Development Of Drug Design : A New Anticancer Drug

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Development of Drug Design
Scientists aim to produce a new anticancer drug which will meet all requirements by exploring and understanding the structure and reactivity of the molecule. It is specifically focused on transition metal-based anticancer drug. Transition metals have unique properties and reactivity. They have different oxidation state which able them to interact with molecules of different negative charges. The metals are co-ordinated by different ligands which contribute to different chemical properties. The common anticancer drug produced is platinum-based drug. [TALK MORE ON Pt BASED THERAPIES]
Problem with current anticancer drug
Cancer occurs when there is an uncontrolled multiplication of tumour
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Ways on how anticancer drug works
The main target in cancer treatment is to design an inactive, selective pro-drug which will bind to tumour cells only without affecting the healthy cells. Pro-drug contains the active parent drug which will only be released upon an enzymatic or chemical reaction. The activation of metal-based anticancer pro-drugs is different from an organic pro-drug. In the organic pro-drug, its activation mainly uses the conversion of enzyme. On the other hand, a metal-based pro-drug can be activated via three methods. These methods have to consider the timescale of the whole process. There must be enough time for the drug to arrive at the binding site of the DNA before being activated. Moreover, the activation must be carried out before the drug is excreted. Activation via Substitution of Ligand
The first method involves the substitution of ligands shown in Figure 1. A typical activation process is the hydrolysis of a metal-halide bond. An example of a pro-drug is cisplatin, cis-[Pt(NH3)2Cl2] (Figure 2). It is one of the earliest anticancer drugs discovered and is active in treating testicular cancer. By the hydrolysis of Pt-Cl bond in Figure 3, the drug is now active to bind to the DNA of the tumour cell.
[FIGURE 1: Mechanism of ligand substitution]
The rate of exchange of ligand is crucial in drug
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