Synthesis and biological activity of new arenediyne-linked isoxazolidines.
Arenediyne-isoxazolidine conjugates have been synthesized as a new scaffold for the development of bioactive mimics. Some of the synthesized compounds are endowed with antiproliferative activity against three human cancer cell lines. Their thermal reactivity suggests that the biological activity probably could not be linked to the Bergman cyclization.
Dipartimento di Scienze del farmaco e dei prodotti per la salute, University of Messina, Via SS Annunziata, 98168 Messina, Italy. Electronic address: robromeo@unime.it.
Roberto
R
Romeo
Dipartimento di Scienze del farmaco e dei prodotti per la salute, University of Messina, Via SS Annunziata, 98168 Messina, Italy.
Michele
M
Navarra
Dipartimento di Scienze del farmaco e dei prodotti per la salute, University of Messina, Via SS Annunziata, 98168 Messina, Italy. Electronic address: sgiofre@unime.it.
Salvatore V
SV
Giofrè
Dipartimento di Scienze del farmaco e dei prodotti per la salute, University of Messina, Via SS Annunziata, 98168 Messina, Italy.
Caterina
C
Carnovale
Dipartimento di Scienze del farmaco e dei prodotti per la salute, University of Messina, Via SS Annunziata, 98168 Messina, Italy.
Santa
S
Cirmi
Dipartimento di Scienze del Farmaco, University of Catania, Viale Andrea Doria 6, 95125 Catania, Italy.
Giuseppe
G
Lanza
Dipartimento di Scienze del Farmaco, University of Catania, Viale Andrea Doria 6, 95125 Catania, Italy.
Maria A
MA
Chiacchio
D000480:Alkynes / Q000737:chemistry*; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D019073:HT29 Cells; D056945:Hep G2 Cells; D006801:Humans; D007555:Isoxazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D000480:Alkynes; D000970:Antineoplastic Agents; D007555:Isoxazoles
1,3-Dipolar cycloaddition; Antitumor agents; Arenediyne–isoxazolidine conjugates; SH-SY5Y, HT-29, HepG2 cell lines; Sonogashira reaction