Darwish, Shaban; Sadeghiani, Neda; Fong, Shirley; Mozaffari, Saghar; Hamidi, Parinaz; Withana, Thimanthi; Yang, Sun; Tiwari, Rakesh Kumar; Parang, Keykavous published the artcile< Synthesis and antiproliferative activities of doxorubicin thiol conjugates and doxorubicin-SS-cyclic peptide>, Safety of 1,2-Di(pyridin-2-yl)disulfane, the main research area is human embryonic kidney ovarian fibrosarcoma leukemia; cyclopeptide preparation antitumor doxorubicin fluorescence cellular uptake chemotherapy antiproliferative; Anticancer; Cardiotoxicity; Cellular uptake; Cyclic peptide; Disulfide; Doxorubicin; Thiol.
Myocardial toxicity and drug resistance caused by drug efflux are major limitations of doxorubicin (Dox)-based chemotherapy. Dox structure modification could be used to develop conjugates with an improved biol. profile, such as antiproliferative activity and higher cellular retention. Thus, Dox thiol conjugates, Dox thiol (Dox-SH), thiol-reactive Dox-SS-pyridine (SS = disulfide), and a Dox-SS-cell-penetrating cyclic peptide, Dox-SS-[C(WR)4K], were synthesized. Dox was reacted with Traut’s reagent to generate Dox-SH. Cytotoxicity of the compounds was examined in human embryonic kidney (HEK-293), human ovarian cancer (SKOV-3), human fibrosarcoma (HT-1080), and human leukemia (CCRF-CEM) cells. These data indicate that Dox-SH, Dox-SS-Pyr, and Dox-SS-[C(WR)4K] have the potential to be further examined as Dox alternatives and anticancer agents.
European Journal of Medicinal Chemistry published new progress about Antiproliferative agents. 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Safety of 1,2-Di(pyridin-2-yl)disulfane.