Cyclometalated Benzimidazole Osmium(II) Complexes with Antiproliferative Activity in Cancer Cells Disrupt Calcium Homeostasis

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F68081707%3A_____%2F23%3A00572135" target="_blank" >RIV/68081707:_____/23:00572135 - isvavai.cz</a>
Alternative codes found
RIV/61989592:15310/23:73620578
Result on the web
<a href="https://pubs.acs.org/doi/10.1021/acs.inorgchem.3c00501" target="_blank" >https://pubs.acs.org/doi/10.1021/acs.inorgchem.3c00501</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1021/acs.inorgchem.3c00501" target="_blank" >10.1021/acs.inorgchem.3c00501</a>

Result language
angličtina
Original language name
Cyclometalated Benzimidazole Osmium(II) Complexes with Antiproliferative Activity in Cancer Cells Disrupt Calcium Homeostasis
Original language description
We present the synthesis and characterization of six new heteroleptic osmium(II) complexes of the type [Os(C<^>N)(N<^>N)2]OTf (N<^>N = 2,2 '-bipyridine and dipyrido[3,2-d:2 ',3 '-f]quinoxaline, C<^>N = deprotonated methyl 1-butyl-2aryl-benzimidazolecarboxylate) with varying substituents in the R3 position of the phenyl ring of the cyclometalating C<^>N ligand. The new compounds are highly kinetically inert and absorb a full-wavelength range of visible light. An investigation of the antiproliferative activity of the new compounds has been performed using a panel of human cancer and noncancerous 2D cell monolayer cultures under dark conditions and green light irradiation. The results demonstrate that the new Os(II) complexes are markedly more potent than conventional cisplatin. The promising antiprolifer-ative activity of selected Os(II) complexes was also confirmed using 3D multicellular tumor spheroids, which have the characteristics of solid tumors and can mimic the tumor tissue microenvironment. The mechanism of antiproliferative action of complexes has also been investigated and revealed that the investigated Os(II) complexes activate the endoplasmic reticulum stress pathway in cancer cells and disrupt calcium homeostasis.
Czech name
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Czech description
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Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
10402 - Inorganic and nuclear chemistry

Project
<a href="/en/project/GA23-06316S" target="_blank" >GA23-06316S: Medicinal biophysics and biochemistry of light-activated metallodrugs for targeted cancer therapy.</a><br>
Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Publication year
2023
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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