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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 22, Number 9
BKCSDE 22(9)
September 20, 2001 

Synthesis and Antitumor Activity of New Anthracycline Analogues
Young S. Rho, Wan-Joong Kim, Dong Jin Yoo, Heun Soo Kang, Soon-Ryang Chung
Daunomycin, Doxorubicin, Anthracycline derivatives, N-Benzoyl-(2R,3S)-phenylisoserine, LPyroglutamic acid.
New anthracycline analogues 2-9 as potential anticancer agents have been synthesized from daunomycin (1a) and doxorubicin (1b). Compounds 2 and 6 were prepared by the nucleophilic displacement type esterification of 14-bromodaunomycin (1c) with N-benzoyl-(2R,3S)-phenylisoserine and L-pyroglutamic acid in triethyl-amine, respectively. Compounds 3, 7 and 4, 8 were prepared by the reaction of either daunomycin (1a) or doxorubicin (1b) with one equivalent of the corresponding acids in the presence of EDCI/PP. Compounds 5, 9 were obtained from 1b by reaction with 2.2 equivalents of the corresponding acids in the same manner. The cytotoxic activities of the analogues in comparison with adrimycin on cultured SNU-16 and MCF7 cell were described.
963 - 968
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