engleski

Antiproliferative and Antiviral Activity of Three Libraries of Adamantane Derivatives

A number of different antiviral drugs exists nowadays on the market. However, combating viral diseases and finding appropriate drugs with minimal side effects remain a challenge in chemistry, pharmacy and medicine. A major problem in antiviral therapy is the rapid mutations of viruses leading to development of drug resistance. Amantadine (1-aminoadamantane hydrochloride) and rimantadine [1-(2-aminoethyl)adamantane hydrochloride], are widely used as anti-influenza agents that block M2 protein ion channel which prevents fusion of the virus with the host-cell membrane and release of viral RNA into the cytoplasm [1]. The same compounds have been shown to exhibit inhibitory activity - although rather modest - against some other viruses such as HIV [2], hepatitis [3], and herpes simplex virus [4]. However, inappropriate use of these drugs in many countries contributed to an increasing number of resistant influenza viruses [5]. In the search of new drugs and novel mechanisms of action based on yet unknown intracellular targets, it is important to screen new libraries of molecules and develop new structure-activity relationships (SAR). Herein we report an investigation of the antiviral activity in vitro of three libraries of adamantane derivatives. In addition the same libraries of compounds were also tested for antiproliferative activity. Recently we have reported an investigation of antiproliferative activity of a series of adamantylphthalimides, where all investigated compounds exhibited higher activity than the clinically used drug Thalidomide [6].

Antiproliferative agents; Anticancer activity; Antitumor activity

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