NEW HYDRAZONE DERIVATIVES OF ADRIAMYCIN AND THEIR IMMUNOCONJUGATES - A CORRELATION BETWEEN ACID STABILITY AND CYTOTOXICITY

被引:144
作者
KANEKO, T [1 ]
WILLNER, D [1 ]
MONKOVIC, I [1 ]
KNIPE, JO [1 ]
BRASLAWSKY, GR [1 ]
GREENFIELD, RS [1 ]
VYAS, DM [1 ]
机构
[1] BRISTOL MYERS SQUIBB CO,5 RES PKWY,POB 5100,WALLINGFORD,CT 06492
关键词
D O I
10.1021/bc00009a001
中图分类号
Q5 [生物化学];
学科分类号
071010 ; 081704 ;
摘要
New N-substituted hydrazine linkers were synthesized and their hydrazone derivatives of adriamycin were prepared. These functionalized adriamycin derivatives were conjugated with a monoclonal antibody, 5E9. The release rate of adriamycin from the hydrazones and from some of the conjugates was studied, and their relationship to the IC50's of the conjugate against 5E9-positive Daudi cells was investigated.
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页码:133 / 141
页数:9
相关论文
共 36 条
[11]   IMMUNOLOGICAL STUDIES OF HUMAN TROPHOBLAST - MARKERS, SUBSETS AND FUNCTIONS [J].
FAULK, WP ;
MCINTYRE, JA .
IMMUNOLOGICAL REVIEWS, 1983, 75 :139-175
[12]   STRUCTURE AND REACTIVITY IN CARBONYL REACTIONS - TEMPERATURE COEFFICIENTS OF RATE OF FORMATION OF SEVERAL THIOSEMICARBAZONES [J].
FIARMAN, ID ;
GETTLER, JD .
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1962, 84 (06) :961-&
[13]   ORGANIC DISULFIDES + RELATED SUBSTANCES .8. PREPARATION + OXIDATION OF SOME UNSYMMETRICAL DIALKYL + ALKYL PYRIDINIUM DISULFIDES [J].
FIELD, L ;
FERRETTI, A ;
HARLE, H ;
OWEN, TC .
JOURNAL OF ORGANIC CHEMISTRY, 1964, 29 (06) :1632-&
[14]  
GREENFIELD RS, 1990, CANCER RES, V50, P6600
[15]  
GREENFIELD RS, 1989, ANTIBODY IMMUNOCONJ, V2, P201
[16]  
HAYNES BF, 1981, J IMMUNOL, V127, P347
[17]  
HERMENTIN P, 1988, BEHRING I MITT, V82, P197
[18]  
HURWITZ E, 1975, CANCER RES, V35, P1175
[19]   EFFECT INVIVO OF CHEMOTHERAPEUTIC DRUG - ANTIBODY CONJUGATES IN 2 MURINE EXPERIMENTAL TUMOR SYSTEMS [J].
HURWITZ, E ;
MARON, R ;
BERNSTEIN, A ;
WILCHEK, M ;
SELA, M ;
ARNON, R .
INTERNATIONAL JOURNAL OF CANCER, 1978, 21 (06) :747-755
[20]  
KAKEMI K, 1968, CHEM PHARM BULL, V16, P1481