110452-36-3Relevant academic research and scientific papers
High-throughput screening of ecdysone agonists using a reporter gene assay followed by 3-D QSAR analysis of the molting hormonal activity
Wheelock, Craig E.,Nakagawa, Yoshiaki,Harada, Toshiyuki,Oikawa, Nobuhiro,Akamatsu, Miki,Smagghe, Guy,Stefanou, Dimitra,Iatrou, Kostas,Swevers, Luc
, p. 1143 - 1159 (2006)
In this study, 172 diacylhydrazine analogs were examined for their ability to activate an ecdysone (molting hormone)-dependent reporter gene in a silkworm (Bombyx mori) cell-based high-throughput screening assay. The measured EC 50 values (concentration required to cause an effect in 50% of the cells) were used to construct a 3-D QSAR model that describes the ecdysone agonist activities of the diacylhydrazine analogs. Of these compounds, 14 exhibited no activity and were excluded from the 3-D QSAR analysis. The resulting equation described ~74% of the activity for 158 compounds. The final equation consisted of 42% electrostatic and 58% steric effects (r 2 = 0.74 and q2 = 0.45). Comparative molecular field analysis (CoMFA) was used to visualize the steric and electrostatic potential fields that were favorable and unfavorable for biological activity. Of particular interest was the observation that the hydrophobic parameter (log P) was not necessary for describing the observed activities, although previous studies have cited the importance of hydrophobic parameters in both classical and 3-D QSAR analyses of these compounds. Modeling studies of the B. mori ecdysone receptor supported the observed physicochemical parameters required for activity reported by the CoMFA models. Comparison of the present analysis with those performed using other lepidopteran assay systems evidenced a high degree of correlation (r2 = 0.81 for a Sf-9 cell-based assay and r 2 = 0.89 for a Chilo suppressalis integument-based assay), indicating that it is valid to compare the results generated with the B. mori cell-based system to those generated with previous lepidopteran assays. This novel assay system is amendable to a high-throughput screening format and should greatly increase our ability to discover novel agonists of molting hormone (ecdysone) activity.
A convenient way for alkylation of amines using xanthate esters
Sukrutha, Kodipura P.,Swaroop, Toreshettahally R.,Preetham, Ramesh,Lokanath, Neratur K.,Rangappa, Kanchugarakoppal S.,Sadashiva, Maralinganadoddi P.
, p. 2316 - 2323 (2021/06/14)
N-alkylation of amines by the reaction with xanthate esters in the presence of acetic acid catalyst in ethanol is reported. Short reaction time, high yield, general applicability and environmentally benign nature are the noteworthy features of our protocol. The probable mechanism for the formation N-alkylation of amines is proposed.
HDAC INHIBITOR COMPOUNDS AND METHODS OF TREATMENT
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Page/Page column 36; 37; 38, (2015/11/17)
The instant invention describes hydrazide-containing compounds having therapeutic activity, and methods of treating disorders such as cancer, tumors and cell proliferation related disorders, or affect cell differentiation, dedifferentiation or transdiffer
1,2-Reduction of α,β-unsaturated hydrazones using dimethylamine-borane/p-toluenesulfonic acid: An easy route to allyl hydrazines
Casarini, Maria E,Ghelfi, Franco,Libertini, Emanuela,Pagnoni, Ugo M,Parsons, Andrew F
, p. 7925 - 7932 (2007/10/03)
α,β-Unsaturated hydrazones can be easily converted into N-allyl hydrazines by reaction with dimethylamine-borane/p-toluenesulfonic acid under mild reaction conditions. The reduction works well for N′-allylhydrazides but N′-allyl-N,N-dimethylhydrazines are
Convenient Syntheses of 1-Acyl-2-alkylhydrazines
Okawara, Tadashi,Kanazawa, Yasunori,Yamasaki, Tetsuo,Furukawa, Mitsuru
, p. 183 - 184 (2007/10/02)
1-Acyl-2-alkylhydrazines 7 were prepared from hydroxamic acids 1 and amines 6 using 2-chloro-1-methylpyridinium iodide 2 or p-toluenesulfonyl chloride 3 in 27-68percent yield.
