3396-01-8Relevant academic research and scientific papers
IRAK DEGRADERS AND USES THEREOF
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Paragraph 00607-00608; 00604, (2021/06/22)
The present invention provides compounds, compositions thereof, and methods of using the same.
COVALENT TARGETING OF E3 LIGASES
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Paragraph 0591; 0650, (2020/05/19)
Disclosed herein, inter alia, are compositions and methods for targeting E3 ligases. In an aspect is a targeted protein degrader including 1) a targeted protein binder and 2) an E3 Ubiquitin ligase binder, wherein the E3 Ubiquitin ligase is human RNF4 or human RNF114. In an aspect is provided a pharmaceutical composition including a compound as described herein, including embodiments, and a pharmaceutically acceptable excipient.
In silico molecular docking, synthesis of 4-(4-benzoylaminophenoxy) phenol derivatives as androgen receptor antagonists
Elancheran, Ramakrishnan,Kabilan, Senthamaraikannan,Kotoky, Jibon,Ramanathan, Muthiah,Bhattacharjee, Atanu
, p. 307 - 316 (2019/09/12)
Aim and Objective: To study the structural difference, optimization, molecular docking and development of new benzoyl amino phenoxy phenol derivatives as anti-prostate cancer agents. Materials and Methods: Strategies towards the identification of novel be
Design and synthesis of 4-(4-benzoylaminophenoxy)phenol derivatives as androgen receptor antagonists
Yamada, Ayumi,Fujii, Shinya,Mori, Shuichi,Kagechika, Hiroyuki
supporting information, p. 937 - 941 (2013/10/22)
We report the design and synthesis of novel 4-(4-benzoylaminophenoxy)phenol derivatives that bind to the androgen receptor (AR) ligand-binding domain and exhibit potent androgen-antagonistic activity. Compound 22 is one of the most potent of these derivatives, inhibiting the dihydrotestosterone-promoted growth of SC-3 cell line bearing wild-type AR (IC50 0.75 μM), LNCaP cell line bearing T877A-mutated AR (IC50 0.043 μM), and 22Rv1 cell line bearing H874Y-mutated AR (IC50 0.22 μM). Structure-activity relationship studies confirmed that the pharmacophore of these novel AR antagonists is distinct from the nitro- or cyano-substituted anilide substructure of other nonsteroidal AR antagonists. This novel pharmacophore is expected to provide a basis for designing new antiprostate cancer agents.
Design, synthesis and antitumor activity of novel cis-furoquinoline derivatives
Li, Jie,Pei, Shuchen,Zhu, Yingxi,Wu, Jianbo,Chen, Yin,Zhang, Weiyu,Wu, Yong
, p. 379 - 388 (2012/07/03)
A series of novel cis-furoquinoline derivatives was synthesized and tested for their antitumor activities in vitro against HepG2 cells, Lu-04 cells and Leu02 cells to evaluate structure-activity relationships. Assay-based antiproliferative activity study revealed that several compounds had significant effects on cytotoxicity, among which compounds 2f, 2l, 2q were found to be the most active compounds. Above all, compounds 2f, 2l, 2q would be potential anticancer agents which deserved further research.
PHOSPHATE ESTER COMPOUND, METAL SALT THEREOF, DENTAL MATERIAL, AND DENTAL COMPOSITION
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, (2009/06/27)
The invention provides a phosphate compound having an unsaturated double bond and a metal salt thereof; a dental material containing a phosphate compound having an unsaturated double bond and/or a metal salt thereof; and a dental composition containing a
Rho-kinase inhibitors
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Page/Page column 12, (2008/06/13)
Disclosed are compounds and derivatives thereof, their synthesis, and their use as Rho-kinase inhibitors. These compounds are useful for inhibiting tumor growth, treating erectile dysfunction, and treating other indications mediated by Rho-kinase, e.g., c
Correspondence between Molecular Functionality and Crystal Structures. Supramolecular Chemistry of a Family of Homologated Aminophenols
Vangala, Venu R.,Bhogala, Balakrishna R.,Dey, Archan,Desiraju, Gautam R.,Broder, Charlotte K.,Smith, Philip S.,Mondal, Raju,Howard, Judith A. K.,Wilson, Chick C.
, p. 14495 - 14509 (2007/10/03)
The crystal structures and packing features of a family of 13 aminophenols, or supraminols, are analyzed and correlated. These compounds are divided into three groups: (a) compounds 1-5 with methylene spacers of the general type HO-C6H4-(CH2)n- C6H 4-NH2 (n = 1 to 5) and both OH and NH2 in a para position; (b) compounds la, 2a, 2b, 2c, and 3a in which one or more of the methylene linkers in 1 to 3 are exchanged with an S-atom; and (c) compounds 2d, 1b, and 6a prepared with considerations of crystal engineering and where the crystal structures may be anticipated on the basis of structures 1-5, 1a, 2a, 2b, 2c, and 3a. These 13 aminols can be described in terms of three major supramolecular synthons based on hydrogen bonding between OH and NH2 groups: the tetrameric loop or square motif, the infinite N(H)O chain, and β-As sheet. These three synthons are not completely independent of each other but interrelate, with the structures tending toward the more stable β-As sheet in some cases. Compounds 1-5 show an alternation in melting points, and compounds with n = even exhibit systematically higher melting points compared to those with n = odd. The alternating melting points are reflected in, and explained by, the alternation in the crystal structures. The n = odd structures tend toward the β-As sheet as n increases and can be considered as a variable series whereas for n = even, the β-As sheet is invariably formed constituting a fixed series. Substitution of a methylene group by an isosteric S-atom may causes a change in the crystal structure. These observations are rationalized in terms of geometrical and chemical effects of the functional groups. This study shows that even for compounds with complex crystal structures the packing may be reasonably anticipated provided a sufficient number of examples are available.
1-[(hydroxyphenoxy)phenylene]triazenes, polymers crosslinked therewith, and methods therefor
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, (2008/06/13)
Compounds of the structure STR1 where --R' is --F, --CF3, --CN, or --Cl; each --R , which may be the same or different, is independently selected from the group consisting of C1 -C6 alkyl or hydroxyalkyl moieties and aryl moieties; and n is 0 or 1. Such compounds are useful as derivatizing and crosslinking agents for polymers, especially fluorinated poly(arylene ethers).
