- HUMAN TOPOISOMERASE II-TARGETING ORGANOPLATINUM COMPOUNDS
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Some organoplatinum compounds have been synthesized. These organoplatinum compounds are designed to be human Topoisomerase II-targeting drugs.
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- ORGANOPLATINUM COMPOUNDS AND PHARMACEUTICAL COMPOSITION THEREOF AND METHOD OF PREPARING CRYSTAL OF hTop2
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Some organoplatinum compounds have been synthesized. These organoplatinum compounds are designed to be human Topoisomerase II-targeting drugs.
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- Novel "reverse Kahne-type glycosylation": Access to O-, N-, and C-linked epipodophyllotoxin conjugates
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Exposure of epipodophyllotoxin C4-sulfoxides to triflic anhydride, followed by a silyl glycoside, provides a glycoconjugate of the etoposide variety via formal "reverse Kahne glycosylation." To our knowledge, this is the first example of this variant of the Kahne activation method wherein the activating functionality is positioned on the aglycon, rather than on the sugar. Phenols, anilines, or allyl silanes are also efficiently captured at C4, producing the corresponding O-, N-, and C-linked lignan conjugates.
- Berkowitz, David B.,Choi, Sungjo,Bhuniya, Debnath,Shoemaker, Richard K.
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p. 1149 - 1152
(2007/10/03)
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- Antitumor Agents. 3. Synthesis and Biological Activity of 4β-Alkyl Derivatives Containing Hydroxy, Amino, and Amido Groups of 4'-O-Demethyl-4-desoxypodophyllotoxin as Antitumor Agents
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A series of 4β-alkyl (7-10), 4β-aminoalkyl (12a-y), and 4β-amidoalkyl derivatives (14a-g) of 4'-O-demethyl-4-desoxypodophyllotoxin have been synthesized, and their cytotoxicity, inhibition of DNA topoisomerase II (Topo II), and tubulin polymerization were evaluated.All derivatives of 12a-y and 14a-g did not inhibit tubulin polymerization.Many compounds exhibited cytotoxicity and inhibition of Topo II.In particular, 12o, 12s, 12t, and 12u strongly inhibited Topo II (IC5050 (μM) 32.5, 60.9, 58.8, and 33.6, respectively) and were strong cytotoxicity against P388 cells (IC50 (M) 1.0, 4.1, 3.3, and 3.0 x 1E-9, respectively), compared with VP-16 (IC50 (μM) 59.2, IC50 (M) 1 x 1E-8, respectively).These compounds were nearly equal to or superior to VP-16 in antitumor activity in vivo (L1210, P388, and Lewis lung) and were more cytotoxic against various human cell lines in vitro than V-16.
- Terada, Tadafumi,Fujimoto, Katsuhiko,Nomura, Makoto,Yamashita, Jun-ichi,Wierzba, Konstanty,et al.
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p. 1689 - 1699
(2007/10/02)
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- Antitumor agents. II: Regio- and stereospecific syntheses of 1-β-alkyl-1-desoxypodophyllotoxin derivatives and biological activity
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1-β-Alkyl derivatives of 1-desoxypodophyllotoxin were synthesized, and their cytotoxicity and inhibitory effects on DNA topoisomerase II (Topo-II) and tubulin polymerization were examined. The reaction of epipodophyllotoxin derivatives (1a-c) with trimeth
- Terada,Fujimoto,Nomura,Yamashita,Wierzba,Kobunai,Takeda,Minami,Yoshida,Yamaguchi,Yamada
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p. 907 - 912
(2007/10/02)
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