18920-70-2Relevant academic research and scientific papers
Liquid-Phase Total Synthesis of Plecanatide Aided by Diphenylphosphinyloxyl Diphenyl Ketone (DDK) Derivatives
Chang, Ninghui,Chao, Jie,Li, Haidi,Li, Jun,Qin, Chuanguang,Tian, Guang,Zhang, Zixin
supporting information, p. 3323 - 3328 (2020/04/20)
Plecanatide is an oral guanylate cyclase-C agonist for the treatment of gastrointestinal disorders. The large-scale supply of plecanatide is restrained primarily by its industrial manufacture. Herein we developed diphenylphosphinyloxyl diphenyl ketone (DD
Inducing apoptosis through upregulation of p53: structure–activity exploration of anthraquinone analogs
Agbowuro, Ayodeji A.,Anifowose, Abiodun,Lu, Wen,Tan, Chalet,Tripathi, Ravi,Wang, Binghe,Yang, Xiaoxiao
, p. 1199 - 1210 (2020/06/17)
We previously reported a series of p53-elevating anthraquinone compounds with considerable cytotoxicity for acute lymphoblastic leukemia (ALL) cells. To further develop this class of compounds, we examined the effect of a few key structural features on the anticancer structure–activity relationship (SAR) in ALL cells. The active analogs showed comparable cytotoxicity and upregulation of p53 but did not induce significant downregulation of MDM2 as seen with the lead compound AQ-101, indicating the importance of the anthraquinone core scaffold for MDM2 regulation. The result from the current study not only contributes to the SAR framework of these anthraquinone derivatives but also opens up new chemical space for further optimization work.
INDENE DERIVATIVES USEFUL IN TREATING PAIN AND INFLAMMATION
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Page/Page column 130, (2019/10/29)
Compounds of formula (I): wherein,R1, R2, R3, R4a, R4b and R5 are described herein, or a stereoisomer, enantiomer or tautomer thereof or mixtures thereof, or a pharmaceutically acceptable s
PHOTOACTIVATABLE FOULING-RESISTANT COPOLYMERS
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Paragraph 00155, (2017/03/14)
A photoactivatable fouling-resistant copolymer composed of a photoactivatable monomer and a hydrophilic monomer is disclosed. The photoactivatable monomer includes an aryl ketone derivative having one or more polar groups or alkyl groups.
Design and synthesis of norendoxifen analogues with dual aromatase inhibitory and estrogen receptor modulatory activities
Lv, Wei,Liu, Jinzhong,Skaar, Todd C.,Flockhart, David A.,Cushman, Mark
, p. 2623 - 2648 (2015/04/14)
Both selective estrogen receptor modulators and aromatase inhibitors are widely used for the treatment of breast cancer. Compounds with both aromatase inhibitory and estrogen receptor modulatory activities could have special advantages for treatment of br
Radiosynthesis and evaluation of an 18F-labeled positron emission tomography (PET) radioligand for brain histamine subtype-3 receptors based on a nonimidazole 2-aminoethylbenzofuran chemotype
Bao, Xiaofeng,Lu, Shuiyu,Liow, Jeih-San,Zoghbi, Sami S.,Jenko, Kimberly J.,Clark, David T.,Gladding, Robert L.,Innis, Robert B.,Pike, Victor W.
experimental part, p. 2406 - 2415 (2012/06/01)
A known chemotype of H3 receptor ligand was explored for development of a radioligand for imaging brain histamine subtype 3 (H 3) receptors in vivo with positron emission tomography (PET), namely nonimidazole 2-aminoethylbenzofurans,
Synthesis and characterization of fluorinated polyimides derived from novel unsymmetrical diamines
Yang, Fengchun,Li, Yanfeng,Ma, Tao,Bu, Qianqian,Zhang, Shujiang
experimental part, p. 767 - 775 (2010/09/04)
Two kinds of aromatic, unsymmetrical diamines with ether-ketone group, 3-amino-4'-(4-amino-2- trifluoromethylphenoxy)-benzophenone and 4-amino-4'-(4-amino-2-trifluoromethylphenoxy)-benzophenone, were successfully synthesized with two different synthetic r
Optimised synthesis and photochemistry of antenna-sensitised 1-acyl-7-nitroindolines
Papageorgiou, George,Corrie, John E.T.
, p. 609 - 616 (2007/10/03)
Benzophenone antenna-sensitised 1-acyl-7-nitroindolines show a significantly enhanced extent of photochemical cleavage in aqueous solution over their non-sensitised analogues and release the carboxylate derived from their 1-acyl group. The present work in
Discovery and SAR development of 2-(phenylamino) imidazolines as postacyclin receptor antagonists
Clark, Robin D.,Jahangir, Alam,Severance, Daniel,Salazar, Rick,Chang, Thomas,Chang, David,Jett, Mary Frances,Smith, Steven,Bley, Keith
, p. 1053 - 1056 (2007/10/03)
On the basis of screening hits (1a,b), a series of selective, high affinity prostacyclin receptor antagonists was developed. The optimized lead compound 25d [(4,5-dihydro-1H-imidazol-2-yl)-[4-(4-isopropoxybenzyl)phenyl] amine] had analgesic activity in the rat.
Synthesis and structure-activity relationship for new series of 4-phenoxyquinoline derivatives as specific inhibitors of platelet-derived growth factor receptor tyrosine kinase
Kubo, Kazuo,Ohyama, Shin-Ichi,Shimizu, Toshiyuki,Takami, Atsuya,Murooka, Hideko,Nishitoba, Tsuyoshi,Kato, Shinichiro,Yagi, Mikio,Kobayashi, Yoshiko,Iinuma, Noriko,Isoe, Toshiyuki,Nakamura, Kazuhide,Iijima, Hiroshi,Osawa, Tatsushi,Izawa, Toshio
, p. 5117 - 5133 (2007/10/03)
We discovered a new series of 4-phenoxyquinoline derivatives as potent and selective inhibitors of the platelet-derived growth factor receptor (PDGFr) tyrosine kinase. We researched the highly potent and selective inhibitors on the basis of both PDGFr and epidermal growth factor receptor (EGFr) inhibitory activity. First, we found a compound, Ki6783 (1), which inhibited PDGFr autophosphorylation at 0.13 μM, but it did not inhibit EGFr autophosphorylation at 100 μM. After extensive explorations, we found the two desired compounds, Ki6896 (2) and Ki6945 (3), which are substituted by benzoyl and benzamide at the 4-position of the phenoxy group on 4-phenoxyquinoline, respectively. These inhibitory activities were 0.31 and 0.050 μM, respectively, but neither of them inhibited EGFr autophosphorylation at 100 μM. We further investigated the profile of both compounds toward various tyrosine and serine/threonine kinases. The three compounds specifically inhibited PDGFr rather than the other kinases.
