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Indian Journal of Chemistry -Section A (IJC-A) >
IJC-A Vol.50A [2011] >
IJC-A Vol.50A(03-04) [March-April 2011] >
| Title: | Copper(I) complexes of modified nucleobases and vitamin B3 as potential chemotherapeutic agents: In vitro and in vivo studies |
| Authors: | Sanghamitra, N J M
Adwankar, M K
Juvekar, A S
Khurajjam, V
Wycliff, C
Samuelson, A G |
| Keywords: | Bioinorganic chemistry
Metallodrugs
Copper
Antitumor activity
Thiopyrimidine
Nicotinamide
Cytotoxicity
Lipophilicity |
| Issue Date: | Mar-2011 |
| Publisher: | NISCAIR-CSIR, India |
| Abstract: | Three new complexes of Cu(I) have been
synthesized using ancillary ligands like thiopyrimidine (tp) a modified nucleobase, and nicotinamide (nic) or vitamin B3, and characterized by spectroscopy and X-ray
crystallography. In vitro
cytotoxicity studies of the complexes on various human cancer cell lines such
as Colo295, H226, HOP62, K562, MCF7 and T24 show that [Cu(PPh3)2(tp)Cl] (1) and [Cu(PPh3)2(tp)]ClO4 (2)
have in vitro cytotoxicity comparable
to cisplatin. Complex [Cu(nic)3PPh3]ClO4
(3) is non-toxic and increases
the life span by about 55 % in spontaneous breast tumor model. DNA binding and
cleavage studies show that complex (3)
binds to calf thymus DNA with an apparent binding constant of 5.9 x 105 M and
completely cleaves super-coiled DNA at a concentration of 400  M, whereas complexes (1) and
(2) do not bind DNA and do not show
any cleavage even at 1200 M. Thus, complex (3) may exhibit cytotoxicity via DNA
cleavage whereas the mechanism of cytotoxicity of (1) and (2) probably
involves a different pathway. |
| Page(s): | 465-473 |
| CC License: |  CC Attribution-Noncommercial-No Derivative Works 2.5 India |
| ISSN: | 0975-0975(Online); 0376-4710(Print) |
| Source: | IJC-A Vol.50A(03-04) [March-April 2011]
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