2006
DOI: 10.2174/092986706777585004
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Review Camptothecin: Current Perspectives

Abstract: The review provides a detailed discussion of recent advances in the medicinal chemistry of camptothecin, a potent antitumor agent that targets topoisomerase I. Thousands of CPT derivatives have been synthesized. Two of them, Topotecan and Irinotecan, are commercially approved for use in clinic as antitumor agents while more are still in clinic trials. This review summarizes the current status of the modern synthetic approaches to CPT, the mechanism of action of CPT, the structure-activity relationship(SAR), a … Show more

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Cited by 248 publications
(121 citation statements)
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References 55 publications
(81 reference statements)
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“…The results of our study confirm the findings of previous studies in mouse bone marrow cells for camptothecin [Backer et al, 1990;Holmström and Winters, 1992], topotecan [Aydemir and Bilaloglu, 2003], and irinotecan [Hardman et al, 2002]. Under the conditions described, topotecan was the most genotoxic compound, followed by camptothecin then irinotecan, probably because substitutions of amino groups for the 9-carbon of the camptothecin A ring lead to compounds with greater in vivo activity [Li et al, 2006]. These replacements greatly increase the antitumor activity of topotecan compared with the camptothecin parent molecule, and could be responsible for its higher genetic toxicity in the somatic mouse bone marrow cells.…”
Section: Resultssupporting
confidence: 90%
See 1 more Smart Citation
“…The results of our study confirm the findings of previous studies in mouse bone marrow cells for camptothecin [Backer et al, 1990;Holmström and Winters, 1992], topotecan [Aydemir and Bilaloglu, 2003], and irinotecan [Hardman et al, 2002]. Under the conditions described, topotecan was the most genotoxic compound, followed by camptothecin then irinotecan, probably because substitutions of amino groups for the 9-carbon of the camptothecin A ring lead to compounds with greater in vivo activity [Li et al, 2006]. These replacements greatly increase the antitumor activity of topotecan compared with the camptothecin parent molecule, and could be responsible for its higher genetic toxicity in the somatic mouse bone marrow cells.…”
Section: Resultssupporting
confidence: 90%
“…The antitumor activity of camptothecin is thought to be due to its ability to stabilize the reversible covalent DNAtopoisomerase I complex [Hsiang et al, 1985;Giovanella et al, 1989;Liu et al, 2000;Li et al, 2006;Pommier, 2006;Hartmann and Lipp 2006], preventing the religation step of the breakage/rejoining reaction mediated by the enzyme. The net result is that the drug causes fragmentation of chromosomal DNA, cell death and extensive sister chromatid exchange and chromosomal aberrations [Hsiang et al, 1989;Backer et al, 1990;Holmström and Winters, 1992;Mosesso et al, 2000;Sortibrán et al, 2006;Orta et al, 2008].…”
Section: Introductionmentioning
confidence: 99%
“…An example can be found in camptothecin which is a renowned anti-cancer compound that can be extracted from Nyssaceae arbo (Wen et al, 2005). It is worth mentioning that camptothecin is not a perfect and inexhaustible compound in cancer treatment because of the side-effect on gastrointestinal system and bone marrow, and moderate solubility in aqueous media (Zhu et al, 1978;Kehrer et al, 2001;Li et al, 2006). However, 10-hydroxycamptothecin, which can also be extracted from Nyssaceae arbo exists at a low content of 0.001% but shows higher anti-cancer activity and lower side-effect compared to camptothecin.…”
Section: To Improve Existing Anti-cancer Drugsmentioning
confidence: 99%
“…Interest in camptothecin increased in the 1980s and 90s, after the discovery of its mechanism of action based on inhibition of nuclear enzyme topoisomerase I which is involved in DNA replication [3]. This interest resulted in the synthesis of many analogues, two of which were introduced as a medicine in anticancer therapy (topotecan, irinotecan), while some other are at the stage of clinical trials [4]. Camptothecins exist in two forms: lactone, stable at pH<5.…”
Section: Introductionmentioning
confidence: 99%