- Synthesis, biological evaluation and molecular docking studies of novel 2-(2-cyanophenyl)-N-phenylacetamide derivatives
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A series of novel 2-(2-cyanophenyl)-N-phenylacetamide derivatives 3(a-u) were designed and synthesized via selective amidation of methyl-2-(2-cyanophenyl)acetates over amidine formation by using AlMe3 as catalyst in good yields. All the newly s
- Konidena, Lakshmi Narayana Sharma,Boda, Sathish Kumar,Chettu, Suresh Kumar,Sorra, Kumaraswamy,Enaganti, Sreenivas,Mukkavilli, Praveena,Kameswara Rao,Anantha Lakshmi,Korupolu, Raghu Babu
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- (Cyanovinyl)ketenes from azafulvenones. An apparent retro-Wolff rearrangement
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Flash vacuum pyrolyses or pulsed pyrolysis of azole esters 1b and 20 and their carboxylic acids 1a and 19 or acid chloride 1c give five-membered ring ketenes (azafulvenones) 2 and 24 which dimerize to diketopiperazines 3 and 21 but also undergo efficient
- Qiao,Meutermans,Wong,Traubel,Wentrup
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- 1, 2 - DIHYDRO- 3H- PYRAZOLO [3, 4 - D] PYRIMIDIN -3 - ONE ANALOGS
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Compounds of Formula (I) are provided herein. Such compounds, as well as pharmaceutically acceptable salts and compositions thereof, are useful for treating diseases or conditions, including conditions characterized by excessive cellular proliferation, such as breast cancer.
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- Macrocyclic derivative of pyrazole[3,4-d]pyrimidin-3-one and pharmaceutical composition and application thereof
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The present invention relates to a macrocyclic derivative of pyrazole[3,4-d]pyrimidin-3-one as shown in the formula (I) and/or a pharmaceutically acceptable salt thereof, and a composition of a compound of the formula (I) and/or a pharmaceutically acceptable salt thereof, a preparation method thereof, application thereof as a Wee1 inhibitor and application thereof as a sensitizer for cancer chemotherapy or radiotherapy. The macrocyclic derivative of pyrazole[3,4-d]pyrimidin-3-one can effectively inhibit Wee1 and related signaling pathways, and has good cancer treatment and/or relieving effect.The formula is shown in the description.
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Paragraph 0332; 0414; 0415; 0416
(2018/10/19)
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- Expedient drug synthesis and diversification via ortho-C-H iodination using recyclable PdI2 as the precatalyst
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(Figure Presented) Pd(II)-catalyzed ortho-C-H iodination reactions of phenylacetic acid substrates have been achieved using recyclable PdI2 as the precatalyst. This class of substrates is incompatible with the classic amide formation/ortho-lithiation/iodination sequence. The power of this new technology is demonstrated by facile drug functionalization and drastically shortened syntheses of the drugs diclofenac and lumiracoxib.
- Mei, Tian-Sheng,Wang, Dong-Hui,Yu, Jin-Quan
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supporting information; experimental part
p. 3140 - 3143
(2010/09/03)
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- A multi-task palladium catalyst involved in heck-reduction-cyclization sequences for the preparation of 4-benzyl-1,2-dihydroisoquinolin-3-ones: An unusual homogeneous-heterogeneous sustainable approach
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A mixed homogeneous-heterogeneous catalysis that exploits a multi-task palladium catalyst has been developed for one-pot sequential Heck-reduction-cyclization (HRC) reactions leading to novel 4-benzyl-1,2- dihydroisoquinolin-3-ones. The HRC sequence requires mild conditions and allows the separation of the palladium residues under the form of an in situ generated Pd(0)/C catalyst by simple filtration. The homemade and recovered catalyst can be efficiently reused for Suzuki-Miyaura reactions and reductive processes making it useful for sustainable chemistry. Georg Thieme Verlag Stuttgart New York.
- Laudien, Julia,Fouquet, Eric,Zakri, Cécile,Felpin, Fran?ois-Xavier
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experimental part
p. 1539 - 1543
(2010/08/22)
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- Arylacetamide κ opioid receptor agonists with reduced cytochrome P450 2D6 inhibitory activity
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Some κ opioid receptor agonists of the arylacetamide class, for example, ICI 199441 (1), were found to strongly inhibit the activity of cytochrome P450 2D6 (CYP2D6) (1: CYP2D6 IC50 = 26 nM). Certain analogs bearing a substituted sulfonylamino group, for example, 13, were discovered to have significantly reduced CYP2D6 inhibitory activity (13: CYP2D6 IC50 > 10 μM) while displaying high affinity toward the cloned human κ opioid receptor, good κ/δ and κ/μ selectivity, and potent in vitro and in vivo agonist activity.
- Le Bourdonnec, Bertrand,Ajello, Christopher W.,Seida, Pamela R.,Susnow, Roberta G.,Cassel, Joel A.,Belanger, Serge,Stabley, Gabriel J.,DeHaven, Robert N.,DeHaven-Hudkins, Diane L.,Dolle, Roland E.
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p. 2647 - 2652
(2007/10/03)
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- Sulfonylamino phenylacetamide derivatives and methods of their use
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Sulfonylamino phenylacetamide derivatives of the general formula are disclosed. Pharmaceutical compositions containing the compounds and methods for their use are also disclosed. In certain embodiments, the compounds of the invention that, preferably: (1) bind with high affinity to κ opioid receptors; (2) display good opioid receptor selectivity of κ versus μ and κ versus δ; and (3) do not substantially inhibit cytochrome P450 enzymatic activity, in particular CYP2D6, CYP2C9 and CYP3A4.
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- 1,2-disubstituted-6-oxo-3-phenyl-piperidine-3-carboxamides and combinatorial libraries thereof
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The invention relates to combinatorial libraries containing two or more novel piperidine-3-carboxamide derivative compounds, methods of preparing the piperidine-3-carboxamide derivative compounds and piperidine-3-carboxamide derivative compounds bound to a resin
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