- PEPTIDOMIMETIC COMPOUNDS AND ANTIBODY-DRUG CONJUGATES THEREOF
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This invention relates to peptidomimetic linkers and anti-body drug conjugates thereof, to pharmaceutical compositions containing them, and to their use in therapy for the prevention or treatment of cancer.
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Page/Page column 168; 169
(2015/07/07)
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- Design, synthesis, and antitumor activity of 4-halocolchicines and their pro-drugs activated by cathepsin B
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Novel colchicine derivatives possessing various substituents at the C4 position were prepared. Among them, 4-halo derivatives 3-6 were found to exhibit higher activity against cancer cell lines (A549, HT29, HCT116) as well as on mice transplanted with the HCT116 human colorectal carcinoma cell line than colchicine (1). Further, utilizing the 4-substituted colchicines, we prepared pro-drugs having a dipeptide side chain and demonstrated that these pro-drugs were activated by cathepsin B, an enzyme overexpressed in tumor cells, and exhibited selective toxicity to the tumor cells.
- Yasobu, Naoko,Kitajima, Mariko,Kogure, Noriyuki,Shishido, Yoshiyuki,Matsuzaki, Takeshi,Nagaoka, Masato,Takayama, Hiromitsu
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scheme or table
p. 348 - 352
(2011/07/09)
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- PALLADIUM-CATALYZED REACTION OF TRIBUTYLTIN HYDRIDE. SELECTIVE AND VERY MILD DEPROTECTION OF ALLYL AND ALLYLOXYCARBONYL DERIVATIVES OF AMINO-ACIDS.
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Allyl(All) and Allyloxycarbonyl(Alloc) amino-acid derivatives are deprotected through palladium-catalyzed hydrostannolysis by Bu3SnH in a highly selective manner.Benzyl and benzyloxycarbonyl groups are stable under these conditions.Moreover the allyl and Alloc groups seem orthogonal to the t-butyl and t-butoxycarbonyl protecting groups.
- Guibe, F.,Dangles, O.,Balavoine, G.
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p. 2365 - 2368
(2007/10/02)
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