scholarly journals The effect of geometric isomerism on the anticancer activity of the monofunctional platinum complex trans-[Pt(NH3)2(phenanthridine)Cl]NO3

2018 ◽  
Vol 54 (22) ◽  
pp. 2788-2791 ◽  
Author(s):  
Wen Zhou ◽  
Mohammad Almeqdadi ◽  
Michael E. Xifaras ◽  
Imogen A. Riddell ◽  
Ömer H. Yilmaz ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Platinum Complex ◽  
Cross Linking ◽  
Geometric Isomerism ◽  
Antitumor Properties

The trans-DDP based phenanthridine Pt(ii) complex displays significant antitumor properties, with a different spectrum of activity than that of classic bifunctional cross-linking agents like cisplatin.

scholarly journals cis-Diammine[3-(3-chloro-7-methoxy-9,10-dihydroacridin-9-ylideneamino)propan-1-amine-κ2N,N′]platinum(II) dinitrate

IUCrData ◽  
2016 ◽  
Vol 1 (4) ◽  
Author(s):  
Young Cheun ◽  
Seongmin Lee
Keyword(s):  
Crystal Structure ◽  
Hydrogen Bonding ◽  
Anticancer Activity ◽  
Secondary Amine ◽  
Complex Cation ◽  
Platinum Complex ◽  
Complex Salt ◽  
Title Complex

The title complex salt, [Pt(C16H17N3)(NH3)2](NO3)2, is of interest with respect to anticancer activity. The secondary amine of 9-aminoacridine coordinates with the platinum(II) atom, leading to imine–platinum complex cation formation. The crystal structure displays extensive N—H...O and N—H...N hydrogen bonding and weak C—H...Cl and C—H...O hydrogen bonding.

scholarly journals Protein ruthenation and DNA alkylation: chlorambucil-functionalized RAPTA complexes and their anticancer activity

2015 ◽  
Vol 44 (8) ◽  
pp. 3614-3623 ◽  
Author(s):  
Alexey A. Nazarov ◽  
Samuel M. Meier ◽  
Olivier Zava ◽  
Yulia N. Nosova ◽  
Elena R. Milaeva ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Active Agent ◽  
Dna Alkylation ◽  
Cross Linking

The conjugation of chlorambucil to the RAPTA scaffold results in an anticancer active agent capable of cross-linking DNA and proteins.

NMR studies probing the directionality of DNA interstrand cross-linking by the trinuclear platinum complex BBR3464

2003 ◽  
Vol 96 (1) ◽  
pp. 239 ◽  
Author(s):  
Donald S. Thomas ◽  
Murray S. Davies ◽  
Junyong Zhang ◽  
Susan J. Berners-Price ◽  
Nicholas Farrell
Keyword(s):  
Platinum Complex ◽  
Cross Linking ◽  
Nmr Studies

Effect of Geometric Isomerism in Dinuclear Platinum Antitumor Complexes on DNA Interstrand Cross-Linking†

Biochemistry ◽  
1999 ◽  
Vol 38 (34) ◽  
pp. 10997-11005 ◽  
Author(s):  
Jana Kašpárková ◽  
Olga Nováková ◽  
Oldřich Vrána ◽  
Nicholas Farrell ◽  
Viktor Brabec
Keyword(s):  
Cross Linking ◽  
Geometric Isomerism ◽  
Dinuclear Platinum ◽  
Antitumor Complexes

scholarly journals Synthesis and antitumor properties of some new N-(5-R-benzyl-1,3-thiazol-2-yl)-4,5-dihydro-1H-imidazole-2-carboxamides

2020 ◽  
pp. 150
Author(s):  
Volodymyr Ya Horishny ◽  
Iryna V Drapak ◽  
Taras I Chaban ◽  
Yuriy V Ostapiuk ◽  
Vasyl S Matiychuk
Keyword(s):  
Anticancer Activity ◽  
Anticancer Agents ◽  
Therapeutic Program ◽  
Activity Screening ◽  
Antitumor Properties

New N-(5-R-benzyl-1,3-thiazol-2-yl)-2-morpholin-4-yl-2-oxoacetamides have been prepared in good yields via the reaction of N-(5-R-benzyl-1,3-thiazol-2-yl)-2-chloroacetamides with sulfur and morfoline. These compounds react with ethendiamine to form a series of novel N-[5-R-benzyl)-1,3-thiazol-2-yl]-4,5-dihydro-1H-imidazole-2-carboxamides with excellent yields. Anticancer activity screening of synthesized compounds was carried out within the framework of the Developmental Therapeutic Program of the National Cancer Institute's (DTP, NCI, Bethesda, Maryland, USA). It was shown that compounds are promising for new anticancer agents' search.

