2-substituted estradiol bis-sulfamates, multitargeted antitumor agents: synthesis, in vitro SAR, protein crystallography, and in vivo activity
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STX140, but not paclitaxel, inhibits mammary tumour initiation and progression in C3(1)/SV40 T/t-antigen transgenic miceSynthesis and cytotoxic activity of pentacyclic triterpenoid sulfamates.Class III beta-tubulin expression and in vitro resistance to microtubule targeting agents.Synthesis, anti-tubulin and antiproliferative SAR of steroidomimetic dihydroisoquinolinones.Optimisation of tetrahydroisoquinoline-based chimeric microtubule disruptors.Synthesis and biological evaluations of putative metabolically stable analogs of VN/124-1 (TOK-001): head to head anti-tumor efficacy evaluation of VN/124-1 (TOK-001) and abiraterone in LAPC-4 human prostate cancer xenograft model.A 2-methoxyestradiol bis-sulphamoylated derivative induces apoptosis in breast cell linesQuantitative proteomic analysis revealed lovastatin-induced perturbation of cellular pathways in HL-60 cells.Steroidomimetic Tetrahydroisoquinolines for the Design of New Microtubule Disruptors.Targeted NF1 cancer therapeutics with multiple modes of action: small molecule hormone-like agents resembling the natural anticancer metabolite, 2-methoxyoestradiol.The In Vitro and In Vivo Activity of the Microtubule Disruptor STX140 Is Mediated by Hif-1 Alpha and CAIX ExpressionA bis-sulphamoylated estradiol derivative induces ROS-dependent cell cycle abnormalities and subsequent apoptosis.Inclusion complexes of 2-methoxyestradiol with dimethylated and permethylated β-cyclodextrins: models for cyclodextrin-steroid interaction.In vivo inhibition of angiogenesis by sulphamoylated derivatives of 2-methoxyoestradiol.The therapeutic potential of a series of orally bioavailable anti-angiogenic microtubule disruptors as therapy for hormone-independent prostate and breast cancers.The use of steroid sulfatase inhibitors as a novel therapeutic strategy against hormone-dependent endometrial cancer.The in vivo properties of STX243: a potent angiogenesis inhibitor in breast cancer.2-Methoxyoestradiol-3,17-O,O-bis-sulphamate and 2-deoxy-D-glucose in combination: a potential treatment for breast and prostate cancer.Carbonic anhydrase as a model for biophysical and physical-organic studies of proteins and protein-ligand binding.BCRP expression does not result in resistance to STX140 in vivo, despite the increased expression of BCRP in A2780 cells in vitro after long-term STX140 exposure.Molecular crosstalk between apoptosis and autophagy induced by a novel 2-methoxyestradiol analogue in cervical adenocarcinoma cells.Tetrahydroisoquinolinone-based steroidomimetic and chimeric microtubule disruptors.Autophagy induced by a sulphamoylated estrone analogue contributes to its cytotoxic effect on breast cancer cells.Discovery and Development of the Aryl O-Sulfamate Pharmacophore for Oncology and Women's Health.Sulfatase inhibitors: a patent review.Anticancer steroids: linking natural and semi-synthetic compounds.Synthesis, antitubulin, and antiproliferative SAR of C3/C1-substituted tetrahydroisoquinolines.Docking, synthesis, and in vitro evaluation of antimitotic estrone analogs.In vitro effects of an in silico-modelled 17β-estradiol derivative in combination with dichloroacetic acid on MCF-7 and MCF-12A cells.Tubulin inhibitors targeting the colchicine binding site: a perspective of privileged structures.Cloning, expression and purification of the complete domain of the η-carbonic anhydrase from Plasmodium falciparum.The in vitro effects of a novel estradiol analog on cell proliferation and morphology in human epithelial cervical carcinoma.Insights into the binding mode of sulphamates and sulphamides to hCA II: crystallographic studies and binding free energy calculations.Design, Synthesis and Biochemical Evaluation of Novel Selective Estrogen Receptor Ligand Conjugates Incorporating an Endoxifen-Combretastatin Hybrid Scaffold.Modes of cell death induced by tetrahydroisoquinoline-based analogs in MDA-MB-231 breast and A549 lung cancer cell lines.
P2860
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P2860
2-substituted estradiol bis-sulfamates, multitargeted antitumor agents: synthesis, in vitro SAR, protein crystallography, and in vivo activity
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2006 nî lūn-bûn
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2006 թուականի Դեկտեմբերին հրատարակուած գիտական յօդուած
@hyw
2006 թվականի դեկտեմբերին հրատարակված գիտական հոդված
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2006年の論文
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2006年学术文章
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2006年学术文章
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2006年学术文章
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2006年学术文章
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2006年学术文章
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2006年學術文章
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name
2-substituted estradiol bis-su ...... lography, and in vivo activity
@ast
2-substituted estradiol bis-su ...... lography, and in vivo activity
@en
2-substituted estradiol bis-su ...... lography, and in vivo activity
@nl
type
label
2-substituted estradiol bis-su ...... lography, and in vivo activity
@ast
2-substituted estradiol bis-su ...... lography, and in vivo activity
@en
2-substituted estradiol bis-su ...... lography, and in vivo activity
@nl
prefLabel
2-substituted estradiol bis-su ...... lography, and in vivo activity
@ast
2-substituted estradiol bis-su ...... lography, and in vivo activity
@en
2-substituted estradiol bis-su ...... lography, and in vivo activity
@nl
P2093
P50
P356
P1476
2-substituted estradiol bis-su ...... lography, and in vivo activity
@en
P2093
Andrew Smith
Atul Purohit
Barry V L Potter
Mathew P Leese
Michael J Reed
Simon P Newman
P304
P356
10.1021/JM060705X
P407
P577
2006-12-28T00:00:00Z