Cancer patients need better anticancer drugs, and medicinal chemistry can play a critical
role in the discovery of these drugs. For an efficient drug discovery process, chemists working on the
synthesis of potential anticancer agents need to use reliable screening methods. These methods should
not only detect the compounds with the highest therapeutic potential, but should also predict whether
such potential is high enough to deserve additional attention. Unfortunately, the current strategies for
assessing anticancer activity in vitro are unable to do this reliably. This review article analyzes these
strategies and describes an alternative screening approach. It is based on establishing suitable experimental
conditions to detect compounds that improve the selective cytotoxicity of the drugs used in
cancer therapy. This patient-oriented approach is easy to implement and may help medicinal chemists, and other researchers
involved in cancer drug discovery, assess in vitro anticancer activity more reliably.
Keywords: Antitumor activity, cancer, cytotoxic activity, drug discovery, screening, selectivity.
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