6214-60-4Relevant academic research and scientific papers
5-FLUOROURACIL DERIVATIVES, PREPARATION METHODS AND USES THEREOF
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Paragraph 0121, (2021/07/30)
Disclosed is a 5-fluorouracil derivative having the molecular structure shown in general formula VI, in which Ra and Rb groups are an alkoxy group or a fluorine-substituted alkoxy group having 1, 2, 3, or 4 carbon atoms, and are mono-, bis-, tri-, tetra- or penta-substituted on a phenyl group; a linking group L1 is an alkyl or alkenyl group having 1, 2, 3, or 4 carbon atoms, a linking group L2 is oxygen, or an alkyl or alkoxy group having 1, 2, 3, or 4 carbon atoms, or an amino acid, or an alkyl group having 1, 2, 3, or 4 carbon atoms containing an amino moiety, or a furyl group, and an X group is O or —NH—. Further disclosed is a method for preparing such a derivative and a use of the same in the treatment of cancer, tumor diseases, and diseases caused by abnormal neovascularization in a human or non-human mammal, and a medicament or a composition containing the 5-fluorouracil derivative.
Preparation and application for 5-fluorouracil substituted carboxylic acid derivative
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Paragraph 0066; 0067; 0070; 0071, (2018/03/26)
The invention discloses a preparation and an application for a compound compounded from stilbene and diphenylethane antitumor drugs and 5-fluorouracil antitumor drugs. The compound provided by the invention has a general structural formula (I) as describe
TARGETED THERAPEUTICS
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Paragraph 00644, (2015/03/28)
The present invention provides pharmacological compounds including an effector moiety conjugated to a binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.
TARGETED THERAPEUTICS
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Paragraph 00598; 00600, (2015/09/28)
The present invention provides pharmacological compounds including an effector moiety conjugated to a binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.
TARGETED THERAPEUTICS
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Paragraph 00941; 00943, (2016/01/30)
The present invention provides pharmacological compounds including an effector moiety conjugated to a binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.
PHARMACEUTICAL COMPOSITION COMPRISING MODIFIED HEMOGLOBIN-BASED THERAPEUTIC AGENT FOR CANCER TARGETING TREATMENT AND DIAGNOSTIC IMAGING
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Paragraph 0022; 0094, (2014/11/27)
The present invention provides a pharmaceutical composition containing hemoglobin-based therapeutic agent for treating cancer. The hemoglobin moiety can target cancer cells and the therapeutic moiety (i.e. active agent/therapeutic drug) can kill the cance
TARGETED THERAPEUTICS
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Paragraph 00591; 00593, (2013/11/05)
The present invention provides pharmacological compounds including an effector moiety conjugated to a binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.
Design, synthesis and biological activity of 5-fluorouracil-distamycin hybrids
Baraldi,Romagnoli,Martinez,Pineda de las Infantas,Gallo,Espinosa,Rutigliano,Bianchi,Gambari
, p. 390 - 403 (2007/10/03)
The design, synthesis, and the evaluation of the cytotoxic activity of a novel group of hybrids, namely a molecular combination of the natural antibiotic agent distamycin A and the antimetabolite 5-fluorouracil is reported and structure-activity relationships are discussed. This homologous series 7a-f consisted of the oligopeptides distamycin A joined to 5-fluorouracil by aliphatic carboxylic acid moieties containing a polymethylene chain [(CH2)n, where n=1 up to 6). In vitro antitumor activity of this new class of derivatives was appreciable for compounds with at least two methylenes (compounds 7b-f). For these compounds the in vitro antitumor activity was not influenced by the length of the -[CH2]n linker, being comparable to that of the parent compound distamycin A. Arrested polymerase-chain experiments demonstrated selective binding of the 5-fluorouracil-distamycin hybrids to A+T rich DNA sequences.
