A two-step synthesis of medicinally-important 1,8-naphthalimide peptidyls by solid phase organic synthesis |
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Authors: | Tamara Brider Gary Gellerman |
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Institution: | Department of Biological Chemistry, Ariel University Center of Samaria, PO Box 3, Ariel 40700, Israel |
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Abstract: | 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. |
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Keywords: | Solid-phase organic synthesis (SPOS) 1 8-Naphthalimide peptidyls Bi- and tri-nuclei intercalators Fmoc chemistry |
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