Synthesis and biological evaluation of new camptothecin derivatives obtained by modification of position 20

Riva, Elena; Comi, D.; Borrelli, Stella; Colombo, Francesco; Danieli, Bruno; Borlak, Jürgen; Evensen, Lasse; Lorens, James B.; Fontana, Gabriele; Gia, Ornella; Via, Lisa Dalla; Passarella, Daniele

doi:10.1016/j.bmc.2010.09.069

Cited by 26 publications

(19 citation statements)

References 44 publications

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“…Compound 11 (10 mg, 0.009 mmol) was dissolved in DCM, and compound 12 [12] (6 mg, 0.0117 mmol) and a catalytic amount of DMAP were added. The reaction mixture stirred for 6 h and monitored by RP-HPLC (gradient of 10% to 90% ACN in water, 20 min).…”

Section: Compound 13mentioning

confidence: 99%

Modular theranostic prodrug based on a FRET-activated self-immolative linker

Redy

Shabat

2012

Journal of Controlled Release

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Section: Compound 13mentioning

confidence: 99%

Modular theranostic prodrug based on a FRET-activated self-immolative linker

Redy

Shabat

2012

Journal of Controlled Release

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“…Thus, dimeric and trimeric compounds, which exhibited a strongly pronounced antitumor effect, have been synthesized based on artemizinine. 6 Meanwhile, symmetric compounds containing two quaternary nitrogen atoms separated by different size spacers are generally known to exhibit high biological activity. 2 The strategy of bivalent ligands has been successfully implemented for searching for acetylcholinesterase inhibitors.…”

Section: Introductionmentioning

confidence: 99%

New quaternary ammonium camphor derivatives and their antiviral activity, genotoxic effects and cytotoxicity

Соколова

Yarovaya

Shernyukov

et al. 2013

Bioorganic & Medicinal Chemistry

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The synthesis and biological evaluation of a novel series of dimeric camphor derivatives are described. The resulting compounds were studied for their antiviral activity, cyto- and genotoxicity. Compounds 3a and 3d in which the quaternary nitrogen atoms are separated by the C5H10 and С9H18 aliphatic chain, exhibited the highest efficiency as an agent inhibiting the reproduction of the influenza virus A(H1N1)pdm09. The cytotoxicity data of compounds 3 and 4 revealed their moderate activity against malignant cell lines; compound 3f had the highest activity for the CEM-13 cells. These results show close agreement with the data of independent studies on toxicity of these compounds, in particular that the toxicity of compounds strongly depends on spacer length.

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“…Thus, nucleophilic addition gave the compounds 46-48 (Scheme 2). The structure of these compounds were confirmed by their 1 (28)(29)(30)(31)(32)(33)(34)(35)(36)(37)(38)(39)(40)(41)(42)(43)(44)(45). IC 50 is the concentration at which the enzyme activity is inhibited by 50% and is calculated from Graph Prism software.…”

Section: Chemistrymentioning

confidence: 68%