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Clinical pharmacology of camptothecins

Cancer Chemotherapy and Pharmacology, 1998
Camptothecins (CPTs) are a unique class of chemotherapeutic agent which inhibit DNA synthesis by inhibiting topoisomerase I activity. Structure-activity studies on the original CPT alkaloid led to the development of the new analogues irinotecan (CPT-11), topotecan, and 9-aminocamptothecin, which have improved water solubility and lower toxicity.
L, Iyer, M J, Ratain
openaire   +2 more sources

Camptothecin induced DDX5 degradation increased the camptothecin resistance of osteosarcoma

Experimental Cell Research, 2020
Osteosarcoma (OS) is the most common primary malignant bone tumor in children and adolescents. Unfortunately, chemo-resistance is a huge obstacle in the treatment of OS. However, the underlying molecular mechanisms of OS chemo-resistance still remain unknown.
Xingkai, Zhao   +3 more
openaire   +2 more sources

Camptothecins in clinical development

Expert Opinion on Investigational Drugs, 2004
Following 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
openaire   +2 more sources

Pharmacology of Camptothecin Esters

Annals of the New York Academy of Sciences, 2000
Abstract: 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
openaire   +2 more sources

Covalently crosslinked organophosphorous derivatives‐chitosan hydrogel as a drug delivery system for oral administration of camptothecin

European journal of pharmaceutics and biopharmaceutics, 2019
Graphical abstract Figure. No Caption available. ABSTRACT Hydrogels are widely studied as drug delivery system. In this work we propose the employment of tetrakis(hydroxymethyl)phosphonium chloride as crosslinking agent to obtain covalent hydrogels based
Mayte Martínez-Martínez   +5 more
semanticscholar   +1 more source

Total Synthesis of (+)‐Camptothecin.

ChemInform, 2002
A 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
openaire   +1 more source

Synthesis of an immunoconjugate of camptothecin

Bioorganic & Medicinal Chemistry Letters, 2002
The 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
openaire   +2 more sources

Clinical applications of the camptothecins

Biochimica et Biophysica Acta (BBA) - Gene Structure and Expression, 1998
The camptothecin topoisomerase I-targeting agents are new class of antitumor drugs with demonstrated clinical activity in human malignancies, such as colorectal cancer and ovarian cancer. Currently, irinotecan and topotecan are the most widely used camptothecin analogs in clinical use and clinical trials are ongoing to better characterize their spectra
C H, Takimoto, J, Wright, S G, Arbuck
openaire   +2 more sources

Fungicidal activities of camptothecin semisynthetic derivatives against Colletotrichum gloeosporioides in vitro and in mango fruit

Postharvest Biology and Technology, 2019
Increasing attention to the resistance of plant pathogenic fungi to fungicides and their residues impels the development of more efficient fungicides with novel mechanisms of action.
Gang Feng   +11 more
semanticscholar   +1 more source

Possible clues for camptothecin biosynthesis from the metabolites in camptothecin-producing plants.

Fitoterapia, 2019
The plant derived camptothecin (CPT) is a pentacyclic pyrroloquinoline alkaloid with unique antitumor activity. Successive discoveries of new CPT-producing plants occurred in recent years due to market demands.
Xiang Pu   +6 more
semanticscholar   +1 more source

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