Indandione is a hydrocarbon classified as bicyclic aromatic β-diketone. It can be applied in many fields of science and industry. It is successfully used as a substrate in organic synthesis, pharmaceutical sciences and as a substrate for the production of dyes. Indandione derivatives and analogs are useful in medicine, chemistry and the judiciary. Among the indandione derivatives can find compounds that have interesting properties and many of them have biological activity (incl. anticancer, anticoagulation, anti-inflamatory, antimicrobial activities). Based on the indan-1,3-dione structure created acetylcholinesterase inhibitors. Indan-1,3-dione derivatives are also used as a derivating agent for the analysis of fatty aldehydes and a substance that is an element of dye-sensitized solar cells. This work presents a brief overview of construction, properties and activities of indandione and its derivatives. This work describes selected indandione derivatives that have properties useful in medicine and industry with particular regard to the anticoagulants and neuroprotective activities in AD.
2-Arylidene-indan-1,3-done derivatives have very different properties, thanks to which they find various applications in science, medicine, and industry. Selected derivatives show antiviral, antibacterial, and anti-inflammatory activity. This paper presents a procedure for the synthesis of a series of indan-1,3-dione derivatives that present antiproliferative activity. The aim of the work was to develop a method of simple synthesis and purification, evaluate the fulfillment of the Lipiński’s and Veber’s rule, and determine the potential scope of application of the obtained series of compounds. The structure of the synthesized compounds was confirmed, and their lipophilicity was determined using experimental and computational methods. Their antiproliferative activity against selected cell lines was tested in accordance with the MTT protocol; the ability to bind to albumin was tested, and the parameters related to the toxicity of substances in silico were determined. The selected compounds which showed antiproliferative activity were strongly bound to albumin and, in most cases, met the Lipiński’s and Veber’s rule. Thus, the obtained results suggest that 2-arylidene-indan-1,3-done derivatives appear to be good candidates for drugs with a potential leading structure for further development.
Heterocyclic oxime ethers play a significant role in organisms due to their biological activity. Lipophilicity is an important parameter that may affect biological activity of the compounds 1-(benzofuran-2-yl)ethan-1-one oxime and its nine biologically active ethers. The relationship between the structure and lipophilicity parameters (log k w values) of the ten compounds is here described. Reversed phase high performance liquid chromatography (RP-HPLC) method was used having methanol, 2-propanol and acetonitrile as organic modifiers of the mobile phases. Both experimental (log k w ) and calculated (log P) parameters showed to be strongly positively correlated. The weakest correlation with all the data was for the log k w methanol. For all of analyzed compounds, log k w values are smaller than 5 (except for analyses carried out in methanol), and this result corresponds to the Lipinski's rule in the range of lipophilicity. Therefore, in the case of their use as drugs, they will be probably active after oral application.
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