Molecular mechanisms of cytotoxic side effects of platinum anti-cancer drugs – a molecular orbital studyReport as inadecuate




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Abstract : The side effects of Pt drugs have been examined by evaluating the literature on Pt chemistry, pharmacology, cellular transport, and clinical efficacy and correlating these studies with molecular orbital computations. It is concluded that Pt chemotherapeutical regimes are dominated by side reactions, particularly hydrolysis in blood serum and delivery efficiency. For example, it is shown that transplatin is therapeutically inactive because it hydrolyses faster in blood serum than ciplatin, so little transplatin reaches its target DNA. The reactivity of charged hydrolysis products determines the severity of side effect. The reactivity indicators of the approved Pt drugs and their various hydrolysed species are calculated. The cellular uptake of Pt is fastest for neutral species, with high lipophilicity, since their desolvation penalties for crossing the cell membrane are lowest. Objective Cytotoxic side effects of antineoplastic chemotherapeutic Pt drugs: to examine biophysical molecular properties that could be used to predict the propensity of Pt drugs to cause unwanted side effects

Keywords : molecular orbital computations Platinum drugs anti-cancer side effects cellular uptake





Author: Clifford Fong -

Source: https://hal.archives-ouvertes.fr/



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