Sökning: onr:"swepub:oai:DiVA.org:uu-258756" >
Insights into the s...
Insights into the structure-activity relationships of chiral 1,2-diaminophenylalkane platinum(II) anticancer derivatives
-
Berger, Gilles (författare)
-
Fusaro, Luca (författare)
-
Luhmer, Michel (författare)
-
visa fler...
-
Czapla-Masztafiak, Joanna (författare)
-
Lipiec, Ewelina (författare)
-
Szlachetko, Jakub (författare)
-
Kayser, Yves (författare)
-
- Fernandes, Daniel L. A. (författare)
- Uppsala universitet,Fysikalisk kemi
-
- Sa, Jacinto (författare)
- Uppsala universitet,Fysikalisk kemi
-
Dufrasne, Francois (författare)
-
Bombard, Sophie (författare)
-
visa färre...
-
(creator_code:org_t)
- 2015-05-16
- 2015
- Engelska.
-
Ingår i: Journal of Biological Inorganic Chemistry. - : Springer Science and Business Media LLC. - 0949-8257 .- 1432-1327. ; 20:5, s. 841-853
- Relaterad länk:
-
https://urn.kb.se/re...
-
visa fler...
-
https://doi.org/10.1...
-
visa färre...
Abstract
Ämnesord
Stäng
- The structure-activity relationships of chiral 1,2-diaminophenylalkane platinum(II) anticancer derivatives are studied, including interactions with telomeric- and genomic-like DNA sequences, the pKa of their diaqua species, structural properties obtained from DFT calculations and resonant X-ray emission spectroscopy. The binding modes of the compounds to telomeric sequences were elucidated, showing no major differences with conventional cis-platinum(II) complexes like cisplatin, supporting that the cis-square planar geometry governs the binding of small Pt(II) complexes to G4 structures. Double-stranded DNA platination kinetics and acid-base constants of the diaqua species of the compounds were measured and compared, highlighting a strong steric dependence of the DNA-binding kinetics, but independent to stereoisomerism. Structural features of the compounds are discussed on the basis of dispersion-corrected DFT, showing that the most active series presents conformers for which the platinum atom is well devoid of steric hindrance. If reactivity indices derived from conceptual DFT do not show evidences for different reactivity between the compounds, RXES experiments provide new insight into the availability of platinum orbitals for binding to nucleophiles.
Ämnesord
- NATURVETENSKAP -- Biologi -- Biokemi och molekylärbiologi (hsv//swe)
- NATURAL SCIENCES -- Biological Sciences -- Biochemistry and Molecular Biology (hsv//eng)
Nyckelord
- Cancer
- Platinum
- G-quadruplex
- Conceptual DFT
- RXES
Publikations- och innehållstyp
- ref (ämneskategori)
- art (ämneskategori)
Hitta via bibliotek
Till lärosätets databas
- Av författaren/redakt...
-
Berger, Gilles
-
Fusaro, Luca
-
Luhmer, Michel
-
Czapla-Masztafia ...
-
Lipiec, Ewelina
-
Szlachetko, Jaku ...
-
visa fler...
-
Kayser, Yves
-
Fernandes, Danie ...
-
Sa, Jacinto
-
Dufrasne, Franco ...
-
Bombard, Sophie
-
visa färre...
- Om ämnet
-
- NATURVETENSKAP
-
NATURVETENSKAP
-
och Biologi
-
och Biokemi och mole ...
- Artiklar i publikationen
-
Journal of Biolo ...
- Av lärosätet
-
Uppsala universitet