Cytostatic Activity of Some Novel Amidocarbamate Derivatives of Ketoprofen (Clinical Report‪)‬

1. Introduction Ketoprofen (Ket) is a non-steroidal anti-inflammatory drug (NSAID) with pronounced analgesic and antipyretic properties. Various ketoprofen derivatives have been synthesized in order to minimize side-effects, prolong plasma half-life and increase solubility [1,2]. Some amides have proved to be useful prodrugs, while the others possess anti-inflammatory activity independent of the parent compound. It has been demonstrated that amidation of NSAIDs improves selectivity towards COX-2 [3], while modification of the carboxylic group to hydroxamic acid leads to inhibition of both cyclooxygenase and 5-lipoxygenase, these two enzymes are crucial in inflammatory processes [4,5]. Glycine amides of ketoprofen and several-other well-known NSAIDs are significantly less irritating to gastric mucosa, while their anti-inflammatory activities are comparable to their parent drugs [6]. Numerous studies suggest that NSAIDs are promising anticancer drugs and may be associated with reduced risk of colon, lung, liver and other types of cancers [7]. In this paper, a series of novel amidocarbamate derivatives of ketoprofen 4a-j was prepared, characterized and screened for their antioxidative, cytostatic and antiviral activities.