New 7-azaindole palladium and platinum complexes: crystal structures and theoretical calculations. In vitro anticancer activity of the platinum compounds

2010 ◽  
Vol 39 (13) ◽  
pp. 3290 ◽  
Author(s):  
José Ruiz ◽  
Venancio Rodríguez ◽  
Concepción de Haro ◽  
Arturo Espinosa ◽  
José Pérez ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Crystal Structures ◽  
Theoretical Calculations ◽  
Platinum Complexes ◽  
Platinum Compounds ◽  
Palladium And Platinum Complexes

Topological control of supramolecular crystal structures of phenylene bis-monothiooxamate derivatives and in vitro anticancer activity

2017 ◽  
Vol 1149 ◽  
pp. 803-811 ◽  
Author(s):  
Tamyris T. da Cunha ◽  
Willian X.C. Oliveira ◽  
Ivana M. Marzano ◽  
Carlos B. Pinheiro ◽  
Elene Cristina Pereira-Maia ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Crystal Structures

scholarly journals 1,2,4-Triazine Sulfonamides: Synthesis by Sulfenamide Intermediates, In Vitro Anticancer Screening, Structural Characterization, and Molecular Docking Study

Molecules ◽  
2020 ◽  
Vol 25 (10) ◽  
pp. 2324
Author(s):  
Danuta Branowska ◽  
Zbigniew Karczmarzyk ◽  
Ewa Wolińska ◽  
Waldemar Wysocki ◽  
Maja Morawiak ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Anticancer Activity ◽  
Estrogen Receptor Alpha ◽  
Theoretical Calculations ◽  
Molecular Structures ◽  
Breast Cancer Cell Lines ◽  
In Vitro Tests ◽  
Molecular Docking Study ◽  
Ic50 Values

In this study, we synthesized novel sulfonamides with a 1,2,4-triazine moiety according to pharmacophore requirements for biological activity. All the synthesized compounds were tested in vitro to verify whether they exhibited anticancer activity against the human breast cancer cell lines MCF-7 and MDA-MB-231. Among them, two most active ones, having IC50 values of 50 and 42 µM, respectively, were found to show higher anticancer activity than chlorambucil used as the reference in the in vitro tests. In addition, two other compounds, which had IC50 values of 78 and 91 µM, respectively, exhibited a similar level of activity as chlorambucil. X-ray analysis carried out for two of the compounds confirmed their synthesis pathway as well as their assumed molecular structures. Furthermore, a conformational analysis was performed, and electronic parameters of molecules were characterized using theoretical calculations at AM1 and DFT level. Moreover, molecular docking revealed the mode of binding of the investigated 1,2,4-triazine sulfonamides with the human estrogen receptor alpha (ERα).

The Synthesis and in Vitro Cytotoxicity of Two trans-Platinum Complexes of Heterocyclic Amines

2003 ◽  
Vol 56 (7) ◽  
pp. 685 ◽  
Author(s):  
Georgina Giannikopoulos ◽  
Chih-Lynne Teo ◽  
Matthew D. Hall ◽  
Ronald R. Fenton ◽  
Trevor W. Hambley
Keyword(s):  
Crystal Structures ◽  
Platinum Complexes ◽  
In Vitro Cytotoxicity ◽  
Heterocyclic Amines ◽  
Monoclinic Space Group ◽  
Triclinic Space Group ◽  
Space Group ◽  
R Value

The syntheses and crystal structures of the platinum(II) complexes trans-[PtCl2(DMSO)(C4H9NO)] and trans-[PtCl2(DMSO)(dmdze)] are described and the mechanisms leading to their formation are discussed. The complex trans-[PtCl2(DMSO)(C4H9NO)] crystallizes in the triclinic space group P1, a 8.1432(8), b 8.5224(8), c 9.0801(9) Å, α 111.780(1), β 91.074(2), γ 98.349(2)°, Z 2, and its structure was refined to an R value of 0.019 on 2470 F. The cytotoxicity of this complex was determined and was found to be lower than that of cisplatin. The complex trans-[PtCl2(DMSO)(dmdze)] crystallizes in the monoclinic space group C2/c, a 23.498(5), b 8.048(2), c 17.859(6) Å, β 120.88(2), Z 8, and its structure was refined to an R value of 0.034 on 2712 F.

