Bleomycin mimic

Date: Jul.2000
(1) An artificial Cu(II) complex with intringuing oxygen radicalquenching profile. X-ray structure, cytochrome c assay, and ESR study.
Msami Otsuka, Honoo Satake, Satoru Murakami, Mitsunobu Doi, Toshimasa Ishida, Masakatsu Shibasaki and Yukio Sugiura. (1996). Bioorg. Med. Chem. 4, 1703-1708.

Since reactive oxygen species (ROS) play critical roles invarious biological processes, such as defense of human biochemical system or signal transduction pathways associated with immune responce and growth control, development of oxygen activators or scavengers of oxygen radical is of increasing importance. Recently, we have reported that novel ligand, constructed from pyridine and histidine units, namely HPH, showed potent activity to active molecular oxygen, as demonstrated by ESR spin trapping. Herein we reported our finding that replacement of the secondary amino linkage of HPH by a peptide bond, as envisaged in HPH-Pep switches the oxygen-activating capability to the reverse activity to scavenge oxygen radical. In addtion, enzyyme assay and ESR studies indicated that the Cu(II) complex of the new ligand HPH-Pep has an intriguing radical-scavenged superoxide specifically wothout and hydroxyl radical, and HPH-Pep-Cu(II) did not generate hydorgen peroxide upon scavenging superoxide.

(2) Synthesis, Characterization, and spectroscopic properties of three novel pentadentate copper(II) complex related to the metal-chelating inhibitors against DNS binding with HIV-EP1.
Kurosaki, H.; Sharma, R.K.; Aoki, S.; Inoue, T.; Okamoto, Y.; Sugiura, Y.; Doi, M.; Ishida, D.; Otsuka, M.; Goto, M. (2001)
J. Chem. Soc., Dalton Trans. 441-447.

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X-Ray Data Summary
formulaC23 H21 Cu N6 O5, 2(H2 O)
weight 561.03
space groupP43212
Cell Crystal
a 16.854(5) Ang. description block
b 16.854(5) Ang. colour green
c 19.824(9) Ang. size (mm) 0.5x0.3x0.3
alpha 90 deg. Dx (g/ml) 1.324
beta 90 deg. F(000) 2320
gamma 90 deg. mu(CuKa) 1.523
volume 5631(3) Ang^3
Z 8
Diffrn measurementRefinementspace
device type Rigaku AFC5R/RU-200 Flack -0.16(9)
decay 1.0 % parameters 335
index limit 0-h-19, 0-k-13, -22-L-0 restraints 0
theta (deg.) 3.44-62.22 R_factor_gt 0.0791
total reflections2548 wR_factor_gt 0.2103
reflections(obs) 2375 .gt. 2sigma(I) dela rho_max 1.173 e A^3
Structurespace space space space space space delta rho_min -0.407 e A^3
solution SHELXS-97 shift/su_maxlt.0.001
refinementSHELXL-97 Goodness of fit 1.092

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