TY - JOUR
T1 - Novel cytotoxic 7-iminomethyl and 7-aminomethyl derivatives of camptothecin
AU - Dallavalle, Sabrina
AU - Ferrari, Anna
AU - Merlini, Lucio
AU - Penco, Sergio
AU - Carenini, Nives
AU - De Cesare, Michelandrea
AU - Perego, Paola
AU - Pratesi, Graziella
AU - Zunino, Franco
PY - 2001/2/12
Y1 - 2001/2/12
N2 - A series of new 7-iminomethyl derivatives of camptothecin were obtained from camptothecin-7-aldehyde and aromatic alicyclic and aliphatic amines. Their hydrogenation led to the corresponding amines. All the imines and the less polar amines showed a marked increase of the cytotoxic activity against H460 non-small lung carcinoma cell line, with respect to topotecan. The lipophilicity of the substituent in position 7 of camptothecin seems to play an important role for cytotoxic potency. The 7-phenyliminomethyl derivative showed efficacy comparable to topotecan in vivo against NSCLC H460 xenografted in athymic nude mice.
AB - A series of new 7-iminomethyl derivatives of camptothecin were obtained from camptothecin-7-aldehyde and aromatic alicyclic and aliphatic amines. Their hydrogenation led to the corresponding amines. All the imines and the less polar amines showed a marked increase of the cytotoxic activity against H460 non-small lung carcinoma cell line, with respect to topotecan. The lipophilicity of the substituent in position 7 of camptothecin seems to play an important role for cytotoxic potency. The 7-phenyliminomethyl derivative showed efficacy comparable to topotecan in vivo against NSCLC H460 xenografted in athymic nude mice.
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U2 - 10.1016/S0960-894X(00)00649-1
DO - 10.1016/S0960-894X(00)00649-1
M3 - Article
C2 - 11212094
AN - SCOPUS:0035847695
SN - 0960-894X
VL - 11
SP - 291
EP - 294
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 3
ER -