(References retrieved automatically from Web of Science and SciELO through information on FAPESP grants and their corresponding numbers as mentioned in the publications by the authors)
ROCHA, FILLIPE V.; FARIAS, RENAN L.; LIMA, MAURO A.; BATISTA, VICTOR S.; NASCIMENTO-JUNIOR, NAILTON M.; GARRIDO, SAULO S.; LEOPOLDINO, ANDREA M.; GOTO, RENATA N.; OLIVEIRA, ADRIANO B.; BECK, JOHANNES; LANDVOGT, CHRISTIAN; MAURO, ANTONIO E.; NETTO, ADELINO V. G. Computational studies, design and synthesis of Pd(II)-based complexes: Allosteric inhibitors of the Human Topoisomerase-II alpha. Journal of Inorganic Biochemistry, v. 199, OCT 2019. Web of Science Citations: 7.
ROCHA, FILLIPE V.; BARRA, CAROLINA V.; GARRIDO, SAULO S.; MANENTE, FRANCINE A.; CARLOS, IRACILDA Z.; ELLENA, JAVIER; FUENTES, ANDREA S. C.; GAUTIER, ARNAUD; MOREL, LAURENT; MAURO, ANTONIO E.; NETTO, ADELINO V. G. Cationic Pd(II) complexes acting as topoisomerase II inhibitors: Synthesis, characterization, DNA interaction and cytotoxicity. Journal of Inorganic Biochemistry, v. 159, p. 165-168, JUN 2016. Web of Science Citations: 11.

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