PT  - JOURNAL ARTICLE
AU  - SHAHNAZ A. HAMAD
AU  - PHILIP BEALE
AU  - JUN QING YU
AU  - FAZLUL HUQ
TI  - Synthesis and Antitumour Activity of a New Trinuclear Platinum Compound [{&lt;em&gt;cis&lt;/em&gt;-PtCl(NH&lt;sub&gt;3&lt;/sub&gt;)&lt;sub&gt;2&lt;/sub&gt;μ {&lt;em&gt;trans&lt;/em&gt;-Pt(3-hydroxypyridine)&lt;sub&gt;2&lt;/sub&gt;H&lt;sub&gt;2&lt;/sub&gt;N(CH&lt;sub&gt;2&lt;/sub&gt;)&lt;sub&gt;5&lt;/sub&gt;NH&lt;sub&gt;2&lt;/sub&gt;)&lt;sub&gt;2&lt;/sub&gt;}] Cl&lt;sub&gt;4&lt;/sub&gt; in Human Ovarian Cancer Cells
DP  - 2014 Apr 01
TA  - Anticancer Research
PG  - 1923--1929
VI  - 34
IP  - 4
4099  - http://ar.iiarjournals.org/content/34/4/1923.short
4100  - http://ar.iiarjournals.org/content/34/4/1923.full
SO  - Anticancer Res2014 Apr 01; 34
AB  - A trinuclear platinum compound with a cis-geometry for the terminal metal centers coded as QH5 has been synthesized and investigated for activity against the human ovarian A2780, A2780cisR and A2780ZD0473R cancer cell lines. Cellular accumulation of platinum, level of platinum–DNA binding and nature of interaction of the compound with pBR322 plasmid DNA have also been determined. QH5 is found to be more active than cisplatin against all the three cell lines and to have much lower resistant factors than cisplatin. The compound is 2.5-times more active than cisplatin against the A2780cisR cell line and 11.5-times more active than cisplatin against A2780ZD0473R cell line. When the activity of QH5 in A2780 cell line is compared with its activity in the A2780ZD0473R cell line, it is found to be 2.4-times more active against the resistant A2780ZD0473R cancer cell line than the parent A2780 cell line, thus indicating that it has been able to overcome mechanisms of resistance operating in the A2780ZD0473R cell lines. The higher activity of QH5 as compared to cisplatin is found to be associated with higher platinum accumulation at all time points and high level of platinum-DNA binding at 24 h in all the three human ovarian cancer cell lines. Provided QH5 has the right toxicity profile and its in vitro activity is complemented with sufficient activity in vivo, the compound may have the potential for development as a novel platinum–based anticancer drug targeted to ovarian cancer.