TY - JOUR
T1 - Synthesis and cytotoxicity of new platinum(IV) complexes of mixed carboxylates
AU - Song, Rita
AU - Park, Sun Young
AU - Kim, Yeong Sang
AU - Kim, Youngmee
AU - Kim, Sung Jin
AU - Ahn, Byung Tae
AU - Sohn, Youn Soo
N1 - Funding Information:
This research was supported by the Basic Research Program of the Korea Science and Engineering Foundation (R03-2000-000-000080(2002)) and the Ministry of Science and Technology in Korea.
PY - 2003/8/1
Y1 - 2003/8/1
N2 - In order to develop new antitumor platinum(IV) complexes with highly tuned lipophilicity, a series of (diamine)Pt(IV) complexes of the formula [PtIV(dach)L3L′] or [PtIV(dach)L2L″2] (dach=trans-(±)-1,2-diaminocyclohexane; L=acetato, propionato; L′=acetato, propionato, valerato or pivalato; L″=trifluoroacetato) have been synthesized by electrophilic substitution of the tris(carboxylato)hydroxoplatinum(IV) complexes, [PtIV(dach)L3OH] (L=acetato, propionato), with various carboxylic anhydrides such as acetic, trifluoroacetic, pivalic and valeric anhydrides. The present platinum(IV) complexes were fully characterized by means of elemental analyses, 1H NMR, mass and IR spectroscopies. The complexes 8 and 10, satisfying the appropriate range of lipophilicity (logP=0.18-1.54), exhibited high activity (ED50, 5.1 and 1.3 μM, respectively) compared with other complexes, which implies that the lipophilicity is an important factor for the antitumor activity of this series of complexes.
AB - In order to develop new antitumor platinum(IV) complexes with highly tuned lipophilicity, a series of (diamine)Pt(IV) complexes of the formula [PtIV(dach)L3L′] or [PtIV(dach)L2L″2] (dach=trans-(±)-1,2-diaminocyclohexane; L=acetato, propionato; L′=acetato, propionato, valerato or pivalato; L″=trifluoroacetato) have been synthesized by electrophilic substitution of the tris(carboxylato)hydroxoplatinum(IV) complexes, [PtIV(dach)L3OH] (L=acetato, propionato), with various carboxylic anhydrides such as acetic, trifluoroacetic, pivalic and valeric anhydrides. The present platinum(IV) complexes were fully characterized by means of elemental analyses, 1H NMR, mass and IR spectroscopies. The complexes 8 and 10, satisfying the appropriate range of lipophilicity (logP=0.18-1.54), exhibited high activity (ED50, 5.1 and 1.3 μM, respectively) compared with other complexes, which implies that the lipophilicity is an important factor for the antitumor activity of this series of complexes.
KW - Anticancer
KW - Cytotoxicity
KW - Lipophilicity
KW - Platinum(IV)
UR - http://www.scopus.com/inward/record.url?scp=12444317692&partnerID=8YFLogxK
U2 - 10.1016/S0162-0134(03)00149-1
DO - 10.1016/S0162-0134(03)00149-1
M3 - Article
C2 - 12888269
AN - SCOPUS:12444317692
SN - 0162-0134
VL - 96
SP - 339
EP - 345
JO - Journal of Inorganic Biochemistry
JF - Journal of Inorganic Biochemistry
IS - 2-3
ER -