scholarly journals Synthesis, Characterization, and Anticancer Activity of New Benzofuran Substituted Chalcones

2016 ◽  
Vol 2016 ◽  
pp. 1-8 ◽  
Author(s):  
Demet Coşkun ◽  
Suat Tekin ◽  
Süleyman Sandal ◽  
Mehmet Fatih Coşkun
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Antitumor Activities ◽  
Cell Viability Assay ◽  
Anticancer Properties ◽  
Viability Assay ◽  
Diphenyltetrazolium Bromide ◽  
Antitumor Properties ◽  
Mcf 7

Benzofuran derivatives are of great interest in medicinal chemistry and have drawn considerable attention due to their diverse pharmacological profiles including anticancer activity. Similarly, chalcones, which are common substructures of numerous natural products belonging to the flavonoid class, feature strong anticancer properties. A novel series of chalcones, 3-aryl-1-(5-bromo-1-benzofuran-2-yl)-2-propanones propenones (3a–f), were designed, synthesized, and characterized.In vitroantitumor activities of the newly synthesized (3a–f) and previously synthesized (3g–j) chalcone compounds were determined by using human breast (MCF-7) and prostate (PC-3) cancer cell lines. Antitumor properties of all compounds were determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Cell viability assay for the tested chalcone compounds was performed and thelog⁡IC50values of the compounds were calculated after 24-hour treatment. Our results indicate that the tested chalcone compounds show antitumor activity against MCF-7 and PC-3 cell lines (p<0.05).

DNA Cross-Linking Patterns Induced by an Antitumor-Active Trinuclear Platinum Complex and Comparison with Its Dinuclear Analogue

2009 ◽  
Vol 15 (21) ◽  
pp. 5245-5253 ◽  
Author(s):  
Jianhui Zhu ◽  
Yongmei Zhao ◽  
Yanyan Zhu ◽  
Ziyi Wu ◽  
Miaoxin Lin ◽  
...  
Keyword(s):  
Platinum Complex ◽  
Cross Linking

scholarly journals Simple Trans-Platinum Complex Bearing 3-Aminoflavone Ligand Could Be a Useful Drug: Structure-Activity Relationship of Platinum Complex in Comparison with Cisplatin

2020 ◽  
Vol 21 (6) ◽  
pp. 2116
Author(s):  
Małgorzata Fabijańska ◽  
Magdalena Orzechowska ◽  
Agnieszka J. Rybarczyk-Pirek ◽  
Justyna Dominikowska ◽  
Alicja Bieńkowska ◽  
...  
Keyword(s):  
Gene Expression ◽  
Ovarian Cancer ◽  
Anticancer Activity ◽  
Evaluation Method ◽  
Elevated Temperatures ◽  
Platinum Complex ◽  
Cell Viability Assay ◽  
Viability Assay ◽  
Diphenyltetrazolium Bromide ◽  
Relationship Of

Following previous studies devoted to trans–Pt(3-af)2Cl2, in this paper, the molecular structure and intermolecular interactions of the title complex are compared with other cisplatin analogues of which the crystal structures are presented in the Cambridge Structural Database (CSD). Molecular Hirshfeld surface analysis and computational methods were used to examine a possible relationship between the structure and anticancer activity of trans–Pt(3-af)2Cl2. The purpose of the article was also to investigate the effect of hyperthermia on the anticancer activity of cisplatin, cytostatics used in the treatment of patients with ovarian cancer and a new analogue of cisplatin-trans–Pt(3-af)2Cl2. The study was conducted on two cell lines of ovarian cancer sensitive to Caov-3 cytostatics and the OVCAR-3 resistant cisplatin line. The study used the MTT (3-(4,5-dimethylthiazol-2,5-diphenyltetrazolium bromide) cell viability assay, LDH (lactate dehydrogenase), and the quantitative evaluation method for measuring gene expression, i.e., qPCR with TagMan probes. Reduced survivability of OVCAR-3 and Caov-3 cells exposed to cytostatics at elevated temperatures (37 °C, 40 °C, 43 °C) was observed. Hyperthermia may increase the sensitivity of cells to platinum-based antineoplastic drugs and paclitaxel, which may be associated with the reduction of gene expression related to apoptotic processes.

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