scholarly journals Platinum and ruthenium complexes as promising molecules in cancer therapy

2019 ◽  
Vol 147 (1-2) ◽  
pp. 105-109 ◽  
Author(s):  
Natasa Avramovic ◽  
Nikola Ignjatovic ◽  
Aleksandar Savic
Keyword(s):  
Cancer Therapy ◽  
Anticancer Activity ◽  
Specific Interaction ◽  
Ruthenium Complexes ◽  
Platinum Complexes ◽  
Chemotherapeutic Agents ◽  
Cross Resistance ◽  
Main Challenge

Cancer is one of the most common fatal diseases in humans nowadays. About 20 million new cancer cases are expected in the next two decades worldwide. The development of new chemotherapeutic agents with improved properties is presently the main challenge in the medicinal chemistry. Cisplatin was introduced to oncology in 1978 as first chemotherapeutic agent regarding its specific interaction with DNA, leading to its damage and causing the cell death. Since the first application of cisplatin in cancer therapy, there has been a growing interest in new metal-based compounds, in particular platinum and ruthenium complexes, with better anticancer activity and less side-effects compared to cisplatin. Carboplatin and oxaliplatin have shown promising action against some types of cancer, which are resistant to cisplatin. With the aim to overcome cross-resistance to these Pt(II) drugs, bioavailable platinum complexes (satraplatin and picoplatin) firstly found application as orally administered drugs, as well as some combined therapies of Pt(II) drugs (cisplatin, picoplatin) with specific resistant modulators. In recent years, novel polymer and liposomal formulations of platinum drugs (prolindac, lipoplatin, lipoxal, aroplatin) have been designed with strategy to improve drug delivery to target cancer cells and reduce toxicity. Complexes based on ruthenium have great potential to become leading candidates for the medical use in anticancer therapy. Some of these compounds have shown good anticancer activity, both in vitro and in vivo and two of them (KP1019 and NAMI-A) have passed clinical trials and given promising results.

Efficacy of newly developed platinum complexes against osteosarcoma, bone-targeting platinum, and proteasome inhibitory platinum.

2012 ◽  
Vol 30 (15_suppl) ◽  
pp. 10075-10075
Author(s):  
Kentaro Igarashi ◽  
Norio Yamamoto ◽  
Toshiharu Shirai ◽  
Katsuhiro Hayashi ◽  
Hideji Nishida ◽  
...  
Keyword(s):  
Side Effects ◽  
Platinum Complex ◽  
Annexin V ◽  
Platinum Complexes ◽  
Clinical Results ◽  
Platinum Compound ◽  
Platinum Compounds ◽  
Ic50 Value

10075 Background: Cisplatin is one of the most effective anti-cancer drugs available for the treatment of human solid tumors including osteosarcoma. As we had already reported, we have utilized caffeine in our chemotherapy protocol. And we achieved excellent clinical results. But effectiveness of cisplatin has been limited by side effects, and resistance. Here we developed two novel platinum compounds. 3Pt is trinuclear platinum complex bearing geminal bisphosphonate moieties, 1Pt is mononuclear platinum complex which has proteasome inhibitory activity. We performed comparative studies of our novel platinum compounds with osteosarcoma. Methods: Two novel platinum complexes were synthesized by Prof. Odani at school of pharmaceutical sciences of our university and cisplatin and caffeine were obtained from constructor. Three cell lines (MG63, 143B, and LM8) were used. Cell survival after a 72 hrs exposure to these compounds was assessed by WST-8 assay, and IC50 value was calculated for each compound. Apoptosis was assessed by DNA fragmentation and Annexin V-FITC/propidium iodine assay. Results: Each compound strongly caused concentration-dependent cytocidal effect. IC50 value of trinuclear compound is superior to cisplatin, and both complexes showed caffeine potentiation. Apoptosis induction and acetylation of histon H2AX were observed. In vivo, 1Pt showed almost same, 3Pt showed strong antitumor effect compared to cisplatin. Conclusions: Two novel platinum compounds that we developed showed strong ant-tumor effect in osteosarcoma in vitro and in vivo. As bisphosphonate has high affinity to calcium ions, 3Pt targets bone tissue and expected to reduce side effects at extraskeletal sites and to overcome the drug resistance. Proteasome inhibitory platinum compound has never been reported before, we will investigate its anti-tumor mechanism precisely.

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