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Search for "antiproliferative" in Full Text gives 109 result(s) in Beilstein Journal of Organic Chemistry.
Chemical modification allows phallotoxins and amatoxins to be used as tools in cell biology
Beilstein J. Org. Chem. 2012, 8, 2072–2084, doi:10.3762/bjoc.8.233
- incubation time (Table 1). Phalloidin displayed no antiproliferative activity up to a concentration of 10−3 M in the culture medium. In contrast, the most lipophilic ester derivative, phalloidin oleate (1e), showed an IC50 value of proliferation inhibition of 2.5 × 10−6 M, and was thus ca. 1000 times more
- , were highly toxic for mouse fibroblasts, and their antiproliferative activity was comparable to the most lipophilic derivative, phalloidin oleate (Figure 4a). Their toxicity was found to be dependent on the configuration of the polymer, since phalloidin bound to D-configurated polylysine was about 10
Reactions of nitroxides XIII: Synthesis of the Morita–Baylis–Hillman adducts bearing a nitroxyl moiety using 4-acryloyloxy-2,2,6,6-tetramethylpiperidine-1-oxyl as a starting compound, and DABCO and quinuclidine as catalysts
Beilstein J. Org. Chem. 2012, 8, 1515–1522, doi:10.3762/bjoc.8.171
- ones [21][22][23][24]. Some recent results concerning MBH reaction have been presented [6][16][18][25][26][27][28][29][30][31][32][33]. MBH adducts themselves are reported to be antiproliferative agents [34]; however, they are often applied as a tool for building more complex target structures, usually
Unprecedented deoxygenation at C-7 of the ansamitocin core during mutasynthetic biotransformations
Beilstein J. Org. Chem. 2012, 8, 861–869, doi:10.3762/bjoc.8.96
- mutants and mutasynthetic approaches. We suggest that the formation of these derivatives is based on elimination at C-7/C-8 followed by reduction(s) of the intermediate enone. In bioactivity tests, only ansamitocin derivatives bearing an ester side chain at C-3 showed strong antiproliferative activity
- -proansamitocin 8 (3.5 mg/L) and two diastereomeric byproducts 9a and 9b (7.6 mg/L; 1:1 ratio) from the fermentation broth of A. pretiosum Δasm12/21 (Figure 1). We also showed that none of these proansamitocin derivatives exhibit antiproliferative activity. Herein, we describe the unprecedented formation of
- )ansamitocin derivatives lacking the ester side chain at C-3 (11b, 11g–h, 12–16) do not show any antiproliferative activity (IC50 > 800 nM) for at least two of the cell lines listed in Table 1. Compounds 11c–e, bearing the ester side chain at C-3, predominantly showed activities in the pM range. As seen also
Marilones A–C, phthalides from the sponge-derived fungus Stachylidium sp.
Beilstein J. Org. Chem. 2011, 7, 1636–1642, doi:10.3762/bjoc.7.192
- activity towards three cancer cell lines (NCI-H460, MCF7 and SF268). Marilone A and C (1, 3) showed weak antiproliferative activity with an average GI50 of 36.7 and 26.6 µM, respectively (see Supporting Information File 1). Marilone B (2) was assayed in a panel of 44 psychoactive receptors, including 11
Natural product biosyntheses in cyanobacteria: A treasure trove of unique enzymes
Beilstein J. Org. Chem. 2011, 7, 1622–1635, doi:10.3762/bjoc.7.191
- majuscula strain found in Curacao, and it exhibits potent antiproliferative and cytotoxic activities [44]. This intriguing structure contains a thiazoline and a cyclopropyl ring. Interestingly, the pathway comprises a HMG-CoA synthase cassette, highly similar to the one of the jamaicamide assembly line
Efficient syntheses of 25,26-dihydrodictyostatin and 25,26-dihydro-6-epi-dictyostatin, two potent new microtubule-stabilizing agents
Beilstein J. Org. Chem. 2011, 7, 1372–1378, doi:10.3762/bjoc.7.161
- , PA 15260, USA Department of Pharmaceutical Sciences, School of Pharmacy, 3501 Terrace Street, University of Pittsburgh, Pittsburgh, PA 15261 USA 10.3762/bjoc.7.161 Abstract The dictyostatins are powerful microtubule-stabilizing agents that have shown antiproliferative activity against a variety of
- microtubule-stabilizing agents include taxanes, epothilones, and discodermolides, among others [3][4]. Dictyostatin (1a) is an exceptionally potent microtubule-stabilizing agent that has shown antiproliferative activity in a variety of human cancer cell lines in the low nanomolar range. Isolated first in 1994
Symmetrical and unsymmetrical α,ω-nucleobase amide-conjugated systems
Beilstein J. Org. Chem. 2010, 6, No. 34, doi:10.3762/bjoc.6.34
- against it within the group tested. Very recently, Accetta et al. reported remarkable symmetrical amide-conjugated bis-α,ω-uracil based systems (IV). These compounds exhibited antiproliferative and erythroid differentiation induction properties towards human chronic myelogenous leukaemia K562 cells [3
Microwave assisted synthesis of triazoloquinazolinones and benzimidazoquinazolinones
Beilstein J. Org. Chem. 2007, 3, No. 11, doi:10.1186/1860-5397-3-11
- ] anticancer, [5] anti-inflammatory, [6] anticonvulsant, [7] and antiproliferative activities as well as inhibitory effects for thymidylate synthase and poly-(ADP-ribose) polymerase (PARP). [8] An interesting method for quinazoline synthesis involved [5+1] annulation during the reaction of β-dicarbonyl
Colchitaxel, a coupled compound made from microtubule inhibitors colchicine and paclitaxel
Beilstein J. Org. Chem. 2006, 2, No. 13, doi:10.1186/1860-5397-2-13
- combination had antagonistic effects. Other researchers found that the antiproliferative effect of paclitaxel was relatively little affected by the presence of microtubule depolymerizing agent, N-acetylcolchinol [50]. Workers who studied cells cultured in vitro found high IC50 levels, in the 10–50 nM range
- , for antiproliferative activity of paclitaxel and vinorelbine individually, but synergy with concentrations as low as 3 nM and 0.01 nM respectively [51]. Thus, differing model systems yielded results variously suggesting antagonistic, non-additive, or synergistic effects. However, there is evidence
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