TY - JOUR
T1 - Synthesis and biological evaluation of (+)-neopeltolide analogues
T2 - Importance of the oxazole-containing side chain
AU - Fuwa, Haruhiko
AU - Noguchi, Takuma
AU - Kawakami, Masato
AU - Sasaki, Makoto
PY - 2014/6/1
Y1 - 2014/6/1
N2 - We describe the synthesis and biological evaluation of (+)-neopeltolide analogues with structural modifications in the oxazole-containing side chain. Evaluation of the antiproliferative activity of newly synthesized analogues against A549 human lung adenocarcinoma cells and PANC-1 human pancreatic carcinoma cells have shown that the C19-C20 and C26-C27 double bonds within the oxazole-containing side chain and the terminal methyl carbamate group are essential for potent activity.
AB - We describe the synthesis and biological evaluation of (+)-neopeltolide analogues with structural modifications in the oxazole-containing side chain. Evaluation of the antiproliferative activity of newly synthesized analogues against A549 human lung adenocarcinoma cells and PANC-1 human pancreatic carcinoma cells have shown that the C19-C20 and C26-C27 double bonds within the oxazole-containing side chain and the terminal methyl carbamate group are essential for potent activity.
KW - Antiproliferative activity
KW - Macrolides
KW - Marine natural products
KW - Structure-activity relationships
KW - Suzuki-Miyaura coupling
UR - http://www.scopus.com/inward/record.url?scp=84899975405&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84899975405&partnerID=8YFLogxK
U2 - 10.1016/j.bmcl.2014.04.031
DO - 10.1016/j.bmcl.2014.04.031
M3 - Article
C2 - 24792465
AN - SCOPUS:84899975405
SN - 0960-894X
VL - 24
SP - 2415
EP - 2419
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 11
ER -