Journal Article10.1021/ACS.INORGCHEM.9B00281
Synthesis of Gold(I) Complexes Containing Cinnamide: In Vitro Evaluation of Anticancer Activity in 2D and 3D Spheroidal Models of Melanoma and in Vivo Angiogenesis
V. Ganga Reddy,T. Srinivasa Reddy,Steven H. Privér,Yutao Bai,Shweta Mishra,Donald Wlodkowic,Nedaossadat Mirzadeh,Suresh K. Bhargava +7 more
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TL;DR: Mechanical investigations of 3c activity indicate thioredoxin reductase inhibition through steric and hydrogen-bonding interactions, followed by the induction of oxidative stress and a mitochondrial pathway of cell death, which showed significant antiangiogenic properties in a transgenic zebrafish Tg(fli1a:EGFP) in vivo model.
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Abstract: A series of alkynylgold(I) phosphine complexes containing methoxy-substituted cinnamide moieties (3a-3c and 4a-4c) have been synthesized and characterized. All of the synthesized complexes were evaluated for their cytotoxicity against three human cancer cell lines A549 (lung), D24 (melanoma), and HT1080 (fibrosarcoma) and the human embryonic kidney 293 cell line (Hek293T) as a proxy model for noncancer cells. Most of the synthesized compounds showed antiproliferative activity against cancer cell lines at low micromolar concentrations. Among these, complex 3c showed a broad spectrum of anticancer activity with IC50 values in the range of 1.53-6.05 μM against all tested cancer lines. Complex 3c possessed 20 times higher cytotoxicity than the reference drug cisplatin against D24 melanoma cells and showed significant anticancer activity in 3D spheroidal models of melanoma cells. Mechanistic investigations of 3c activity indicate thioredoxin reductase inhibition through steric and hydrogen-bonding interactions, followed by the induction of oxidative stress and a mitochondrial pathway of cell death. Compound 3c also showed significant antiangiogenic properties in a transgenic zebrafish Tg(fli1a:EGFP) in vivo model.
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Citations
Pyrazolo-benzothiazole hybrids: Synthesis, anticancer properties and evaluation of antiangiogenic activity using in vitro VEGFR-2 kinase and in vivo transgenic zebrafish model
Velma Ganga Reddy,T. Srinivasa Reddy,Chetna Jadala,M. Soumya Reddy,Faria Sultana,Ravikumar Akunuri,Suresh K. Bhargava,Donald Wlodkowic,Pabbaraja Srihari,Pabbaraja Srihari,Ahmed Kamal +10 more
TL;DR: Results provide strong evidence that compound 14 could be considered for a lead candidate in anticancer and antiangiogenic drug discovery.
84
Exploration of carbamide derived pyrimidine-thioindole conjugates as potential VEGFR-2 inhibitors with anti-angiogenesis effect
Sravani Sana,Velma Ganga Reddy,Sonal Bhandari,T. Srinivasa Reddy,Ramya Tokala,Akash P. Sakla,Suresh K. Bhargava,Nagula Shankaraiah +7 more
TL;DR: Molecular docking studies have shown that compound 12k capably intermingled with catalytically active residues GLU-885, ASP-1046 of the VEGFR-2 through hydrogen-bonding interactions, which indicates the inhibition of colony formation and cell migration by 12k in a dose-dependent manner.
79
Advances in alkynyl gold complexes for use as potential anticancer agents
TL;DR: The current understanding of structure–activity relationships (SARs), mode of action and cytotoxicity of alkynyl gold complexes were summarized.
63
Cinnamide derived pyrimidine-benzimidazole hybrids as tubulin inhibitors: Synthesis, in silico and cell growth inhibition studies.
Sravani Sana,Velma Ganga Reddy,T. Srinivasa Reddy,Ramya Tokala,Rajesh Kumar,Suresh K. Bhargava,Nagula Shankaraiah +6 more
TL;DR: In this article, a new class of piperazine-linked cinnamide derivatives of benzimidazole-pyrimidine hybrids have been designed and synthesized, and their in vitro cytotoxicity profiles were explored on selected human cancer cell lines.
53
A review on metal complexes and its anti-cancer activities: Recent updates from in vivo studies.
Suman Adhikari,Priyatosh Nath,Alakesh Das,Abhijit Datta,Nabajyoti Baildya,Asim K. Duttaroy,Surajit Pathak +6 more
- 29 Jan 2024
TL;DR: Some of the most recently developed Pt, Ru, Au, Au, Cu, Ir, and Os complexes that have shown significant in vivo antitumor properties between 2017 and 2023 are highlighted.
49
References
A short history of SHELX
TL;DR: This paper could serve as a general literature citation when one or more of the open-source SH ELX programs (and the Bruker AXS version SHELXTL) are employed in the course of a crystal-structure determination.
An empirical correction for absorption anisotropy
TL;DR: A least-squares procedure is described for modeling an empirical transmission surface as sampled by multiple symmetry-equivalent and/or azimuth rotation-equ equivalent intensity measurements.
7.8K
In vivo imaging of embryonic vascular development using transgenic zebrafish.
TL;DR: It is found that the zebrafish fli1 promoter is able to drive expression of enhanced green fluorescent protein (EGFP) in all blood vessels throughout embryogenesis, and these transgenic lines allow detailed analysis of both wild type and mutant embryonic vasculature.
2.2K
Cisplatin as an Anti-Tumor Drug: Cellular Mechanisms of Activity, Drug Resistance and Induced Side Effects
TL;DR: Understanding of the biochemical mechanisms triggered by cisplatin in tumor cells may lead to the design of more efficient platinum derivates (or other drugs) and might provide new therapeutic strategies and reduce side effects.
1.6K
On the medicinal chemistry of gold complexes as anticancer drugs
TL;DR: The spectrum of gold complexes described as antiproliferative compounds comprises a broad variety of different species including many phosphine complexes as well as gold in different oxidation states.
782