WebCamptothecin is a cytotoxic plant alkaloid originally isolated from C. acuminate that inhibits DNA and RNA synthesis in mammalian cells and is an effective anti-tumor agent (1). Research studies indicate that camptothecin inhibits topoisomerase I with an IC 50 of 679 nM (2). Camptothecin binds and stabilizes topoisomerase I–DNA cleavage ... WebIn vitro experiments in various cell lines have suggested that exatecan may be 6 and 28 times more active than SN-38 (7-ethyl-10-hydroxycamptothecin, the active metabolite of irinotecan) and topotecan respectively. Furthermore, it has a 2–10 times higher therapeutic index than irinotecan and topotecan.
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WebApr 10, 2024 · The compound camptothecin showed hydrogen bond interaction with A:TYR73, A:ASN69, and A:SER60, while hydrophobic interaction with A: ... could bind to the interface of the DNA-topoisomerase I complex of M. oryzae and affect the translation and carbohydrate metabolism/energy metabolism leading to cell death [59]. WebSep 11, 2007 · Camptothecin is an alkaloid isolated from the stem wood of the Chinese tree, Camptotheca acuminata. This compound selectively inhibits the nuclear enzyme DNA topoisomerase, type I. Several semisynthetic analogs of camptothecin have demonstrated antitumor activity. Type Small Molecule Groups Experimental Structure Similar … WebThe discovery of the natural product camptothecin in the early 1960s provided the lead structure for a novel, highly promising class of antitumor agents. Significant progress involving the understanding of the mechanism of action, the drug metabolism, chemistry driven analoging programs and clinical research fnr dose and schedule optimization ... city breaks in vienna