Synthesis of [PtCl2(4,4'-dialkoxy-2,2'-bipyridine)] Complexes and their In Vitro Anticancer Properties

Authors

Van Vo, University of Nevada, Las VegasFollow
Ontida Tanthmanatham, University of Nevada, Las VegasFollow
Haesook Han, University of Nevada, Las VegasFollow
Pradip K. Bhowmik, University of Nevada, Las VegasFollow
Bryan L. Spangelo, University of Nevada, Las VegasFollow

Document Type

Article

Publication Date

8-2013

Publication Title

Metallomics

Volume

5

Issue

8

First page number:

973

Last page number:

987

Abstract

A series of [Pt(II)Cl2(4,4'-dialkoxy-2,2'-bipyridine)] complexes of the general formula of [Pt(II)Cl2(4,4'-bis(RO)-2,2'-bipyridine)] (where R = -(CH2)n-1CH3, n = 2-6, 8) were synthesized and characterized using (1)H NMR, (13)C NMR spectroscopy, elemental analysis, mass spectroscopy, and differential scanning calorimetry measurements. The in vitro anti-proliferative activities of these compounds were evaluated against human cancer cell lines A549 (lung adenocarcinoma), DU145 (prostate carcinoma), MCF-7 (breast adenocarcinoma), and MDA-MB-435 (melanoma) using the MTS cell proliferation assay. Several Pt(II) coordination compounds were found to have greatly enhanced activity compared to cisplatin after a one hour treatment in all cell lines tested. A structure-activity relationship was observed, that is, the activity increases as the carbon chain length of the alkyl group increases. The activity was maximum when the carbon chain length reached four or five carbons and decreased with the longer carbon chain length. Fluorescence microscopy and flow cytometry data indicate that the main mode of cell death is through apoptosis with some necrotic responses.

Keywords

2; 2'-Dipyridyl/chemical synthesis; 2; 2'-Dipyridyl/chemistry; Antineoplastic Agents/chemical synthesis; Antineoplastic Agents/chemistry; Apoptosis; Breast Neoplasms/drug therapy; Carbon/chemistry; Cell Line; Tumor; Cell Proliferation; Cell Survival; Dose-Response Relationship; Drug; Drug Screening Assays; Antitumor; Female; Flow Cytometry; Humans; Lung Neoplasms/drug therapy; Magnetic Resonance Spectroscopy; Male; Mass Spectrometry; Microscopy; Fluorescence; Necrosis; Organoplatinum Compounds/chemical synthesis; Organoplatinum Compounds/chemistry; Prostatic Neoplasms/drug therapy; Pyridines/chemical synthesis; Pyridines/chemistry; Structure-Activity Relationship

Disciplines

Cancer Biology | Chemistry | Life Sciences | Physical Sciences and Mathematics

Language

English

Permissions

Use Find in Your Library, contact the author, or interlibrary loan to garner a copy of the item. Publisher policy does not allow archiving the final published version. If a post-print (author's peer-reviewed manuscript) is allowed and available, or publisher policy changes, the item will be deposited.

Repository Citation

Vo, V., Tanthmanatham, O., Han, H., Bhowmik, P. K., Spangelo, B. L. (2013). Synthesis of [PtCl2(4,4'-dialkoxy-2,2'-bipyridine)] Complexes and their In Vitro Anticancer Properties. Metallomics, 5(8), 973-987.