874110-84-6Relevant academic research and scientific papers
Enhancing the Cytotoxic Activity of Anticancer PtIV Complexes by Introduction of Lonidamine as an Axial Ligand
Nosova, Yulia N.,Foteeva, Lidia S.,Zenin, Ilia V.,Fetisov, Timur I.,Kirsanov, Kirill I.,Yakubovskaya, Marianna G.,Antonenko, Taisya A.,Tafeenko, Viktor A.,Aslanov, Leonid A.,Lobas, Anna A.,Gorshkov, Mikhail V.,Galanski, Markus,Keppler, Bernhard K.,Timerbaev, Andrei R.,Milaeva, Elena R.,Nazarov, Alexey A.
, p. 1785 - 1791 (2017)
The synthesis and in vitro cytotoxicity of a series of PtIV complexes with lonidamine as a ligand coordinated in axial position are described. Lonidamine was found to affect strongly the in vitro cytotoxic activity of these new complexes, lowering the IC50 values down to the nanomolar range. Lipophilicity assessed in terms of log P showed no direct correlation with cytotoxicity.
Ru(III) complexes with lonidamine-modified ligands
Babkov, Denis A.,Gracheva, Yulia A.,Kirsanov, Kirill I.,Milaeva, Elena R.,Nazarov, Alexey A.,Okulova, Yulia N.,Ott, Ingo,Redkozubova, Olga M.,Schmidt, Claudia,Shevtsova, Elena F.,Shtil, Alexander A.,Shutkov, Ilya A.,Sokolova, Elena V.,Spasov, Alexander A.,Tyurin, Vladimir Yu.
, (2021/12/17)
A series of bifunctional Ru(III) complexes with lonidamine-modified ligands (lonidamine is a selective inhibitor of aerobic glycolysis in cancer cells) was described. Redox properties of Ru(III) complexes were characterized by cyclic voltammetry. An easy
Lysosomal-targeted anticancer half-sandwich iridium(III) complexes modified with lonidamine amide derivatives
Xie, Yongkang,Zhang, Shumiao,Ge, Xingxing,Ma, Wenli,He, Xiaolin,Zhao, Yao,Ye, Juan,Zhang, Hongmin,Wang, Anwei,Liu, Zhe
, (2020/03/05)
Ten half-sandwich iridium complexes containing lonidamine amide derivatives were synthesized and characterized. Unlike lonidamine, which acts on mitochondria, its iridium complexes successfully targeted lysosomes and induced lysosomal damage. Antiproliferation studies showed that most of the complexes have higher anticancer activity against A549 and HeLa cells than cisplatin. The antitumor activity of complex 6 is 2.69 times that of cisplatin against A549 cells. We also performed antitumor tests on ligands L1 and L5, and proved that they exhibit excellent antitumor activity only after binding to the metal center. The bovine serum albumin (BSA) binding test showed that the complexes had the ability to bind to BSA, and they interact with BSA by a static mechanism. The complexes can also cause changes in mitochondrial membrane potential and can produce active oxygen species better than active control. NADH/NAD+ transformation experiments were used to determine if the production of ROS was caused by the transformation of NADH/NAD+. We also explored the way that the complexes enter cells.
Antiproliferative activity of Pt(IV) complexes with lonidamine and bexarotene ligands attached via succinate-ethylenediamine linker
Okulova,Zenin,Shutkov,Kirsanov,Kovaleva,Lesovaya,Fetisov,Milaeva,Nazarov
, (2019/08/01)
We present the synthesis and cytotoxic potencies of new Pt(IV) complexes with lonidamine and bexarotene ligand tethered to Pt-center via a succinate-ethylenediamine linker. The in vitro results for a series of complexes with cisplatin, dichloride(ethane-1,2-diamine)platinum(II), or oxaliplatin core indicate that the addition to the structure lonidamine or bexarotene moiety can confer activity or selectivity of Pt(IV) complexes.
MITO-LONIDAMINE, COMPOSITIONS AND METHODS OF USE
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Paragraph 0099; 00100, (2019/07/20)
The present invention relates to mito-lonidamine compounds, compositions and methods of use in the treatment of cancer.
Structure-activity relationship study and discovery of indazole 3-carboxamides as calcium-release activated calcium channel blockers
Bai, Sha,Nagai, Masazumi,Koerner, Steffi K.,Veves, Aristidis,Sun, Lijun
, p. 393 - 397 (2017/01/17)
Aberrant activation of mast cells contributes to the development of numerous diseases including cancer, autoimmune disorders, as well as diabetes and its complications. The influx of extracellular calcium via the highly calcium selective calcium-release activated calcium (CRAC) channel controls mast cell functions. Intracellular calcium homeostasis in mast cells can be maintained via the modulation of the CRAC channel, representing a critical point for therapeutic interventions. We describe the structure-activity relationship study (SAR) of indazole-3-carboxamides as potent CRAC channel blockers and their ability to stabilize mast cells. Our SAR results show that the unique regiochemistry of the amide linker is critical for the inhibition of calcium influx, the release of the pro-inflammatory mediators β-hexosaminidase and tumor necrosis factor α by activated mast cells. Thus, the indazole-3-carboxamide 12d actively inhibits calcium influx and stabilizes mast cells with sub-μM IC50. In contrast, its reverse amide isomer 9c is inactive in the calcium influx assay even at 100?μM concentration. This requirement of the specific 3-carboxamide regiochemistry in indazoles is unprecedented in known CRAC channel blockers. The new structural scaffolds described in this report expand the structural diversity of the CRAC channel blockers and may lead to the discovery of novel immune modulators for the treatment of human diseases.
Organometallic anticancer agents that interfere with cellular energy processes: A subtle approach to inducing cancer cell death
Nazarov, Alexey A.,Gardini, Daniel,Baquié, Mathurin,Juillerat-Jeanneret, Lucienne,Serkova, Tatiana P.,Shevtsova, Elena P.,Scopelliti, Rosario,Dyson, Paul J.
supporting information, p. 2347 - 2350 (2013/03/28)
Two hybrid compounds comprising an antimetastatic ruthenium-arene fragment tethered to an indazole-3-carboxylic acid derivative that inhibits aerobic glycolysis in cancer cells have been prepared and evaluated in a variety of cancer cell lines, including highly relevant human glioblastoma cells, with an apparent synergistic action between the two components observed.
