Steriods are well-known scaffolds that have a widespread occurrence in different compounds characterized by extensive biological properties including anticancer activity. Structural modifications on steroids always generate potential lead compounds with superior bioactivity, and creation of steroid hybrids by combining steroid with other anticancer pharmacophores in one molecule, which can exert the anticancer activity through different mechanisms, is one of the most promising strategies to enhance efficiency, overcome drug resistance and reduce side effects. Sugars and azoles, can act on diverse receptors, proteins and enzymes in cancer cells, are pharmacologically significant scaffolds in the development of novel anticancer agents. Therefore, steroid-sugar hybrids cardiac glycosides and steroid-azole hybrids are privileged scaffolds for the discovery of novel anticancer candidates. This review emphasized on the development, the structure-activity relationship and the mechanism of action of cardiac glycosides and steroid-azole hybrids with potential application for fighting against various cancers including drug-resistant forms to facilitate further rational design of novel drug candidates covering articles published between 2015 and 2020.
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