6500-65-8Relevant academic research and scientific papers
ACYL HYDRAZONE LINKERS, METHODS AND USES THEREOF
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Paragraph 00239, (2019/07/04)
The present application is directed to compounds of Formula (I)-(VI): (I), (II), (III), (IV), (V) (VI), (VII) and (VIII), compositions comprising these compounds and their uses, for example as medicaments and/or diagnostics.
A 2 - methoxy - 6, 7, 8, 9 - tetrahydrobenz cyclohepta - 5 - ketone (by machine translation)
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Paragraph 0048; 0055; 0056, (2018/03/24)
The invention discloses a method for synthesizing 2 - methoxy - 6, 7, 8, 9 - tetrahydrobenz cyclohepta - 5 - one method, its steps are: halogen anisole with glutaric anhydride reaction for the preparation of 5 - (3 - methoxyphenyl) - 5 - oxo-valeric acid, reducing 5 - (3 - methoxyphenyl) - 5 - oxo-valeric acid for the preparation of 5 - (3 - methoxyphenyl) pentanoic acid; 5 - (3 - methoxyphenyl) pentanoic acid through the intramolecular Friedel-crafts acylation reaction to obtain 2 - methoxy - 6, 7, 8, 9 - tetrahydrobenz cyclohepta - 5 - one. The method of the invention the synthesis step is short, low cost, the total yield is high, can be used for industrial production. (by machine translation)
Structural interrogation of benzosuberene-based inhibitors of tubulin polymerization
Herdman, Christine A.,Devkota, Laxman,Lin, Chen-Ming,Niu, Haichan,Strecker, Tracy E.,Lopez, Ramona,Liu, Li,George, Clinton S.,Tanpure, Rajendra P.,Hamel, Ernest,Chaplin, David J.,Mason, Ralph P.,Trawick, Mary Lynn,Pinney, Kevin G.
, p. 7497 - 7520 (2015/12/18)
The discovery of 3-methoxy-9-(3′,4′,5′-trimethoxyphenyl)-6,7-dihydro-5H-benzo[7]annulen-4-ol (a benzosuberene-based analogue referred to as KGP18) was originally inspired by the natural products colchicine and combretastatin A-4 (CA4). The relative struct
A photo-favorskii ring contraction reaction: The effect of ring size
Kammath, Viju Balachandran,?olomek, Tomá?,Ngoy, Bokolombe Pitchou,Heger, Dominik,Klán, Petr,Rubina, Marina,Givens, Richard S.
, p. 1718 - 1729 (2013/03/29)
The effect of ring size on the photo-Favorskii induced ring-contraction reaction of the hydroxybenzocycloalkanonyl acetate and mesylate esters (7a-d, 8a-c) has provided new insight into the mechanism of the rearrangement. By monotonically decreasing the ring size in these cyclic derivatives, the increasing ring strain imposed on the formation of the elusive bicyclic spirocyclopropanone 20 results in a divergence away from rearrangement and toward solvolysis. Cycloalkanones of seven or eight carbons undergo a highly efficient photo-Favorskii rearrangement with ring contraction paralleling the photochemistry of p-hydroxyphenacyl esters. In contrast, the five-carbon ring does not rearrange but is diverted to the photosolvolysis channel avoiding the increased strain energy that would accompany the formation of the spirobicyclic ketone, the "Favorskii intermediate 20". The six-carbon analogue demonstrates the bifurcation in reaction channels, yielding a solvent-sensitive mixture of both. Employing a combination of time-resolved absorption measurements, quantum yield determinations, isotopic labeling, and solvent variation studies coupled with theoretical treatment, a more comprehensive mechanistic description of the rearrangement has emerged.
The total synthesis of hypodematine
Kang, Zhi-Yun,Zhang, Qing-Jian,Chen, Ruo-Yun,Zhang, Pei-Cheng,Yu, De-Quan
, p. 840 - 848 (2013/09/23)
Hypodematine, isolated from Hypodematium sinense Iwatsuki as an alkaloid with a new skeleton, was synthesized via nine reaction steps, in which the synthesis of 2-aryl-1-benzazocines via Beckmann rearrangement of 5H-benzocyclohepten-5-one oxime mesylate i
FUSED TETRACYCLE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
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Page/Page column 115-116, (2012/05/04)
The present invention relates to novel Fused Tetracycle Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, A', B, G, R1, U, V, W, W', X, X', Y and Y' are as defined herein. The present invention also relates to compositions comprising at least one Fused Tetracycle Derivative, and methods of using the Fused Tetracycle Derivatives for treating or preventing HCV infection in a patient.
Efficient Method for Preparing Functionalized Benzosuberenes
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Page/Page column 16, (2012/06/01)
The disclosed process can efficiently synthesize functionalized benzosuberenes. The process provides an improved method of production of benzosuberene and compounds containing a benzosuberene moiety, which is characterized by a ring closing methodology comprising reaction of a 5-phenylpentanoic acid with Eaton's reagent to form the benzosuberone. The process, optionally, further includes steps for adding a functional group at the ketone position.
An amino-benzosuberene analogue that inhibits tubulin assembly and demonstrates remarkable cytotoxicity
Tanpure, Rajendra P.,George, Clinton S.,Sriram, Madhavi,Strecker, Tracy E.,Tidmore, Justin K.,Hamel, Ernest,Charlton-Sevcik, Amanda K.,Chaplin, David J.,Trawick, Mary Lynn,Pinney, Kevin G.
supporting information, p. 720 - 724 (2013/11/06)
The recent discovery of a small-molecule benzosuberene-based phenol that demonstrates remarkable picomolar cytotoxicity against selected human cancer cell lines and strongly inhibits tubulin polymerization (1-2 μM) inspired the design and synthesis of a variety of new, structurally diverse benzosuberene derivatives. An efficient synthetic route to functionalized benzosuberenes was developed. This methodology utilized a Wittig reaction, followed by a selective alkene reduction and ring-closing cyclization to form the core benzosuberone structure. This synthetic route facilitated the preparation of a 4-nitro-1-(3′,4′,5′-trimethoxyphenyl) benzosuberene derivative and its corresponding 4-amino analogue in good yield. The 4-amino analogue was a strong inhibitor of tubulin polymerization (1.2 μM), demonstrated enhanced cytotoxicity against the human cancer cell lines examined (GI50 = 33 pM against SK-OV-3 ovarian cancer, for example), and exhibited a concentration dependent disruption of a pre-established capillary-like network of tubules formed from human umbilical vein endothelial cells.
Combretastatin analogs with tubulin binding activity
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Page/Page column 25, (2008/06/13)
Analogs of combretastatin have been discovered which demonstrate impressive cytotoxicity as well as a remarkable ability to inhibit tubulin polymerization. Such compounds are excellent clinical candidates for the treatment of cancer in humans. In addition, certain of these ligands, as pro-drugs, may well prove to be tumor selective vascular targeting chemotherapeutic agents or to have vascular targeting activity resulting in the selective prevention and/or destruction of nonmalignant proliferating vasculature.
Uracil compounds as P2-purinoreceptor 7-transmembrane G-protein coupled receptor antagonists
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, (2008/06/13)
Compounds of formula I or salts thereof where for example Y is a group of the formula (i) and R1is a group of formula (ii) are provided along with compositions containing them and processes for their preparation. The compounds are P2-purinoreceptor 7-transmembrane G-protein coupled receptor antagonists, and are useful in the treatment of inflammatory conditions.
