Novel peptidomimetic compounds containing redox active chalcogens and quinones as potential anticancer agents

Abstract

CitationNovel peptidomimetic compounds containing redox active chalcogens and quinones as potential anticancer agents.

Sulfur, selenium and tellurium pseudopeptides: Synthesis and biological evaluation

“…Furthermore, we have also shown that the tellurium containing compounds 6 and 5 are generally able to enhance the oxidation of thiols in the presence of H 2 O 2 , using a simple in vitro thiophenol oxidation assay. 11,12 In continuation of our previous work, the ROS levels in (the more robust) A 431 cells were monitored using the standard fluorescent 2`, 7` dichlorodihydrofluorescin diacetate (DCHFA) assay, which can be considered as a general ROS indicator, as DCHFA reacts readily with most common ROS, including H 2 O 2 , lipid hydroperoxides and ONOO − . 17 As suspected, in the concentration range used, sulfur and selenium based compounds were unable to disturb the ROS levels in A 431 melanoma cells over a 1 h treatment period.…”

Synthesis and antitumor activity of selenium-containing quinone-based triazoles possessing two redox centres, and their mechanistic insights

“…GPx targets redox sensitive thiol proteins, while simultaneously generating reactive oxygen species at a critical threshold. Thus, these drugs act as ROS-users and ROS-enhancers to affect downsteam targets [37]. This action would complement the mechanism of action of β-lap, since death caused by this agent relies upon the hyperactivation of PARP1, which is stimulated by ROS (H 2 O 2 ) [24].…”

Groebke–Blackburn–Bienaymé multicomponent reaction: emerging chemistry for drug discovery

“…The component variations, postmodifications and secondary transformations will also be discussed. For general information about MCRs, IMCRs and their applications in the synthesis of biologically relevant heterocycles, the reader is directed towards more comprehensive reviews and monographs [13,18,19,[22][23][24][25][26][27][28][29][30][31][32][33][34][35][36][37]. …”

“…Furthermore, the advancement of the reaction was only depicted on the basis of various catalysts explored, neglecting its synthetic applications, scopes and secondary transformations. With this in mind and our interest in MCRs and drug discovery [18][19][20][21][22][23], we herein summarize the efforts of the chemical community in the progress and applications of GBBR since 1998. This review will cover the biological profiles, synthetic scopes and respective proposed mode(s) of action of GBBR products.…”