Results 141 to 150 of about 23,580 (195)
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Total Synthesis of (+)‐Camptothecin.
ChemInform, 2002A total synthesis of (+)-camptothecin is described. The approach is based on a room temperature LUMOdiene-controlled Diels–Alder cycloaddition of the electron deficient N-sulfonyl-1-aza-1,3-butadiene 6 with the electron rich dienophile 1,1,3,3-tetraethoxypropene (7) for assembly of a pyridine precursor to the D-ring pyridone. The 20(S) tertiary alcohol
Brian S.J. Blagg, Dale L. Boger
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Camptothecins in clinical development
Expert Opinion on Investigational Drugs, 2004Following the realisation that DNA topoisomerase I is a useful therapeutic target to be exploited for the design of potential inhibitors, topoisomerase I inhibitors now represent an established class of effective agents. In spite of intense efforts in the field, only camptothecins have a clinical relevance.
Franco, Zunino, Graziella, Pratesi
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Pharmacology of Camptothecin Esters
Annals of the New York Academy of Sciences, 2000Abstract: An intact lactone ring of camptothecins is a structural requirement for their anticancer activity. Propionate esters of camptothecin (CPT) and 9‐nitrocamptothecin (9NC), CZ48 and CZ112, respectively, have been synthesized as derivatives resistant to lactone hydrolysis and are chemotherapeutically active.
J G, Liehr +4 more
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Synthesis of an immunoconjugate of camptothecin
Bioorganic & Medicinal Chemistry Letters, 2002The first immunoconjugate of camptothecin has been synthesized wherein the drug is attached to the tumor-recognizing antibody BR96 via a Cathepsin B cleavable linker. Endocytosis of the immunoconjugate upon binding to the tumor cell followed by enzymatic cleavage of the linker inside the endosome ensures tumor-specific release of the drug. In this way,
Michael A, Walker +4 more
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Liposomal delivery of camptothecins
Pharmaceutical Science & Technology Today, 2000The use of liposomal drug delivery systems to improve the therapeutic index of pharmaceutical agents is exemplified by camptothecin-based drugs. This highly active class of anticancer agents possesses a unique mechanism of action with some inherent shortcomings, which might have been solved by liposomal formulation.
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