143360-01-4Relevant academic research and scientific papers
A para-C–H Functionalization of Aniline Derivatives via In situ Generated Bulky Hypervalent Iodinium Reagents
Tian, Chao,Yao, Xu,Ji, Weizhe,Wang, Qian,An, Guanghui,Li, Guangming
supporting information, p. 5972 - 5979 (2018/11/23)
A practical para-C-H functionalization of aniline derivatives has been developed using an in situ generated bulky hypervalent iodinium reagent. Para-iodo, bromo, chloro, nitro, trifluormethyl aniline derivatives can be obtained efficiently, in many cases in 10 min in a transition metal-free manner. Medicinal chemicals or intermediates can be purified without column chromatography or recrystallization, which significantly reduces the waste and simplifies the work-up process.
Identification of 4,5-dihydro-1 H -pyrazolo[4,3- h ]quinazoline Derivatives as a new class of orally and selective polo-like kinase 1 inhibitors
Beria, Italo,Ballinari, Dario,Bertrand, Jay Aaron,Borghi, Daniela,Bossi, Roberto Tiberio,Brasca, Maria Gabriella,Cappella, Paolo,Caruso, Michele,Ceccarelli, Walter,Ciavolella, Antonella,Cristiani, Cinzia,Croci, Valter,De Ponti, Anna,Fachin, Gabriele,Ferguson, Ronald Dale,Lansen, Jacqueline,Moll, Jurgen Karl,Pesenti, Enrico,Posteri, Helena,Perego, Rita,Rocchetti, Maurizio,Storici, Paola,Volpi, Daniele,Valsasina, Barbara
experimental part, p. 3532 - 3551 (2010/09/11)
Polo-like kinase 1 (Plk1) is a fundamental regulator of mitotic progression whose overexpression is often associated with oncogenesis and therefore is recognized as an attractive therapeutic target in the treatment of proliferative diseases. Here we discuss the Structure-activity relationship of the 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline class of compounds that emerged from a high throughput screening (HTS) campaign as potent inhibitors of Plk1 kinase. Furthermore, we describe the discovery of 49, 8-{[2-methoxy-5-(4- methylpiperazin-1-yl)phenyl]amino}-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h] quinazoline-3-carboxamide, as a highly potent and specific ATP mimetic inhibitor of Plk1 (IC50 = 0.007 μM) as well as its crystal structure in complex with the methylated Plk136-345 construct. Compound 49 was active in cell proliferation against different tumor cell lines with IC 50 values in the submicromolar range and active in vivo in the HCT116 xenograft model where it showed 82% tumor growth inhibition after repeated oral administration.
SUBSTITUTED PYRAZOLO-QUINAZOLINE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS
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Page/Page column 87-88, (2008/12/06)
Pyrazolo-quinazoline derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may
Studies on enamides. VI. An improvised methodology for orton rearrangement under neutral condition
Ghosh,Baul
, p. 2783 - 2786 (2007/10/03)
A highly efficient methodology in neutral medium has been developed for the synthesis of bromoanilides from the corresponding anilides using N-bromosuccinimide in carbon tetrachloride under irradiation with visible light. The products are obtained in highly pure crystalline state with an excellent yield.
Reexamination of the Thermolytic Rearrangement of 4-Halophenyl Azides to 2-Aminophenols and other Products
Gershon, H.,Clarke, D. D.,Gershon, M.
, p. 367 - 380 (2007/10/02)
The halogenation of derivatives of 2-aminophenol with N-chloro- and N-bromosuccinimides at ambient temperatures in acetic acid was studied.With the necessary compounds available, a reexamination of the thermolytic rearrangement of 2-halophenyl azides to 2-aminophenols and other products was undertaken.It is certain that the rearrangement of 4-halophenyl azides to 2-aminophenols occurs but the products identified in this study differ significantly from those reported previously by Suschitzky et al. (1963, 1966). Keywords: Acetylated-2-amino-5-halophenols; 2-Acetamido-5-haloanisoles; 6-Halo-2-methylbenzoxazoles; 6-Halobenzoxazolones; 6-Halotriacetylaminophenols; 1H-NMR spectra; Fungicidal activity.
