120330-27-0Relevant articles and documents
Antiproliferative Activity of Polyether Antibiotic - Cinchona Alkaloid Conjugates Obtained via Click Chemistry
Skiera, Iwona,Antoszczak, Micha?,Trynda, Justyna,Wietrzyk, Joanna,Boratyński, Przemys?aw,Kacprzak, Karol,Huczyński, Adam
, p. 911 - 917 (2015)
A series of eight new conjugates of salinomycin or monensin and Cinchona alkaloids were obtained by the Cu(I)-catalysed 1,3-dipolar Huisgen cycloaddition (click chemistry) of respective N-propargyl amides of salinomycin or monensin with four different Cinchona alkaloid derived azides. In vitro antiproliferative activity of these conjugates evaluated against three cancer cell lines (LoVo, LoVo/DX, HepG2) showed that four of the compounds exhibited high antiproliferative activity (IC50 below 3.00 μm) and appeared to be less toxic and more selective against normal cells than two standard anticancer drugs.
Synthesis, anticancer and antibacterial activity of salinomycin N-benzyl amides
Antoszczak, Michal,Augustynowicz-Kope, Ewa,Brzezinski, Bogumil,Huczyski, Adam,Maj, Ewa,Wietrzyk, Joanna,Napirkowska, Agnieszka,Stefaska, Joanna,Janczak, Jan
, p. 19435 - 19459 (2014)
A series of 12 novel monosubstituted N-benzyl amides of salinomycin (SAL) was synthesized for the first time and characterized by NMR and FT-IR spectroscopic methods. Molecular structures of three salinomycin derivatives in the solid state were determined using single crystal X-ray method. All compounds obtained were screened for their antiproliferative activity against various human cancer cell lines as well as against the most problematic bacteria strains such as methicillin-resistant Staphylococcus aureus (MRSA) and Staphylococcus epidermidis (MRSE), and Mycobacterium tuberculosis. Novel salinomycin derivatives exhibited potent anticancer activity against drug-resistant cell lines. Additionally, two N-benzyl amides of salinomycin revealed interesting antibacterial activity. The most active were N-benzyl amides of SAL substituted at-ortho position and the least anticancer active derivatives were those substituted at the-para position.
Synthesis and antimicrobial activity of amide derivatives of polyether antibiotic - Salinomycin
Huczynski, Adam,Janczak, Jan,Stefanska, Joanna,Antoszczak, Michal,Brzezinski, Bogumil
experimental part, p. 4697 - 4702 (2012/08/13)
For the first time a direct and practical approach to the synthesis of eight amide derivatives of polyether antibiotic - salinomycin is described. The structure of allyl amide (3a) has been determined using X-ray diffraction. Salinomycin and its amide der
