Synthesis, characterization, and in vitro antimalarial and antitumor activity of new ruthenium(II) complexes of chloroquine.
Synthesis, characterization, and in vitro antimalarial and antitumor activity of new ruthenium(II) complexes of chloroquine.
复制标题
DOI：
10.1021/ic802220w
复制
发表时间：
2009-02-02
影响因子：
4.6
通讯作者：
Sánchez-Delgado RA
中科院分区：
文献类型：
--
作者：
Rajapakse CS;Martínez A;Naoulou B;Jarzecki AA;Suárez L;Deregnaucourt C;Sinou V;Schrével J;Musi E;Ambrosini G;Schwartz GK;Sánchez-Delgado RA
The new RuII chloroquine complexes [Ru(η6-arene)(CQ)Cl2] (CQ = chloroquine; arene = p-cymene 1, benzene 2), [Ru(η6-p-cymene)(CQ)(H2O)2][BF4]2 (3), [Ru(η6-p-cymene)(CQ)(en)][PF6]2 (en = ethylenediamine) (4), and [Ru(η6-p-cymene)(η6-CQDP)][BF4]2 (5, CQDP = chloroquine diphosphate) have been synthesized and characterized by use of a combination of NMR and FTIR spectroscopy with DFT calculations. Each complex is formed as a single coordination isomer: in compounds 1–4 chloroquine binds to ruthenium in the η1-N mode through the quinoline nitrogen atom whereas in complex 5 an unprecedented η6 bonding through the carbocyclic ring is observed. Compounds 1, 2, 3, and 5 are active against CQ-resistant (Dd2, K1 and W2) and CQ-sensitive (FcB1, PFB, F32 and 3D7) malaria parasites (Plasmodium falciparum); importantly, the potency of these complexes against resistant parasites is consistently higher than that of the standard drug chloroquine diphosphate. Complexes 1 and 5 also inhibit the growth of colon cancer cells, independently of the p53 status and of liposarcoma tumor cell lines with the latter showing increased sensitivity, especially to complex 1 (IC50 8 µM); this is significant because this type of tumor does not respond to currently employed chemotherapies.
登录
查看更多内容
影响因子：
1.2
作者：
Dougan, Sarah J.;Sadler, Peter J.
通讯作者：
Sadler, Peter J.
影响因子：
2.8
作者：
FISH, RH;KIM, HS;FONG, RH
通讯作者：
FONG, RH
DOI：
10.1039/b205432a
发表时间：
2002-01-01
期刊：
JOURNAL OF THE CHEMICAL SOCIETY-DALTON TRANSACTIONS
影响因子：
--
作者：
Beagley, P;Blackie, MAL;Smith, PJ
通讯作者：
Smith, PJ
DOI：
10.1039/dt9740000233
发表时间：
1974-01-01
期刊：
JOURNAL OF THE CHEMICAL SOCIETY-DALTON TRANSACTIONS
影响因子：
--
作者：
BENNETT, MA;SMITH, AK
通讯作者：
SMITH, AK
影响因子：
168.9
作者：
Alonso, PL;Sacarlal, J;Cohen, J
通讯作者：
Cohen, J