Synthesis and bioactivity of a Goralatide analog with antileukemic activity
Natural tetrapeptide Goralatide (AcSDKP) is a selective inhibitor of primitive haematopoietic cell proliferation. It is not stable in vivo and decomposes within 4.5 min when applied to live cells. In this work we developed an analog of Goralatide that exhibits cytotoxicity towards human myeloid HL-60, HEL, Nalm-6 leukemia cells, endothelial HUVEC, glioblastoma U251 and transformed kidney 293T cells. The Goralatide analog showed significant stability in organic solution with no tendency to degrade oxidatively.
Li, Zhiliang,Lebedyeva, Iryna O.,Golubovskaya, Vita M.,Cance, William G.,Alamry, Khalid A.,Faidallah, Hassan M.,Dennis Hall,Katritzky, Alan R.
p. 5056 - 5060
(2015/08/03)
Synthesis of l-lys-aminoxy-goralatide
Natural tetrapeptide Goralatide inhibits primitive hematopoietic cell proliferation but reported to be rather unstable in solution (half-life 4.5 min). In this work, we report the synthesis of an aminoxy analog of Goralatide. Aminoxy moiety is expected to
Li, Zhiliang,Lebedyeva, Iryna,Zhao, Deqian,Myers, Lauren,Pillai, Girinath G.,Hall, Charles Dennis,Katritzky, Alan R.
p. 923 - 927
(2015/02/05)
Synthesis of L-Lys-Aminoxy-Goralatide
Natural tetrapeptide Goralatide inhibits primitive hematopoietic cell proliferation but reported to be rather unstable in solution (half-life 4.5min). In this work, we report the synthesis of an aminoxy analog of Goralatide. Aminoxy moiety is expected to
Li, Zhiliang,Lebedyeva, Iryna,Zhao, Deqian,Myers, Lauren,Pillai, Girinath G.,Hall, Charles Dennis,Katritzky, Alan R.
p. 923 - 927
(2015/08/25)
Synthesis and anticonvulsant activities of N-benzyl (2R)-2-acetamido-3-oxysubstituted propionamide derivatives
Lacosamide has been submitted for regulatory approval in the United States and Europe for the treatment of epilepsy. Previous synthetic methods did not permit the elaboration of the structure-activity relationship (SAR) for the 3-oxy site in lacosamide. We report an expedient five-step stereospecific synthesis for N-benzyl (2R)-2-acetamido-3-oxysubstituted propionamide analogs beginning with d-serine methyl ester. The procedure incorporated alkyl (e.g. methyl, primary, secondary, and tertiary) and aryl groups at this position. The SAR for the 3-oxy site showed maximal activity in animal seizure models for small 3-alkoxy substituents.
Morieux, Pierre,Stables, James P.,Kohn, Harold
experimental part
p. 8968 - 8975
(2009/04/06)
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