Organic compounds containing the F or B elements in their structures have recently attracted the interest of the chemists and medicinal chemists because their improved biological properties displayed in comparison to their non-fluorinated or non-borinated parent structures. It is widely been documented that curcumine (CUR) have a high biological potential as antioxidant, anti-inflammatory and anticancer agent, among others, but some drawbacks related to its unfavorable bio-physicochemical properties have prevented its applicability as chemotherapeutic drug. Nevertheless, recent studies have shown that the introduction of the BF 2 functionality in its structure (i.e. CUR-BF 2 adducts) and analogues have significantly improved their biological properties, mainly, their anticancer and antibiotic activities. On the other hand, the BF 2 -adduct BODIPY (i.e. 4,4-difluoro-4-bora-3a-azonia-4a-aza- s -indacene) and derivatives are widely known by their outstanding photophysical properties displayed. However, recently it have increased the interest in such structures, but this time, for the biological properties that these fluorescent compounds are also shown, as convenient probes for diverse biological targets. Focusing on the above findings, we were interested into compile, in this review article, the literature documented since 2000–2020 exclusively engaged with the synthetic strategies established for the synthesis of curcumine-BF 2 adducts, BODIPY and their related derivatives, in which the biological properties displayed by such structures have been highlighted. Remarkably, the biological activities displayed by the aforementioned BF 2 -based compounds are mainly related with cell imaging studies, biomolecules recognition and labels, antibiotic properties and antiproliferative agents, which were conveniently used to organize them in concise Tables and Schemes to facilitate their comparisons, and to underscore the key points of the present review.