105703-65-9Relevant articles and documents
Synthesis, structure, and biological assay of cinnamic amides as potential EGFR kinase inhibitors
Zhang, Mao,Lu, Xiang,Zhang, Hong-Jia,Li, Na,Xiao, Yu,Zhu, Hai-Liang,Ye, Yong-Hao
, p. 986 - 994 (2013/04/23)
A series of derivatives of cinnamic amide (compounds 2a-2v) were synthesized and evaluated for antiproliferative activities against the human breast cancer cell line MCF-7- and EGFR-inhibitory activities. The structures of compounds 2b and 2i were determined by single-crystal X-ray diffraction analysis. Compounds 2f and 2j showed moderate EGFR inhibitory activity with IC50 values of 5.16 and 7.37 μM, respectively. Docking simulation of compound 2f was carried out to illustrate the binding mode of the molecule into the EGFR active site. Structure-activity relationship analysis found that the N-phenyl rings are required for enhancing the activities.
NITROGEN HETEROCYCLIC COMPOUNDS USEFUL AS PDE10 INHIBITORS
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Page/Page column 183, (2011/12/02)
Unsaturated nitrogen heterocyclic compounds of formula (I): (I), as defined in the specification, compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, Huntington's Disease, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
Esters, amides and substituted derivatives of cinnamic acid: Synthesis, antimicrobial activity and QSAR investigations
Narasimhan, Balasubramanian,Belsare, Deepak,Pharande, Devayani,Mourya, Vishnukant,Dhake, Avinash
, p. 827 - 834 (2007/10/03)
A series of esters (Ia-k), substituted derivatives (II a-d) and amides (IIIa-q) of cinnamic acid were synthesized and evaluated as antibacterial and antifungal agents. All the derivatives belonging to the series I, II and III showed antimicrobial activity comparable to the standard. Compounds If and IIc proved to be the most effective compounds. Quantitative structure-activity relationship (QSAR) investigation with multiple linear regression analysis was applied to find a correlation between different calculated physicochemical parameters of the compounds and biological activity. The quantitative models relating the structural features of cinnamic acid derivatives Ia-k, II a-d and IIIa-q and their antimicrobial activity showed that Gram negative Escherichia coli and Candida albicans (fungus) were the most sensitive microorganisms.
AlCl3-mediated Regioselective Migration of a Methoxy Group of N-Methoxy-N-phenylamides to the ortho Position of the Phenyl Ring
Kikugawa, Yasuo,Shimada, Masahiro
, p. 1450 - 1451 (2007/10/02)
AlCl3-mediated decomposition of N-methoxy-N-phenylamides in dichloroethane leads to regioselective intramolecular migration of the methoxy group from the nitrogen to the ortho position of the phenyl ring via a tight ion pair intermediate.
Synthesis of Oxindole Derivatives from N-Alkenyl-o-Chloroanilides with Zero-Valent Nickel Complex
Canoira, L.,Rodriguez, J. G.
, p. 1511 - 1518 (2007/10/02)
Oxindole derivatives have been obtained from N-alkenyl-o-chloroanilides by reaction with tetrakis(triphenylphoaphine)nickel(0) in toluene as solvent in good yields.A detailed analysis of all the products of the reaction allows to confirm the postulated mechanism of the cyclization reaction.The o-chloroanilides of the 3-cyclohexenylacetic acid fails in the cyclization reaction, since the torsional hindrance seems to avoid that the endocyclic double bond may be orthogonally to the ortho-?-nickel complex intermediate on the aromatic ring.
