Breast　cancer　is　the　most　commonly　diagnosed　cancer　in　women　and　is　the　leading　cause　of　cancer-related　mortality　among　female　patients　across　the　world.　Chemotherapy　is　a　critical　means　for　breast　cancer　therapy,　and　administration　of　chemotherapy　could　reduce　the　risk　of　recurrence　by　approximately　one-third　in　early　breast　cancer.　However,　multidrug　resistance　represents　a　principal　obstacle　to　effective　chemotherapeutic　interventions　against　breast　cancer　and　is　an　increasing　clinical　challenge,　creating　an　urgent　demand　to　explore　innovative　chemotherapeutics　to　combat　this　formidable　disease.　Quinazoline　hybrids　with　structural　and　mechanistic　diversity　exhibit　excellent　activity　against　breast　cancers　including　drug-resistant　forms　and　have　the　potential　to　reduce　side　effects　caused　by　the　corresponding　pharmacophores.　Notably,　lapatinib,　a　quinazoline-furan-sulfone　hybrid,　has　already　been　launched　for　breast　cancer　therapy.　Thus,　quinazoline　hybrids　represent　a　fertile　source　for　the　development　of　novel　chemotherapeutics　for　clinical　deployment　in　the　control　and　eradication　of　breast　cancer.　This　review　emphasizes　the　current　scenario　of　quinazoline　hybrids　with　antibreast　cancer　therapeutic　potential　and　focuses　on　structure-activity　relationships　(SARs)　and　modes　of　action,　developed　from　2020　onwards,　to　facilitate　the　rational　discovery　of　more　effective　antibreast　cancer　candidates.This　review　emphasizes　the　current　landscape　of　quinazoline　hybrids　with　antibreast　cancer　therapeutic　potential,　delves　into　structure-activity　relationships　and　mechanisms　of　action　developed　from　2020　onwards,　aiming　to　facilitate　the　rational　discovery　of　more　effective　and　less　toxic　candidates.