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Benzarone
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
Benzarone is a member of the 1-benzofurans. It has been described as antiarrhythmic, agent for anti-varicose therapy, antihemorrhagic drug and vasoprotective agent. In Taiwan, it may be used for the treatment of capillary fragility and capillary bleeding (1).
Amiodarone pulmonary toxicity
Published in Philippe Camus, Edward C Rosenow, Drug-induced and Iatrogenic Respiratory Disease, 2010
Philippe Camus, Thomas V Colby, Edward C Rosenow
The amiodarone molecule (M = 643.3) is notable for the following reasons.It has a benzofuran ring which gives the drug high lipid solubility – hence the storage of amiodarone in tissues, notably the lung, liver and fat. The latter acts as a reservoir for drug bidirectional storage and efflux. The benzofuran ring per se may not explain the drug’s pulmonary toxicity.It has a cationic hydrophilic side-chain, which renders the drug amphiphilic and lysosomotropic. This explains its sequestration in the acidic milieu of lysosomes, where amiodarone blocks phospholipid processing, turnover and clearance, causing phospholipids to build up in cells of lung, liver, nerves and other organs.It has two iodine atoms, which play a mechanistic role in the thyroid and pulmonary adverse effects of the drug, and account for the high Hounsfield numbers on imaging of tissues where amiodarone sequesters, notably liver and lung.
Identification of 3-(piperazinylmethyl)benzofuran derivatives as novel type II CDK2 inhibitors: design, synthesis, biological evaluation, and in silico insights
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2022
Wagdy M. Eldehna, Raed M. Maklad, Hadia Almahli, Tarfah Al-Warhi, Eslam B. Elkaeed, Mohammed A. S. Abourehab, Hatem A. Abdel-Aziz, Ahmed M. El Kerdawy
Benzofuran is a privileged scaffold exhibiting numerous biological activities amongst them are analgesic, antifungal, antibacterial, anti-hyperlipidemic, antihyperglycemic, anti-inflammatory, antioxidant, antipyretic, antiviral, as well as antitumor actions41–44. Benzofuran-based derivatives can exert the antitumor actions via several mechanisms such as the inhibition of farnesyltransferase, oestrogen receptor, human peptide deformylase, tubulin polymerisation, angiogenesis, or carbonic anhydrases41,45. In addition, many benzofuran-based small molecules mediate their anticancer actions through protein kinases inhibition such as GSK-3β44,46, mTOR signalling47,48, Pim-149, Src kinase50, as well as CDK244. Compounds II showed a potent CDK2 inhibitory activity with IC50 of 52.75 nM inducing cell cycle arrest of MCF-7 breast cancer cells wihin the G2/M phase causing cell apoptosis44.
Benzofuran as a promising scaffold for the synthesis of novel antimicrobial agents
Published in Expert Opinion on Drug Discovery, 2022
Ashraf A. Abbas, Kamal M. Dawood
Many infections and diseases in humans and animals are usually caused by the gram-positive pathogen (S. aureus) and antibiotics are commonly used against infections caused by S. aureus. In this regard, it is worth mentioning that most of the benzofuran derivatives, described in this review, are highly potent inhibitors against S. aureus with either equipotent or more potent activity than the reference antibiotic drugs. In addition, most of the reported benzofurans are highly active against a panel of more than 20 Gram-positive and Gram-negative bacterial and fungal microorganisms. The need for new antimicrobial agents is an important issue relating to human health. From the reported data, it can be assumed that several benzofurans are good candidates for development as potential future antibiotic drugs for the treatment of serious bacterial and fungal infections. These findings will undoubtedly drive many specialists in the medicinal and pharmaceutical research fields to make extra efforts and deeper studies into in vivo experiments to reach the outmost challenges and prominent benefits to improve human health and reduce suffering. The occurrence of the benzofuran scaffold in many highly bioactive natural products and synthetic compounds is of great value for researchers working in drug design, discovery and development. Finally, antimicrobial efficacy was greatly affected by the electronic nature of substituents on the benzofuran skeleton(s); therefore, significant efforts must be made to study the effects of substituents that highly enhance the drug-like properties of benzofuran scaffolds.
LSD1 inhibitors for anticancer therapy: a patent review (2017-present)
Published in Expert Opinion on Therapeutic Patents, 2022
Yi-Xin Lv, Sheng Tian, Zhou-Dong Zhang, Tao Feng, Huan-Qiu Li
Many benzofuran derivatives have potent antiproliferative activity, making the benzofuran scaffold an important unit in drug discovery. In a lipophilic environment, acylhydrazone compounds are a class of Schiff base compounds formed by the condensation of hydrazine with an aldehyde or a ketone. They have good biological activity, strong coordination ability, and various coordination modes [50]. In 2020, Ye et al. developed a novel series of benzofuran acylhydrazones against LSD1, and compounds 21 and 22 demonstrated promising LSD1 inhibitory activity (Figure 8), with IC50 values of 7.2 nM and 14.7 nM, respectively [51]. The two hydroxyl groups of compound 21 formed hydrogen bond interactions with Phe558 and Asn806 (Figure 9). Compound 22 was also found to have potent antiproliferative properties in four cancer cell lines (U-87, HT-29, MCF-7, and PANC-1) [52].