244033-13-4Relevant academic research and scientific papers
Synthesis of Novel G Factor or Chloroquine-Artemisinin Hybrids and Conjugates with Potent Antiplasmodial Activity
Athanassopoulos, Constantinos M.,Baltas, Michel,Grellier, Philippe,Menendez, Christophe,Mouray, Elisabeth,Papaioannou, Dionissios,Pepe, Dionissia A.,Toumpa, Dimitra,André-Barrès, Christiane
supporting information, p. 921 - 927 (2020/07/21)
A series of novel hybrids of artemisinin (ART) with either a phytormone endoperoxide G factor analogue (GMeP) or chloroquine (CQ) and conjugates of the same compounds with the polyamines (PAs), spermidine (Spd), and homospermidine (Hsd) were synthesized and their antiplasmodial activity was evaluated using the CQ-resistant P. falciparum FcB1/Colombia strain. The ART-GMeP hybrid 5 and compounds 9 and 10 which are conjugates of Spd and Hsd with two molecules of ART and one molecule of GMeP, were the most potent with IC50 values of 2.6, 8.4, and 10.6 nM, respectively. The same compounds also presented the highest selectivity indexes against the primary human fibroblast cell line AB943 ranging from 16 372 for the hybrid 5 to 983 for the conjugate 10 of Hsd.
Synthetic studies toward the development of novel minoxidil analogs and conjugates with polyamines
Magoulas, George E.,Bariamis, Stavros E.,Athanassopoulos, Constantinos M.,Papaioannou, Dionissios
supporting information; experimental part, p. 1989 - 1993 (2010/06/21)
Syntheses of novel polyamine-modified minoxidil analogs (PMMs) and minoxidil-polyamine conjugates (MPCs) are described in an effort to improve the biological activity and selectivity of minoxidil and its poor solubility in water.
Simple syntheses of the polyamine alkaloid tenuilobine and analogues using selectively N-tritylated polyamines and dicarboxylic acids as bridging elements
Vassis, Stratos,Govaris, Ioannis,Voyagi, Katerina,Mamos, Petros,Papaioannou, Dionissios
, p. 2597 - 2600 (2007/10/03)
Selectively N-tritylated spermidine and spermine derivatives and the monophenacyl ester of 1,16-hexadecanedioic acid (Hda) were used to obtain the polyamine alkaloid tenuilobine and its fully reduced analogue. Other symmetric or side-chain-shortened tenui
Synthesis of spermidine and norspermidine dimers as high affinity polyamine transport inhibitors
Covassin, Laurence,Desjardins, Michel,Charest-Gaudreault, Rene,Audette, Marie,Bonneau, Marie-Josee,Poulin, Richard
, p. 1709 - 1714 (2007/10/03)
A series of novel spermidine and sym-norspermidine dimers was synthesized by crosslinking the polyamine backbones via alkylation of their secondary amino groups to butyl, trans-2-butenyl, 2-butynyl or pxylyl bridges. The resulting hexamines behaved as high-affinity antagonists of polyamine uptake, with a relative potency that was dependent on the geometry of the linker structure.
