29840-57-1Relevant academic research and scientific papers
Si113-prodrugs selectively activated by plasmin against hepatocellular and ovarian carcinoma
Rango, Enrico,D'Antona, Lucia,Iovenitti, Giulia,Brai, Annalaura,Mancini, Arianna,Zamperini, Claudio,Trivisani, Claudia Immacolata,Marianelli, Stefano,Fallacara, Anna Lucia,Molinari, Alessio,Cianciusi, Annarita,Schenone, Silvia,Perrotti, Nicola,Dreassi, Elena,Botta, Maurizio
, (2021)
Si113, a pyrazolo[3,4-d]pyrimidine derivative, gained more attention as an anticancer agent due to its potent anticancer activity on both in vitro and in vivo hepatocellular carcinomas (HCC) and ovarian carcinoma models. But the drawback is the low water
Br?nsted acid-mediated annulations of pyrroles featuring N-tethered α,β-unsaturated ketones and esters: Total syntheses of (±)-tashiromine and (±)-indolizidine 209I
Olivier, Wesley J.,Gardiner, Michael G.,Bissember, Alex C.,Smith, Jason A.
supporting information, p. 5436 - 5441 (2018/05/16)
This study provides the first report of the construction of tetrahydroindolizines and tetrahydropyrrolo[1,2-a]azepines via Br?nsted acid-mediated annulation of pyrroles featuring N-tethered α,β-unsaturated esters. In addition, the Br?nsted acid-catalyzed cyclization of pyrroles featuring pendant α,β-unsaturated ketones was applied to complete total syntheses of the indolizidine alkaloids (±)-tashiromine and (±)-indolizidine 209I.
Directing Group in Decarboxylative Cross-Coupling: Copper-Catalyzed Site-Selective C-N Bond Formation from Nonactivated Aliphatic Carboxylic Acids
Liu, Zhao-Jing,Lu, Xi,Wang, Guan,Li, Lei,Jiang, Wei-Tao,Wang, Yu-Dong,Xiao, Bin,Fu, Yao
supporting information, p. 9714 - 9719 (2016/08/11)
Copper-catalyzed directed decarboxylative amination of nonactivated aliphatic carboxylic acids is described. This intramolecular C-N bond formation reaction provides efficient access to the synthesis of pyrrolidine and piperidine derivatives as well as the modification of complex natural products. Moreover, this reaction presents excellent site-selectivity in the C-N bond formation step through the use of directing group. Our work can be considered as a big step toward controllable radical decarboxylative carbon-heteroatom cross-coupling.
Stereoselective synthesis of (2E,4Z)-dienamides employing (triphenylphosphoranylidene)ketene
Pachali, Steffen,Hofmann, Christine,Rapp, Georg,Schobert, Rainer,Baro, Angelika,Frey, Wolfgang,Laschat, Sabine
body text, p. 2828 - 2835 (2009/09/29)
The three-component reaction between ylide Ph3PCCO, amines and aldehydes is known to afford selectively (￡)-a,ssunsaturated amides. We applied a variant of this methodology to the preparation of (2B,4Z)-dienamides 11 utilizing the phosphonium s
Novel heterobivalent tacrine derivatives as cholinesterase inhibitors with notable selectivity toward butyrylcholinesterase
Elsinghorst, Paul W.,González Tanarro, Camino M.,Gütschow, Michael
, p. 7540 - 7544 (2007/10/03)
Two series of novel heterobivalent tacrine derivatives were synthesized. A trimethoxy substituted benzene was linked to the tacrine moiety by a hydrazide-based linker. The compounds were evaluated as cholinesterase inhibitors, and trimethoxybenzoic acid derivatives with 11- or 12-atom spacers were the most potent inhibitors of human acetylcholinesterase. The inhibitors showed a surprising selectivity toward human butyrylcholinesterase, where several trimethoxyphenylpropionic acid derivatives had IC50 values less than 250 pM.
2-Pyridylcarboxamides which inhibit arachidonic acid release
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, (2008/06/13)
2-Pyridylcarboxamides are provided having the structure STR1 wherein n is 1 to 10; R is hydrogen, lower alkyl, alkali metal or an amine salt; and R1 is C6 -C20 alkyl, C6 -C20 alkenyl, C6 to C20 alkoxy or phenyl. These compounds are useful as inhibitors of arachidonic acid release and as such are useful as antiallergy agents.
N6 -Substituted adenosines
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, (2008/06/13)
Novel N6 -adenosines according to formula I are disclosed. These novel compounds are useful as antihypertensive agents.
