TY - JOUR
T1 - A two-step synthesis of medicinally-important 1,8-naphthalimide peptidyls by solid phase organic synthesis
AU - Brider, Tamara
AU - Gellerman, Gary
PY - 2012/10/17
Y1 - 2012/10/17
N2 - A new approach for a short synthesis of novel medicinally-important mono-, bis- and tris-1,8-naphthalimide peptidyl derivatives is described. The method generates efficiently 1,8-naphthalimides 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 1,8-naphthalimide anticancer candidates.
AB - A new approach for a short synthesis of novel medicinally-important mono-, bis- and tris-1,8-naphthalimide peptidyl derivatives is described. The method generates efficiently 1,8-naphthalimides 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 1,8-naphthalimide anticancer candidates.
KW - 1,8-Naphthalimide peptidyls
KW - Bi- and tri-nuclei intercalators
KW - Fmoc chemistry
KW - Solid-phase organic synthesis (SPOS)
UR - http://www.scopus.com/inward/record.url?scp=84866232948&partnerID=8YFLogxK
U2 - 10.1016/j.tetlet.2012.08.007
DO - 10.1016/j.tetlet.2012.08.007
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AN - SCOPUS:84866232948
SN - 0040-4039
VL - 53
SP - 5611
EP - 5615
JO - Tetrahedron Letters
JF - Tetrahedron Letters
IS - 42
ER -