85209-06-9Relevant academic research and scientific papers
Hedgehog pathway inhibitors of the acylthiourea and acylguanidine class show antitumor activity on colon cancer in vitro and in vivo
Vesci, Loredana,Milazzo, Ferdinando Maria,Stasi, Maria Antonietta,Pace, Silvia,Manera, Francesco,Tallarico, Carlo,Cini, Elena,Petricci, Elena,Manetti, Fabrizio,De Santis, Rita,Giannini, Giuseppe
, p. 368 - 379 (2018/08/17)
Small series of acylguanidine and acylthiourea derivatives were synthesized in gram-scale and assayed for their ability to modulate the Hh signalling pathway. In vitro studies showed a low micromolar inhibitory activity toward tumor cell lines, while the oral administration revealed an excellent ADME profile in vivo. Compound 5 emerged as the most active and safe inhibitor of colon cancer cells both in vitro and in a xenograft mouse model. Based on these data, 5 could be prioritized to further development with the perspective of clinical studies.
Rh(III)-Catalyzed Redox-Neutral Annulation of Primary Benzamides with Diazo Compounds: Approach to Isoquinolinones
Wu, Youzhi,Sun, Peng,Zhang, Kaifan,Yang, Tie,Yao, Hequan,Lin, Aijun
, p. 2166 - 2173 (2016/03/15)
Reported herein is a Rh-catalyzed redox-neutral annulation of primary benzamides with diazo compounds, representing an efficient and economic protocol to isoquinolinones. The procedure exhibited good functional group tolerability, scalability, and regioselectivity, obviating the need for oxidants, and only environmentally benign N2 and H2O were released. Further utilization of the method provided an alternative route to functionalized isoquinolines.
Solvent- and light-controlled unidirectional transit of a nonsymmetric molecular axle through a nonsymmetric molecular wheel
Arduini, Arturo,Bussolati, Rocco,Credi, Alberto,Monaco, Simone,Secchi, Andrea,Silvi, Serena,Venturi, Margherita
, p. 16203 - 16213 (2013/02/23)
The development of a pseudorotaxane motif capable of performing unidirectional threading and dethreading processes under control of external stimuli is particularly important for the construction of processive linear motors based on rotaxanes and, at leas
4-halogenostilbene derivatives and processes for their preparation
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, (2008/06/13)
Novel compounds of the formula STR1 and processes for their preparation are described. X represents bromine or iodine and R1, R2 and R3 have the meaning indicated in the patent claim. The compounds (I) are valuable intermediates for the preparation of fluorescent brighteners of the divinylstilbene type.
SELECTIVE REACTIONS OF α-ARYL WITTIG REAGENTS WITH THE FORMYL MOIETY OF 4-FORMYLBENZOYL CHLORIDE
Waetjen, Frank,Dahl, Otto,Buchardt, Ole
, p. 4741 - 4744 (2007/10/02)
The benzylic Wittig reagents 2a, 2b and 2e react with 4-formylbenzoyl chloride 1 to give 40-60percent yields of products 3 derived from selective attack at the formyl group of 1; The same selectivity is not found for the non-stabilized ylids 2c and 2d or
