130581-21-4Relevant academic research and scientific papers
Kinesin spindle protein (KSP) inhibitors. Part 1: The discovery of 3,5-diaryl-4,5-dihydropyrazoles as potent and selective inhibitors of the mitotic kinesin KSP
Cox, Christopher D.,Breslin, Michael J.,Mariano, Brenda J.,Coleman, Paul J.,Buser, Carolyn A.,Walsh, Eileen S.,Hamilton, Kelly,Huber, Hans E.,Kohl, Nancy E.,Torrent, Maricel,Yan, Youwei,Kuo, Laurence C.,Hartman, George D.
, p. 2041 - 2045 (2005)
Optimization of high-throughput screening (HTS) hits resulted in the discovery of 3,5-diaryl-4,5-dihydropyrazoles as potent and selective inhibitors of KSP. Dihydropyrazole 15 is a potent, cell-active KSP inhibitor that induces apoptosis and generates aberrant mitotic spindles in human ovarian carcinoma cells at low nanomolar concentrations. X-ray crystallographic evidence is presented which demonstrates that these inhibitors bind in an allosteric pocket of KSP distant from the nucleotide and microtubule binding sites.
Hydroxyl- and Halogen-containing Chalcones for the Inhibition of LPS-stimulated ROS Production in RAW 264.7 Macrophages: Design, Synthesis and Structure–Activity Relationship Study
Shrestha, Aarajana,Shrestha, Aastha,Park, Pil-Hoon,Lee, Eung-Seok
, p. 729 - 734 (2019/07/19)
Oxidative stress due to overproduction of reactive oxygen species (ROS) plays a major role in inflammation, cancer, and neurodegenerative disorders. In this study, 60 chalcone derivatives with fluorine (F), trifluoromethyl (CF3), trifluoromethoxy (OCF3), chlorine (Cl), and bromine (Br) in ring A and with or without hydroxy (OH) in ring B were designed, synthesized, and screened for inhibitory activity against lipopolysaccharide (LPS)-stimulated ROS production in RAW 264.7 macrophages. Structure–activity relationship study revealed the importance of a hydroxyl moiety in ring B for enhancing inhibitory activity of ROS production. Furthermore, a hydroxyl group at the ortho-position is more essential for inhibition of ROS production followed by meta- and para-positions. Among all, compound 27 that contains para-chlorine moiety in ring A and ortho-hydroxy in ring B displayed the strongest inhibitory activity (IC50 = 3.42 μM) against LPS-stimulated ROS production in RAW264.7 macrophages.
Mesomorphism in chloro substituted isomeric series including chalconyl central bridge
Namera, Dipti L.,Ranchchh, Avani R.,Bhoya
, p. 233 - 240 (2017/03/08)
A novel homologous series of thermotropic liquid crystals α-4-(4′-n-alkoxy benzoyloxy phenyl) β-2″-chloro benzoyl ethylenes have been synthesized and studied with a view to understand and establish the effect of molecular structure on liquid crystal (LC) properties with reference to molecular flexibility in isomeric series with differing positional status of same functional group. Novel homologues series consist of 12 homologues C1 to C16. C1, C2, and C3 homologues are nonliquid crystals (NLC) and rest of the homologues are liquid crystals. C10 to C16 homologues are enantiotropically smectogenic plus nematogenic and C4 to C8 homologues are enantiotropic nematic. The texture of nematogenic derivatives is threaded or schlieren and that of the smectic mesophase are focal conic of the type smectic A or C. Analytical, thermal and spectral data supported molecular structures of novel homologues. Transition temperatures as determine by a hot stage polarizing optical microscopy (POM) were plotted against number of carbon atom present in n-alkyl chain ‘R’ of left n-alkoxy (-OR) group and the phase transition curves Cr–I/M, Sm–N, N–I were obtained on linking like or related points. The odd–even effect is observed for the N–I transition curve and thus transition curves behaved in normal manner. The even-membered nematic transition curve occupied higher position than the odd-membered transition curve. Present series is predominantly nematogenic and partly smectogenic with middle-ordered melting type.
Design, synthesis, and antitumor evaluation of 2,4,6-triaryl pyridines containing chlorophenyl and phenolic moiety
Thapa, Pritam,Karki, Radha,Yun, Minho,Kadayat, Tara Man,Lee, Eunyoung,Kwon, Han Byeol,Na, Younghwa,Cho, Won-Jea,Kim, Nam Doo,Jeong, Byeong-Seon,Kwon, Youngjoo,Lee, Eung-Seok
experimental part, p. 123 - 136 (2012/07/27)
We have designed and synthesized a series of 2,4,6-triaryl pyridine derivatives containing chlorophenyl and phenolic moeity at 2- and 4- position of the central pyridine, respectively, resulting in a total of 42 compounds. They were evaluated for topoisom
Synthesis and protein tyrosine phosphatase 1B-Inhibitory activity of chalcones
Zhao, Fei,Zhao, Qing-Jie,Zhang, Da-Zhi,Jin, Yong-Sheng,Zhang, Wei
experimental part, p. 5339 - 5342 (2012/06/30)
Protein tyrosine phosphatase 1B (PTP1B) is an effective target for the treatment of type 2 diabetes and obesity. So far less work has been conducted in the structure-activity relationship of the PTP1B inhibitory activity of chalcones. In this work, a libr
