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- W1208452148 abstract "This chapter provides an introduction, describes the Total Synthesis, biogenesis, and medicinal chemistry of camptothecin. Camptotheca acuminata Decne (Nyssaceae) is a tree distributed widely and abundantly in the southern part of China, and the crude alcoholic extract of C. acuminata show antitumor activity in animal tests. Camptothecin has two notable chemical properties: (1) its lack of significant alkalinity causes it to behave as a neutral molecule, and (2) the presence of the C-20 tertiary alcohol imparts an unusual electrophilicity to the lactone carbonyl group, perhaps via a strong intramolecular H bond. All the oxygenated camptothecin analogs showed antitumor activity in animal tests, and may be produced as a result of further metabolism in the plant. The principal effect of camptothecin on cultured mammalian cells is the potent inhibition of polynucleic acid biosynthesis. The drug affects the biosynthesis of ribosomal RNA more than other types of cellular RNA. It does not inhibit significantly protein biosynthesis. Camptothecin induces single-strand breaks in cellular DNA in intact HeLa cells as viewed by alkaline sucrose density gradient analysis; this effect is reversible. At present, camptothecin and 10-hydroxycamptothecin are used clinically only in the People's Republic of China." @default.
- W1208452148 created "2016-06-24" @default.
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- W1208452148 date "1983-01-01" @default.
- W1208452148 modified "2023-10-16" @default.
- W1208452148 title "Chapter 4 Camptothecin" @default.
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- W1208452148 doi "https://doi.org/10.1016/s0099-9598(08)60050-4" @default.
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