37443-73-5Relevant academic research and scientific papers
3,5-Bis(Arylidene)-4-Piperidones Modified by Bisphosphonate Groups as Novel Anticancer Agents
Makarov, Mikhail V.,Rybalkina, Ekaterina Yu.,Brel, Valery K.
, p. 741 - 746 (2015)
Synthetic approaches for conjugating 3,5-bis(arylidene)-4-piperidones with bisphosphonate moiety were elaborated. These approaches are based either on reaction of Grignard reagent containing dioxolane protected 4-piperidone with tetraethyl ethylidenbisphosphonate followed by crotonic condensation with aromatic aldehydes or on Cu(i) catalyzed 1,3-cycloaddition of tetraethyl but-3-yne-1,1-diylbisphosphonate to N-(2-azidoethyl)-3,5-bis(arylidene)-4-piperidones resulting in corresponding 1,2,3-triazole derivatives. Cytotoxic activity of the synthesized conjugates was dependent on the length of linker connecting piperidone nitrogen atom and bisphosphonate residue. Triazole derivatives of 3,5-bis(arylidene)-4-piperidone series displayed moderate in vitro inhibitory properties towards HCT116 and MCF7 human cancer cell lines with IC50 values in the range of 5.0-7.5 M, whereas conjugates with butylene linker between piperidone nitrogen atom and bisphosphonate moiety were significantly less active.
3,5-Bis(arylidene)-4-piperidinones modified with bisphosphonate groups using a 1,2,3-triazole ring: Synthesis and antitumor properties
Makarov,Rybalkina, E. Yu.,Klemenkova,R?schenthaler
, p. 2388 - 2394 (2014)
An approach to the synthesis of new conjugates of 3,5-bis(arylidene)-4-piperidone pharmacophore with bisphosphonate moiety using a 1,2,3-triazole ring as a linker has been developed. The approach is based on a Cu(I)-catalyzed reaction of tetraethyl (but-3
NOVEL THIENOPYRIMIDINE DERIVATIVES OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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Page/Page column 111-112, (2010/11/28)
The present invention relates to a novel thienopyrimidine derivative having an excellent anti? inflammatory and anti-cancer activity, or a pharmaceutically acceptable salt thereof, a process for the preparation thereof and a pharmaceutical composition comprising the same. The compound according to the present invention strongly inhibits IKB kinase-β (IKK-β) involved in the activation of a transcriptional factor, NF-κB, which is associated with inducing various immune and inflammatory diseases, whereby a composition comprising the compound is a useful therapeutic agent against inflammatory diseases, in particular, arthritis and cancer.
Estrogen receptor ligands. Part 8: Dihydrobenzoxathiin SERAMs with heteroatom-substituted side chains
Blizzard, Timothy A.,DiNinno, Frank,Morgan II, Jerry D.,Wu, Jane Y.,Chen, Helen Y.,Kim, Seongkon,Chan, Wanda,Birzin, Elizabeth T.,Yang, Yi Tien,Pai, Lee-Yuh,Zhang, Zhoupeng,Hayes, Edward C.,DaSilva, Carolyn A.,Tang, Wei,Rohrer, Susan P.,Schaeffer, James M.,Hammond, Milton L.
, p. 3865 - 3868 (2007/10/03)
A series of benzoxathiin SERAMs with heteroatom-substituted amine side chains was prepared. Minor modifications in the side chain resulted in significant effects on biological activity, especially in uterine tissue.
