- Catalytic asymmetric Tamura cycloadditions involving nitroalkenes
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The first examples of asymmetric Tamura cycloaddition reactions involving singly activated alkenes are reported. Homophthalic anhydride reacts with α-methyl nitrosytrenes in the presence of an alkaloid-based catalyst to generate fused bicyclic aromatic ketone products with three new stereocentres (which are susceptible to subsequent equilibration) in 12-99% ee. An unusual equilibration process which occurs in methanolic medium in the absence of a recognisable base via proton transfer at the α-carbon of an ester was investigated experimentally and computationally.
- Manoni, Francesco,Farid, Umar,Trujillo, Cristina,Connon, Stephen J.
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p. 1463 - 1474
(2017/02/15)
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- A systematic study on the use of different organocatalytic activation modes for asymmetric conjugated addition reactions of isoindolinones
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In this article we describe a series of new asymmetric Michael reactions of carboxylate-3-substituted isoindolinones used as nucleophiles in the synthesis of valuable chiral tetrasubstituted derivatives. It has been shown that the reactivity and enantiose
- Scorzelli, Francesco,Di Mola, Antonia,De Piano, Francesco,Tedesco, Consiglia,Palombi, Laura,Filosa, Rosanna,Waser, Mario,Massa, Antonio
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supporting information
p. 819 - 828
(2017/01/28)
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- A short and efficient construction of the dibenzo[c,h]chromen-6-one skeleton
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We hereby report a major revision of the synthetic methodology for construction of the dibenzochromenone skeleton. Homophthalic acid derivatives were reacted with thionylchloride/DMF in the presence of NaN 3. As the main product, dibenzochromen
- Delioemeroglu, Murat K.,Oezcan, Sevil,Balcia, Metin
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experimental part
p. 148 - 160
(2010/08/04)
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- Design, synthesis, and biological evaluation of a series of 2-hydroxyisoquinoline-1,3(2H,4H)-diones as dual inhibitors of human immunodeficiency virus type 1 integrase and the reverse transcriptase RNase H domain
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We report herein the synthesis of a series of 19 2-hydroxyisoquinoline-1, 3(2H,4H)-dione derivatives variously substituted at position 7 aimed at inhibiting selectively two-metal ion catalytic active sites. The compounds were tested against HIV-1 reverse
- Billamboz, Muriel,Bailly, Fabrice,Barreca, Maria Letizia,De Luca, Laura,Mouscadet, Jean-Fran?ois,Calmels, Christina,Andréola, Marie-Line,Witvrouw, Myriam,Christ, Frauke,Debyser, Zeger,Cotelle, Philippe
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experimental part
p. 7717 - 7730
(2009/12/07)
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- 4-(Phenylaminomethylene)isoquinoline-1,3(2H,4H)-diones as potent and selective inhibitors of the cyclin-dependent kinase 4 (CDK4)
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The cyclin-dependent kinases (CDKs), as complexes with their respective partners, the cyclins, are critical regulators of cell cycle progression. Because aberrant regulations of CDK4/cyclin D1 lead to uncontrolled cell proliferation, a hallmark of cancer, small-molecule inhibitors of CDK4/cyclin D1 are attractive as prospective antitumor agents. The series of 4-(phenylaminomethylene)isoquinoline-1,3(2H,4H)-dione derivatives reported here represents a novel class of potent inhibitors that selectively inhibit CDK4 over CDK2 and CDK1 activities. In the headpiece of the 4-(phenylaminomethylene) isoquinoline-1,3(2H,4H)-dione, a basic amine substitutent is required on the aniline ring for the CDK4 inhibitory activity. The inhibitory activity is further enhanced when an aryl or heteroaryl substituent is introduced at the C-6 position of the isoquinoline-1,3(2H,4H)-dione core. We present here SAR data and a CDK4 mimic model that explains the binding, potency, and selectivity of our CDK4 selective inhibitors.
- Tsou, Hwei-Ru,Otteng, Mercy,Tran, Tritin,Floyd Jr., M. Brawner,Reich, Marvin,Birnberg, Gary,Kutterer, Kristina,Ayral-Kaloustian, Semiramis,Ravi, Malini,Nilakantan, Ramaswamy,Grillo, Mary,McGinnis, John P.,Rabindran, Sridhar K.
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experimental part
p. 3507 - 3525
(2009/04/07)
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- AMIDE DERIVATIVES
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The invention concerns a compound of the Formula I (A chemical formula should be inserted here - please see paper copy enclosed herewith) wherein m is 0-2 and each R1 is a group such as hydroxy, halogeno, trifluoromethyl heterocyclyl and heterocyclyloxy; R2 is halogeno, trifluoromethyl or (1-6C)alkyl; R3 is hydrogen, halogeno or (1-6C)alkyl; and R4 is (3-6C)cycloalkyl;or pharmaceutically-acceptable salts thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical condions mediated by cytokines.
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Page/Page column 64-65
(2008/06/13)
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- 3,3-disubstituted-oxindole derivatives useful as anticancer agents
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The present invention relates to compounds of formula 1 and to pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein n is 0 or 1 and R1, R2, R3, R4, and R5are as defined herein. The above compounds of formula 1 are useful in the treatment of hyperproliferative disorders, such as cancer, in mammals. The invention also relates to pharmaceutical compositions containing the compounds of formula 1, to methods of inhibiting abnormal cell growth, including cancer, in a mammal by administering the compounds of formula 1 to a mammal requiring such treatment, and to methods of preparing compounds of formula 1.
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- Antihypertensive tricyclic isoindole derivatives
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Tricyclic isoindole derivatives characterized by having a 1,2,3,4,6,10b-hexahydropyrazino[2,1-a]isoindole or 1,3,4,10b-tetrahydropyrimido[6,1-a]isoindol-6(2H)-one nucleus are disclosed. The foregoing compounds are useful antihypertensive agents.
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