- 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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p. 348 - 352
(2011/07/09)
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- 5,6,7,9-tetrahydro-1,2,3-trimethoxy-9-oxobenzo[alpha]heptalene derivative and pharmaceutical use
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Compounds represented by the formula STR1 wherein R1 and R2 each represent a hydrogen atom or a protective group for a hydroxyl group, or R1 and R2 combine to represent a protective group for hydroxyl groups, and R3 represents CH3 O-- or CH3 NH--. These compounds exhibit a strong effect to inhibit proliferation of cancer cells and are expected to be used as a carcinostatic agent.
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- Semisyntheses, X-Ray Crystal Structures and Tubulin-Binding Properties of 7-Oxodeacetamidocolchicine and 7-Oxodeacetamidoisocolchicine
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Commercially available (-)-colchicine (1) has been converted, via deacetylcolchiceine (4), into a mixture of 7-oxodeacetamidocolchicine (2) and 7-oxodeacetamidoisocolchicine (3).The X-ray structures and tubulin-binding properties of these title ketones are described.
- Banwell, Martin G.,Peters, Steven C.,Greenwood, Richard J.,Mackay, Maureen F.,Hamel, Ernest,Lin, Chii M.
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p. 1577 - 1588
(2007/10/02)
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