Antitumour activity of novel 1,10-phenanthroline and 5-amino-1,10-phenanthroline derivatives

Wesselinova, Diana; Neykov, Mihail; Kaloyanov, Nikolay; Toshkova, Reneta; Dimitrov, Georgi

doi:10.1016/j.ejmech.2009.01.036

Cited by 40 publications

(28 citation statements)

References 5 publications

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“…Phenanthroline derivatives attracted attention in the last years especially due to their biological effects [1][2][3] , materials science applications 4 , crystal engineering 5,6 , their unique p-electrons delocalization 7,8 and complexation properties 9 . Phenanthrolines polycyclic skeletons are also present in sterols, sex hormones, cardiac glycosides, bile acids and morphine alkaloids 10 .…”

Section: Introductionmentioning

confidence: 99%

Synthesis, structure, antimycobacterial and anticancer evaluation of new pyrrolo-phenanthroline derivatives

Matarneh

Mangalagiu

Shova³

et al. 2015

Journal of Enzyme Inhibition and Medicinal Chemistry

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A study concerning design, synthesis, structure and in vitro antimycobacterial and anticancer evaluation of new fused derivatives with pyrrolo[2,1-c] [4,7]phenanthroline skeleton is described. The strategy adopted for synthesis involves a [3 + 2] dipolar cycloaddition of several in situ generated 4,7-phenanthrolin-4-ium ylides to different substituted alkynes and alkenes. Stereo-and regiochemistry of cycloaddition reactions were discussed. The structure of the new compounds was proven unambiguously, single-crystal X-ray diffraction studies including. The antimycobacterial and anticancer activity of a selection of new synthesized compounds was evaluated against Mycobacterium tuberculosis H37Rv under aerobic conditions and 60 human tumour cell line panel, respectively. Five of the tested compounds possess a moderate antimycobacterial activity, while two of the compounds have a significant antitumor activity against renal cancer and breast cancer.

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Section: Introductionmentioning

confidence: 99%

Synthesis, structure, antimycobacterial and anticancer evaluation of new pyrrolo-phenanthroline derivatives

Matarneh

Mangalagiu

Shova³

et al. 2015

Journal of Enzyme Inhibition and Medicinal Chemistry

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“…Zhang and co-worker (2008) demonstrated that tri-functional mononuclear platinum(II) complexes and new type binuclear platinum complexes have cytotoxic and antitumor effects against leukemia, colon carcinoma, breast carcinoma, bladder carcinoma and gastricarcinoma cell lines 4 . Moreover, in spite of the fact that there is a scarcity of data concerning the anticancer activity of 1,10-phenanthroline (phen) and its derivatives, some metals with bidentate ligand are known to have anticancer activity against many kinds of cancer 14,15,28,30 . For example, the chemotherapeutic potential of 1,10-phenanthroline (phen) was evaluated using two human carcinoma cell lines (A-498 and Hep-G2) by Deegan et al (2006) in addition; phen and three metal-phen complexes were found cytotoxic and had DNA synthesis inhibition capability with metal complexes.…”

Section: Discussionmentioning

confidence: 99%

Studies on the cytotoxic, apoptotic and antitumoral effects of Au(III) and Pt(II) complexes of 1, 10-phenanthroline on V79 379A and A549 cell lines

Bostancıoğlu

Işık

Genç

et al. 2011

Journal of Enzyme Inhibition and Medicinal Chemistry

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“…Furthermore, a great many pyrrolidine complexes have also provoked a great interest in their diverse spectra of biological and pharmaceutical activities, such as antibacterial and antitumor activities [4][5][6][7][8]. Coordination compounds of platinum have an especially rich history due to the clinical success of cisplatin and related anticancer drugs [9,10]. In previous study [11], we synthesized a new platinum(II) complex (Fig.…”

Section: Introductionmentioning

confidence: 99%

Mechanistic and Conformational Studies on the Interaction of a Platinum(II) Complex Containing an Antiepileptic Drug, Levetiracetam, With Bovine Serum Albumin by Optical Spectroscopic Techniques in Aqueous Solution

Shahabadi

Hadidi

2014

Appl Biochem Biotechnol

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Fluorescence spectroscopy in combination with circular dichroism (CD) and ultraviolet-visible (UV-vis) absorption spectroscopy were employed to investigate the binding of a new platinum(II) complex containing an antiepileptic drug "Levetiracetam" to bovine serum albumin (BSA) under the physiological conditions. In the mechanism discussion, it was proved that the fluorescence quenching of BSA by Pt(II) complex is a result of the formation of Pt(II) complex-BSA complex. The thermodynamic parameters ΔG, ΔH, and ΔS at different temperatures (283, 298, and 310 K) were calculated, and the negative value for ΔH and ΔS indicate that the hydrogen bonds and van der Waals interactions play major roles in Pt(II) complex-BSA association. Binding studies concerning the number of binding sites (n~1) and apparent binding constant K b were performed by fluorescence quenching method. The site marker competitive experiments indicated that the binding of Pt(II) complex to BSA primarily took place in site II. Based on the Förster's theory, the average binding distance between Pt(II) complex and BSA was obtained (r = 5.29 nm). Furthermore, UV-vis, CD, and synchronous fluorescence spectrum were used to investigate the structural change of BSA molecules with addition of Pt(II) complex. These results indicate that the binding of Pt(II) complex to BSA causes apparent change in the secondary structure of BSA and do affect the microenvironment around the tryptophan residue.

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Antitumour activity of novel 1,10-phenanthroline and 5-amino-1,10-phenanthroline derivatives

Cited by 40 publications

References 5 publications

Synthesis, structure, antimycobacterial and anticancer evaluation of new pyrrolo-phenanthroline derivatives

Synthesis, structure, antimycobacterial and anticancer evaluation of new pyrrolo-phenanthroline derivatives

Studies on the cytotoxic, apoptotic and antitumoral effects of Au(III) and Pt(II) complexes of 1, 10-phenanthroline on V79 379A and A549 cell lines

Mechanistic and Conformational Studies on the Interaction of a Platinum(II) Complex Containing an Antiepileptic Drug, Levetiracetam, With Bovine Serum Albumin by Optical Spectroscopic Techniques in Aqueous Solution

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