Combretastatin A-4
Determinants of anti-vascular action by combretastatin A-4 phosphate: role of nitric oxide
... agent combretastatin A-4 phosphate (CA-4-P) has been quantified in two types of murine tumour, the breast adenocarcinoma CaNT and the round cell sarcoma ...
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Synthesis and biological evaluation of Combretastatin A-4 derivatives containing a 3’-O-substituted carbonic ether moiety as potential antitumor agents
... several structure–activity relationships (SARs) have been identified for CA-4, which are summarized in Figure 2. These SARs have demonstrated that the 3,4,5-trimethoxy- substituted A-ring and the cis configuration ...
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“Combretastatin A-4 and its Analogs in Cancer Therapy” by Sonia Arora, Andres F. Gonzalez, Khushbu Solanki, United States of America.
... chemistries. Combretastatin A-4 (CA-4) and combretastatin A-1 (CA-1) have been the most prominent leads for therapeutic applications of the combretastatin A ...
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Original Article Therapeutic effect of hepatocellular carcinoma-targeting liposome delivery system loaded with c[RGDyk] modified combretastatin A-4 and adriamycin: a pharmacodynamics study
... control. Combretastatin A-4 (CA-4, Sigma, USA) and adriamycin (DOX, Sigma, USA) were detected using HPLC method and UV spectrophotome- ter at 480 nm, ...
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Anti-vascular agent Combretastatin A-4-P modulates Hypoxia Inducible Factor-1 and gene expression
... Combretastatin A-4 was originally isolated from the South African bush willow Combretum caffrum. The phos- phate derivative, CA-4-P, was subsequently synthesised as the more soluble prodrug [7]. The ...
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Synthesis and evaluation of azetidinone analogues of combretastatin A 4 as tubulin targeting agents
... 3, 4 and vinblastine 5 and those that inhibit the disassembly of the mitotic spindle once it has formed, such as paclitaxel 6 ...as combretastatin A-4 (2a, figure 1) 7 and podophyllotoxin (4, ...
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Time resolved nanosecond fluorescence lifetime imaging and picosecond infrared spectroscopy of combretastatin A 4 in solution and in cellular systems
... of combretastatin A-4 within the focal volume of two-photon excitation The ultimate objective of this project is to use 2-photon activation of a low activity E-combretastatin to the active Z-isomer ...
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An in vivo role for Rho kinase activation in the tumour vascular disrupting activity of combretastatin A-4 3-O-phosphate
... Colchicine-related microtubule depolymerizing agents are the largest family of low MW drugs to have tumour vascular disrupting activity at relatively non-toxic doses (Tozer et al., 2005; Kanthou and Tozer, 2007; Siemann, ...
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An in vivo role for Rho kinase activation in the tumour vascular disrupting activity of combretastatin A-4 3-O-phosphate
... Colchicine-related microtubule depolymerizing agents are the largest family of low MW drugs to have tumour vascular disrupting activity at relatively non-toxic doses (Tozer et al., 2005; Kanthou and Tozer, 2007; Siemann, ...
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Evaluation of Sydnone-Based Analogs of Combretastatin A-4 Phosphate (CA4P) as Vascular Disrupting Agents for Use in Cancer Therapy
... The lower toxicity of CA4P relative to colchicine is thought to be due to the differences in the reversibility of binding to tubulin. 39 Colchicine is thought to bind strongly and irreversibly, whereas CA4P appears to ...
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Vascular disrupting agent for neovascular age related macular degeneration: a pilot study of the safety and efficacy of intravenous combretastatin a-4 phosphate
... CA4P has been shown to disrupt tumor neovasculature and decrease tumor blood flow in both animals and humans [3]. Multiple human studies have demonstrated significant decrease in tumor blood flow within a few hours of ...
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Synthesis and anticancer activities of polymethylenedioxy analogues of combretastatin A-2
... example, combretastatin A-2 (CA-2) and combretastatin A-4 (CA-4) from Combretum caffrum are among the most potent antimitotic agents that can dis- rupt microtubule ...and 4-methoxy ...
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SYNTHESIS AND BIOLOGICAL EVALUATION OF CYCLOPROPANE DERIVATIVE OF COMBRETASTATIN CA-4-PHOSPHATE
... . Combretastatin A-4 was originally isolated from the South African bush willow Combretum ...CA- 4-P is not yet understood. In-vitro, CA-4-P causes microtubule depolymerization, which leads to ...
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Novel Selective Estrogen Receptor Ligand Conjugates Incorporating Endoxifen Combretastatin and Cyclofenil Combretastatin Hybrid Scaffolds: Synthesis and Biochemical Evaluation
... water-soluble combretastatin A4-phosphate CA-4P (fosbretabulin, Figure 1) was synthesized and is currently under investigation in combination with pazopanib in a Phase 1b and Phase II study for the treatment of ...
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Sydnone Cycloaddition Route to Pyrazole-Based Analogs of Combretastatin A4.
... compound, combretastatin A-4 (CA4), was shown to be effective at causing selective tumor vascular collapse, within minutes, at non-toxic ...disodium combretastatin A-4 3-O- phosphate ...
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Lead identification of conformationally restricted ? lactam type combretastatin analogues: synthesis, antiproliferative activity and tubulin targeting effects
... of combretastatin A-4 are described which contain the 1,4-diaryl-2-azetidinone (β-lactam) ring system in place of the usual ethylene bridge present in the natural combretastatin stilbene ...
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Beta Lactam Estrogen Receptor Antagonists and a Dual Targeting Estrogen Receptor/Tubulin Ligand
... We focused our further efforts on the development of a dual ligand for ER and tubulin. It is known that a trimethoxyaryl ring, found in the natural products colchicine and combretastatin A-4 as well as in ...
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Piperlongumine (piplartine) and analogues: Antiproliferative microtubule destabilising agents
... that combretastatin A-4 (2) and colchicine, established tubulin-destabilising agents, may target the stress response to ROS in MCF-7 breast cancer ...
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Sequential Systemic Administrations of Combretastatin A4 Phosphate and Radioiodinated Hypericin Exert Synergistic Targeted Theranostic Effects with Prolonged Survival on SCID Mice Carrying Bifocal Tumor Xenografts
... An alternative mode of cancer targeting namely a small-molecular sequential dual-targeting therag- nostic strategy (SMSDTTS) has been proposed [3]. In this approach, the tumor vasculature and induced intratumoral ...
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Combretastatin A4 phosphate induces rapid regression of tumor neovessels and growth through interference with vascular endothelial cadherin signaling
... The fluorescence microscopy analysis of VE-cadherin, β-catenin, phospho– β-catenin Ser33/37/Thr41, CD31, ZO-1, occludin, connexin-43, and actin filaments was performed on the FGF-2–stimulated HUVECs in different ...
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