annual report annual report annual report annual report 2005

RADIOCHEMISTRY, STABLE ISOTOPES,
NUCLEAR ANALYTICAL METHODS, GENERAL CHEMISTRY
a
b
69
Fig.1. Linear (a) and seven-membered (b) structures of the platinum(II) complex; possible hydrogen bonds are shown.
cause the most stable conformation of its oxygen
analog – tetrahydrofuran – appeared to be different.
The results published already of ab initio calculations
[13] suggest that the equilibrium conformation
of tetrahydrofuran is an envelope C s structure.
On the contrary, the calculations performed
in our group for the 1-methyltetrahydrofuran ring
suggest that the lowest-energy is associated to even
the most low (C 1 ) symmetry of the ring.
Biological investigations
Cytotoxicity of the studied complex was estimated
in vitro by means of the relative growth test
with 1 hour exposure to the drug, as described elsewhere
[14]. Studies were performed with the mouse
lymphoma cell line L1210. The 50% inhibition dose
(ID 50 ) was determined by extrapolation of the steep
part of survival curves obtained. Concentration
range of the investigated species was 0.01-0.150
mg·cm –3 . Precision of the calculated ID 50 value was
estimated using the propagation of measuring uncertainty
technique, and the error limits of the estimates
for the slope and intercept of survival curves.
If the toxicity of the reference CDDP was found
to be ID 50 =5 µM [15], the ID 50 of the species investigated
in the presented work appeared to be
about 313.8±10.8 and 10.63±1.31 µM for the
ligand and complex, respectively (Fig.2). The latter
value, being comparable to that for CDDP, suggests
the necessity of determining the therapeutic
Fig.2. Cytotoxicity of the studied ligand and platinum(II)
complex.
index of the complex (TI=LD 50
/ID 90
; TI of the
CDDP being 8.1 [16]) as well as of checking its toxicity
against other tumor lines.
We thank Prof. Adam Krówczyński (Department
of Chemistry, Warsaw University) for synthesizing
the ligand.
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