TY - JOUR
T1 - Synthesis of pyrrolidine 3,4-diol derivatives with anticancer activity on pancreatic tumor cells
AU - Steimer, Frederic
AU - Carmona, Ana T.
AU - Moreno-Vargas, Antonio J.
AU - Caffa, Irene
AU - Cea, Michele
AU - Montecucco, Fabrizio
AU - Nencioni, Alessio
AU - Vogel, Pierre
AU - Robina, Inmaculada
PY - 2014
Y1 - 2014
N2 - Novel pyrrolidine 3,4-diol derivatives of the type (2R and 2S,3R,4S)-{[((1R)-1-methoxycarbonyl and hydroxylmethyl)-1-arylmethyl)amino]ethyl}-pyrrolidine-3,4-diol have been prepared and evaluated as α-mannosidase inhibitors and assayed for their anticancer activity in vitro. They all exhibit specific but moderate activity as inhibitors towards α-mannosidase from Jack beans. Compounds 7 and 8b bearing hydroxymethyl and trifluoromethylbiphenyl groups show the best antiproliferative effect in two pancreatic cancer cell lines.
AB - Novel pyrrolidine 3,4-diol derivatives of the type (2R and 2S,3R,4S)-{[((1R)-1-methoxycarbonyl and hydroxylmethyl)-1-arylmethyl)amino]ethyl}-pyrrolidine-3,4-diol have been prepared and evaluated as α-mannosidase inhibitors and assayed for their anticancer activity in vitro. They all exhibit specific but moderate activity as inhibitors towards α-mannosidase from Jack beans. Compounds 7 and 8b bearing hydroxymethyl and trifluoromethylbiphenyl groups show the best antiproliferative effect in two pancreatic cancer cell lines.
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U2 - 10.3987/COM-13-S(S)111
DO - 10.3987/COM-13-S(S)111
M3 - Article
AN - SCOPUS:84986537158
SN - 0385-5414
VL - 8
SP - 1445
EP - 1464
JO - Heterocycles
JF - Heterocycles
IS - 2
ER -