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The fusion of heterocycles onto an anthraquinone scaffold represents a promising strategy to optimize anticancer activity. This study has the aim to synthesize and characterize novel anthra[1,2-b]furan compounds based on the natural product aloe-emodin. Six novel anthra[1,2-b]furans bearing phenyl, n-hexane, and methoxy carbonyl substituents were synthesized starting from aloe-emodin. The synthetic route employed involved acetyl protection of aloe-emodin, electrophilic aromatic halogenation, subsequent Castro–Stephens coupling, spontaneous intramolecular cyclization, and deprotection of hydroxyl groups. These newly synthesized compounds were evaluated for their cytotoxic activity against various cancer cell lines, including lung adenocarcinoma (A5492), colorectal carcinoma (HCT116), hepatocellular carcinoma (HepG2), ovarian cancer (Skov3), and breast cancer (MCF-7), using the CCK8 assay. The anthra[1,2-b]furan derivative 10c, which contains a methoxy carbonyl group, demonstrated excellent potency against lung (A549) and breast (MCF-7) cancer cell lines, with IC50 values of 0.49 and 2.91 µM, respectively. This preliminary cytotoxic finding shows compound 10c as a promising hit for further investigations towards a promising lead compound.

Aloe vera plant is known worldwide for its medicinal properties and application in gel-based products such as shampoo, soap, and sunscreen. However, the demand for these gel-based products has led to a surplus production of Aloe vera processing waste. An Aloe vera gel processing facility could generate up to 4000 kg of Aloe vera waste per month. Currently the Aloe vera waste is being disposed to the landfill or used as fertilizer. A sustainable management system for the Aloe vera processing waste should be considered, due to the negative societal and environmental impacts of the currents waste disposal methods. Therefore, this review focuses on various approaches that can be used to valorize Aloe vera waste into value-added products, such as animal and aquaculture feeds, biosorbents, biofuel and natural polymers. Researchers have reported Aloe vera waste for environmental applications biosorbents used for wastewater treatment of various pollutants. Several studies have also reported on the valorization of Aloe vera waste for production of biofuels such as bioethanol, mixed alcohol fuels, biogas and syngas. Aloe vera waste could also be valorized through isolation and synthesis of natural polymers for application in wound dressing, tissue engineering and drug delivery systems. Aloe vera waste valorization was also reviewed through extraction of value-added bioactive compounds such as aloe-emodin, aloin and aloeresin. These value-added bioactive compounds have various applications in the cosmetics (non-steroidal anti-inflammatory, tyrosinase inhibitors) and pharmaceutical (anticancer agent and COVID 19 inhibitors) industry.

Aloe-emodin is an anthraquinone with a wide range of medicinal applications, including anti-angiogenic, anticancer, antimicrobial, antiviral, anti-inflammatory, and antioxidant activities. In this review, the functionalization of aloe-emodin using various synthetic methods, including alkylation, condensation, esterification, the Finkelstein reaction, and the Kabachnik–Fields reaction was reported. The biological activity of the synthesized aloe-emodin derivatives is discussed, with a focus on their potential future applications as anticancer agents, enzyme inhibitors, anti-inflammatory agents, and antimicrobial agents. This review also discusses the structure–activity relationship (SAR) and the mechanism of action (e.g., molecular docking studies, cell membrane-disrupting capacity, and apoptosis studies). This review highlights the many contributions made towards the design and development of novel, biologically active aloe-emodin derivatives.