New Analogues of Camptothecins: Activity and Resistance

Boven, Epie; Hattum, Annemarie H. Van; Hoogsteen, Ilse J.; Schlüper, Hennie M.M.; Pinedo, H.M.

doi:10.1111/j.1749-6632.2000.tb07035.x

Cited by 18 publications

(4 citation statements)

References 4 publications

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“…Certainly, several researchers have reported that CPT inhibits a cellular enzyme DNA topoisomerase I and induces apoptosis in various cancer cells. [18][19] CPT is a planar pentacyclic quinoline that includes 3 rings of pyrrolo-(3,4-β)-quinoline part (A, B, and C rings), an unsaturated pyridone moiety in ring D and a α-hydroxy lactone ring (E ring), containing one chiral center with (S)-configuration ( Fig. 1) [20][21].…”

Section: Introductionmentioning

confidence: 99%

Safe approaches for camptothecin delivery: Structural analogues and nanomedicines

Botella

Rivero-Buceta

2017

Journal of Controlled Release

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Twenty-(S)-camptothecin is a strongly cytotoxic molecule with excellent antitumor activity over a wide spectrum of human cancers. However, the direct formulation is limited by its poor water solubility, low plasmatic stability and severe toxicity, which currently limits its clinical use. As a consequence, two strategies have been developed in order to achieve safe and efficient delivery of camptothecin to target cells: structural analogues and nanomedicines. In this review, we summarize recent advances in the design, synthesis and development of camptothecin molecular derivatives and supramolecular vehicles, following a systematic classification according to structure-activity relationships (structural analogues) or chemical nature (nanomedicines). A series of organic, inorganic and hybrid materials are presented as nanoplatforms to overcome camptothecin restrictions in administration, biodistribution, pharmacokinetics and toxicity. Nanocarriers which respond to a variety of stimuli endogenously (e.g., pH, redox potential, enzyme activity) or exogenously (e.g., magnetic field, light, temperature, ultrasound) seem the best positioned therapeutic materials for optimal spatial and temporal control over drug release. The main goal of this review is to be used as a source of relevant literature for others interested in the field of camptothecin-based therapeutics. To this end, final remarks on the most important formulations currently under clinical trial are provided.

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Section: Introductionmentioning

confidence: 99%

Safe approaches for camptothecin delivery: Structural analogues and nanomedicines

Botella

Rivero-Buceta

2017

Journal of Controlled Release

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“…As of now, clinical tests are carried out only for compounds 7j and 15a and these results have been given partially consideration in reviews . Below results of investigation of these compounds, in vitro and in vivo discusses.…”

Section: Biological Activity Of Si‐containing Camptothecins and Clinimentioning

confidence: 99%

Silicon‐containing analogs of camptothecin as anticancer agents

Lazareva

Baryshok

Lazarev

2017

Archiv der Pharmazie

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“…Alternatively, the design of bioactive organosilanes can be an intellectual exercise in which a silicon atom is strategically introduced to modify an organic compound of known biological activity or one that plays a role in a biological process 8. Karenitecin11 ( 3 ) is a derivative of the natural product camphothecin, carrying a lipophilic trimethylsilylethyl group on the pyridine ring 12. Promising phase II clinical trials of this silane have recently been completed 13.…”

Section: Introductionmentioning

confidence: 99%

Silanediol Protease Inhibitors: From Conception to Validation

2006

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Keywords: Drug design / Hydrolases / Inhibitors / Peptidomimetics / Proteases / Silanes / Silicon Silanediols are isosteric with the unstable hydrated carbonyl group, but are most commonly associated with polymerization to give silicone polymers. Placement of a silanediol in a dipeptide analogue yields a new kind of nonhydrolyzable transition-state-analogue protease inhibitor. Both metallo and aspartic protease inhibitors have been prepared using silanediols, with enzyme inhibition in the low nanomolar range. Structure-activity comparisons with known inhibitors,

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New Analogues of Camptothecins: Activity and Resistance

Cited by 18 publications

References 4 publications

Safe approaches for camptothecin delivery: Structural analogues and nanomedicines

Safe approaches for camptothecin delivery: Structural analogues and nanomedicines

Silicon‐containing analogs of camptothecin as anticancer agents

Silanediol Protease Inhibitors: From Conception to Validation

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