Abstract: Disclosed is a method of making conjugates of cell binding agents and small molecule drugs comprising reacting a cell binding agent with a bifunctional cross-linking moiety to thereby provide the cell binding agent with a reactive disulfide group and then reacting the modified cell binding agent with a small molecule drug comprising a free thiol group. Bifunctional cross-linking moieties are also disclosed.

Abstract: The present invention relates to compounds according to the structure (I): Where R is —CH3 or —CH2CH2Cl; R? is C1-C7 alkyl or —CH2CH2Cl; R2 or R4 is OPO3H2, NO2, OCO(Glu-OH), NHCO(Glu-OH), NHR7 and unassigned groups of R2, R3, R4, R5 and R6 are, independently H, F, Cl, Br, I, OH, OPO3H2, OCH3, CF3, OCF3, NO2, CN, SO2CH3, SO2CF3, COCH3, COOCH3, SCH3, SF5, NH2, NHR7, N(CH3)2, OPO3H2, or a C1-C7 alkyl group with the proviso that when any two of unassigned groups of R2, R3, R4, R5 or R6 are other than H, the other two of unassigned groups of R2, R3, R4, R5 or R6 are H. R7 is H or polyglutamyl as described. Phosphoric acid and glutamic acid can be a free acid or pharmaceutically acceptable salt thereof.

Abstract: The present invention refers to distamycin and derivatives thereof, such as bromo- or chloro-acryloyl derivatives of distamycin, which are conjugated with glutathione, to a process for their preparation and to pharmaceutical compositions thereof. The compounds of the invention are endowed with a remarkable antitumor activity and are thus useful in therapy in the treatment of cancer.

Abstract: A substituted apicidin derivative, a method of synthesis therefore, and an anti-tumor composition comprising the same are disclosed. The substituent of the derivative is preferably semicarbazone, thiosemicarbazone, hydrazone, tert-butylhydrazone, phenylhydrazone, 2,4-dinitrophenylhydrazone, 4-methoxyphenylhydrazone, 3-methoxyphenylhydrazone, 4-nitrophenylhydrazone, benzylhydrazone, methanesulfonylhydrazone, benzenesulfonylhydrazone, 4-methylbenzenesulfonylhydrazone, benzoylhydrazone, 4-nitrobenzoylhydrazone, carbohydrazone, benzyloxime or acetoxime. The compound has strong inhibition effect against histone deacetylase and detransforming activities and specifically inhibit growth of cancer cells. Therefore, it is useful in preparation of an anti-tumor composition.

Abstract: The present invention concerns compounds of the formula: ##STR1## wherein R is a lower alkyl group, an aryl group or an alkylaryl group and X and Y are the same or different, and each is OH, NH.sub.2, or SH. The aryl group or the aryl moiety of the alkylaryl group may be unsubstituted, monosubstituted, disubstituted or trisubstituted. If substituted, each substituent may independently be an alkyl group, an alkyloxy group or a halogen.The present invention also provides methods for synthesizing the compounds described above.