TY - JOUR
T1 - A fast entry to the novel medicinally-important 9-anilinoacridine peptidyls by solid phase organic synthesis (SPOS)
AU - Brider, Tamara
AU - Gilad, Yossi
AU - Gellerman, Gary
PY - 2011/7/13
Y1 - 2011/7/13
N2 - A new approach to the synthesis of novel medicinally-important mono- and bis-9-anilinoacridine (9-AnA) peptidyl derivatives is described. The method generates efficiently 9-AnAs with variable spacer lengths and charged, polar or hydrophobic residues at desired positions, which can increase binding affinity, conformational stability, intracellular transport and/or biological activity. The synthetic routes reported in this work are both general and applicable, and significantly expand the scope of potential 9-aminoacridine (9-AA) anticancer candidates.
AB - A new approach to the synthesis of novel medicinally-important mono- and bis-9-anilinoacridine (9-AnA) peptidyl derivatives is described. The method generates efficiently 9-AnAs with variable spacer lengths and charged, polar or hydrophobic residues at desired positions, which can increase binding affinity, conformational stability, intracellular transport and/or biological activity. The synthetic routes reported in this work are both general and applicable, and significantly expand the scope of potential 9-aminoacridine (9-AA) anticancer candidates.
KW - 9-Aminoacridine (9-AA)
KW - 9-Anilinoacridine (9-AnA)
KW - Nucleophilic substitution
KW - Peptidyl derivative
KW - Solid phase organic synthesis
UR - http://www.scopus.com/inward/record.url?scp=79958280695&partnerID=8YFLogxK
U2 - 10.1016/j.tetlet.2011.05.023
DO - 10.1016/j.tetlet.2011.05.023
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AN - SCOPUS:79958280695
SN - 0040-4039
VL - 52
SP - 3640
EP - 3644
JO - Tetrahedron Letters
JF - Tetrahedron Letters
IS - 28
ER -