Molecular docking and biological activities of Ni(II), Cu(II) and Co(II) complexes with a new potentially hexadentate polyamine ligand; X-ray crystal structure of the Cu(II) complex.

Three new metal complexes have been obtained from the reaction of a new polyamine (L) with Ni(II), Cu(II), and Co(II) ions. The X-ray structural analysis of the Cu(II) complex shows that the copper atom is in a very distorted square pyramidal environment, coordinated by five of the six nitrogen donor atoms of the potentially hexadentate ligand. To evaluate the biological potential of the ligand and the synthesized metal complexes, their binding behavior with DNA was studied by molecular modeling methods. The Molecular docking studies showed that the free ligand and its complexes were bound to the major groove of DNA. The antioxidant activities of the ligand and its metal complexes were also assessed, in vitro, using 2,2-diphenyl-1-picrylhydrazyl. The synthesized compounds were tested for activity against lung carcinoma epithelial cells (A549) using the MTT cell viability assay. A comparative study of the IC50 values indicated that the Cu(II) complex exhibited the highest activity, while the Co(II) and Ni(II) complexes showed more potent antiproliferative activity than the ligand. The antibacterial activities of the synthesized complexes were evaluated using micro-broth dilution and disk diffusion methods. The complexes showed greater antibacterial activity than the free ligand.Communicated by Ramaswamy H. Sarma.

Unexpected synthesis of 4-(4,5-dihydro-1H-imidazol-2-ylsulfanyl)butyl-H-sulfite as a catalyst for the synthesis of pyrazolophthalazines.

Several attempts for preparation of 4,4'-(2-thioxoimidazolidine-1,3-diyl)bis(butane-1-sulfonic acid) were not successful despite taking 2 mmol of 1,4-butane sultone in reaction with 1 mmol of imidazolidine-2-thione. Instead, 4-(4,5-dihydro-1H-imidazol-2-ylsulfanyl)butyl hydrogen sulfite (DISBHS) was prepared unexpectedly, characterized and used for the synthesis of diverse pyrazolophthalazines from the one-pot three component condensation reaction of phthalhydrazide, malononitrile and aldehydes under mild conditions.

Bacteria and cancer: Different sides of the same coin.

Conventional cancer therapies such as chemotherapy, radiation therapy, and immunotherapy due to the complexity of cancer have been unsuccessful in the complete eradication of tumor cells. Thus, there is a need for new therapeutic strategies toward cancer. Recently, the therapeutic role of bacteria in different fields of medicine and pharmaceutical research has attracted attention in recent decades. Although several bacteria are notorious as cancer-causing agents, recent research revealed intriguing results suggesting the bacterial potential in cancer therapy. Thus, bacterial cancer therapy is an alternative anticancer approach that has promising results on tumor cells in-vivo. Moreover, with the aid of genetic engineering, some natural or genetically modified bacterial strains can directly target hypoxic regions of tumors and secrete therapeutic molecules leading to cancer cell death. Additionally, stimulation of immune cells by bacteria, bacterial cancer DNA vaccine and antitumor bacterial metabolites are other therapeutic applications of bacteria in cancer therapy. The present study is a comprehensive review of different aspects of bacterial cancer therapy alone and in combination with conventional methods, for improving cancer therapy.