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Abstract Metal-based chemotherapeutic agents have gained considerable attention after discovery of cisplatin, cis-[Pt(NH3)2Cl2], drug used for treatment of solid malignancies, in particular, testicular and ovarian cancers. Despite its success, serious concerns have arisen regarding the systematic toxicity, intrinsic resistance and the narrow spectrum of activity for phenotypes of cancer and patient compliance. Thus, much attention has been paid to the development of platinum and non-platinum anticancer drugs based on transition-metal ions bonded to biologically important organic molecules. The choice of metal ions plays an important role in the design of metal-based chemotherapeutic drugs. The biocompatible Zn(II) ion can be utilized to minimize the toxicity, as it is familiar with the biological environment of the human body. The second- and third-row transition-metal ions, Pd(II), Pt(II), Ag(I) and Au(III), have low hydrolysis rates, which is also a recommended feature for the biological systems. Nonsteroidal anti-inflammatory drugs (usually abbreviated to NSAIDs) are a class of drugs that provides analgesic (pain-killing) and antipyretic (fever-reducing) effects. NSAIDs inhibit the activity of both cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) and, thereby, the synthesis of prostaglandins and thromboxanes. Most nonsteroidal anti-inflammatory drugs are weak acids with a pKa of 3-5. They are absorbed well from the stomach and intestinal mucosa. Thus, the discovery of new anti-inflammatory drugs with little or no side effects is essential. 2-(2’-hydroxy-5’-methyl) phenyl benzotriazole (Hhmbt) is a chromophore with a pKa higher than 5 and is expected to have no side effects in the stomach (thus minimizing gastrointestinal bleeding and ulcers). This thesis consists of three main chapters, viz., Chapter 1 (Introduction), which presents an overview of the pertinent literature; Chapter 2 (Experimental) which describes the methods and measurements employed in this study as well as the methods of preparation of the complexes and the conditions employed for the biological applications; and Chapter 3 (Results and Discussion), which details the characterization of the complexes, the in vivo anti-inflammation activity, the in vitro anticancer activity and the in vitro DNA studies, which were carried out by circular dichroism (CD) spectroscopy. |