Cancer　is　one　of　the　most　fatal　threatens　to　human　health　throughout　the　world.　The　major　challenges　in　the　control　and　eradication　of　cancers　are　the　continuous　emergency　of　drug-resistant　cancer　and　the　low　specificity　of　anticancer　agents,　creating　an　urgent　need　to　develop　novel　anticancer　agents.　Organometallic　compounds　especially　ferrocene　derivatives　possess　remarkable　structural　and　mechanistic　diversity,　inherent　stability　towards　air,　heat　and　light,　low　toxicity,　low　cost,　reversible　redox,　ligand　exchange,　and　catalytic　properties,　making　them　promising　drug　candidates　for　cancer　therapy.　Ferrocifen,　a　ferrocene-phenol　hybrid,　has　demonstrated　promising　anticancer　properties　on　drug-resistant　cancers.　Currently,　Ferrocifen　is　in　pre-clinical　trial　against　cancers.　Obviously,　ferrocene　moiety　is　a　useful　template　for　the　development　of　novel　anticancer　agents.　This　review　will　provide　an　overview　of　ferrocene-containing　hybrids　with　potential　application　in　the　treatment　of　cancers　covering　articles　published　between　2010　and　2020.　The　mechanisms　of　action,　the　critical　aspects　of　design　and　structure-activity　relationships　are　also　discussed.　(C)　2020　Elsevier　Masson　SAS.　All　rights　reserved.