Abstract
Aim: Metal carbenic complexes have received considerable attention in both the catalysis and biological fields for their potential applications in cancer and antimicrobial therapies. Results: A small series of new silver and gold N-heterocyclic carbene complexes has been designed and synthesized. Among the tested complexes, one compound was particularly active in inhibiting anchorage-dependent and -independent breast cancer proliferation, and inducing cell apoptosis via a mitochondria-related process. The antitumor activity was associated to the transcriptional activation of the tumor suppressor gene p53 in an Sp1-dependent manner, as evidenced by biological and docking studies. Conclusion: Our results highlight the importance and the versatility of N-heterocyclic carbene complexes of gold and silver as useful tools against breast cancer progression.
| Original language | English |
|---|---|
| Pages (from-to) | 2213-2229 |
| Number of pages | 17 |
| Journal | Future Medicinal Chemistry |
| Volume | 8 |
| Issue number | 18 |
| DOIs | |
| Publication status | Published - Dec 1 2016 |
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Keywords
- breast cancer
- mitochondria
- N-heterocyclic carbene complexes
- p53
- Sp1
- transmetallation
ASJC Scopus subject areas
- Molecular Medicine
- Pharmacology
- Drug Discovery
Cite this
N-heterocyclic carbene complexes of silver and gold as novel tools against breast cancer progression. / Saturnino, Carmela; Barone, Ines; Iacopetta, Domenico; Mariconda, Annaluisa; Sinicropi, Maria Stefania; Rosano, Camillo; Campana, Antonella; Catalano, Stefania; Longo, Pasquale; Andò, Sebastiano.
In: Future Medicinal Chemistry, Vol. 8, No. 18, 01.12.2016, p. 2213-2229.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - N-heterocyclic carbene complexes of silver and gold as novel tools against breast cancer progression
AU - Saturnino, Carmela
AU - Barone, Ines
AU - Iacopetta, Domenico
AU - Mariconda, Annaluisa
AU - Sinicropi, Maria Stefania
AU - Rosano, Camillo
AU - Campana, Antonella
AU - Catalano, Stefania
AU - Longo, Pasquale
AU - Andò, Sebastiano
PY - 2016/12/1
Y1 - 2016/12/1
N2 - Aim: Metal carbenic complexes have received considerable attention in both the catalysis and biological fields for their potential applications in cancer and antimicrobial therapies. Results: A small series of new silver and gold N-heterocyclic carbene complexes has been designed and synthesized. Among the tested complexes, one compound was particularly active in inhibiting anchorage-dependent and -independent breast cancer proliferation, and inducing cell apoptosis via a mitochondria-related process. The antitumor activity was associated to the transcriptional activation of the tumor suppressor gene p53 in an Sp1-dependent manner, as evidenced by biological and docking studies. Conclusion: Our results highlight the importance and the versatility of N-heterocyclic carbene complexes of gold and silver as useful tools against breast cancer progression.
AB - Aim: Metal carbenic complexes have received considerable attention in both the catalysis and biological fields for their potential applications in cancer and antimicrobial therapies. Results: A small series of new silver and gold N-heterocyclic carbene complexes has been designed and synthesized. Among the tested complexes, one compound was particularly active in inhibiting anchorage-dependent and -independent breast cancer proliferation, and inducing cell apoptosis via a mitochondria-related process. The antitumor activity was associated to the transcriptional activation of the tumor suppressor gene p53 in an Sp1-dependent manner, as evidenced by biological and docking studies. Conclusion: Our results highlight the importance and the versatility of N-heterocyclic carbene complexes of gold and silver as useful tools against breast cancer progression.
KW - breast cancer
KW - mitochondria
KW - N-heterocyclic carbene complexes
KW - p53
KW - Sp1
KW - transmetallation
UR - http://www.scopus.com/inward/record.url?scp=84999287074&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84999287074&partnerID=8YFLogxK
U2 - 10.4155/fmc-2016-0160
DO - 10.4155/fmc-2016-0160
M3 - Article
AN - SCOPUS:84999287074
VL - 8
SP - 2213
EP - 2229
JO - Future Medicinal Chemistry
JF - Future Medicinal Chemistry
SN - 1756-8919
IS - 18
ER -