Abstract
For almost 5 decades later since it was first discovered in 1958, efforts continue to be made in the medicinal chemistry of camptothecin (CPT) and its derivatives. Thousands of CPT analogues have been prepared. However, many of the earlier CPT derivatives were either too toxic for clinical use or had very poor pharmacokinetics. Efforts in the last 2 decades were most successful and two derivatives, Irinotecan and topotecan, have been clinically approved by the FDA. This review mainly summarizes the design and synthesis of camptothecin drugs in various stages of preclinical or clinical developments.
Keywords: Camptothecin, analog, synthesis, topoisomerase I, chemical modification, anticancer agent
Current Pharmaceutical Design
Title: Design, Synthesis and Development of Novel Camptothecin Drugs
Volume: 14 Issue: 11
Author(s): Siong Tern Liew and Li-Xi Yang
Affiliation:
Keywords: Camptothecin, analog, synthesis, topoisomerase I, chemical modification, anticancer agent
Abstract: For almost 5 decades later since it was first discovered in 1958, efforts continue to be made in the medicinal chemistry of camptothecin (CPT) and its derivatives. Thousands of CPT analogues have been prepared. However, many of the earlier CPT derivatives were either too toxic for clinical use or had very poor pharmacokinetics. Efforts in the last 2 decades were most successful and two derivatives, Irinotecan and topotecan, have been clinically approved by the FDA. This review mainly summarizes the design and synthesis of camptothecin drugs in various stages of preclinical or clinical developments.
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Cite this article as:
Liew Tern Siong and Yang Li-Xi, Design, Synthesis and Development of Novel Camptothecin Drugs, Current Pharmaceutical Design 2008; 14 (11) . https://dx.doi.org/10.2174/138161208784246180
DOI https://dx.doi.org/10.2174/138161208784246180 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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