- Novel fatty acid synthase (FAS) inhibitors: Design, synthesis, biological evaluation, and molecular docking studies
-
Several novel series of C75 derivatives were synthesized and evaluated for their FAS inhibitory activities. The results showed compound 4-methylene-2-octyl-5-oxo-tetrahydro-thiophene-3-carboxylic acid (1c) had more effective FAS inhibitory (IC50 was 2.56 μM and T.I. was 9.26) and potent anti-tumor activities on HL60 and Hela cells in vitro (IC50 were 5.38 μM and 46.10 μM, respectively).
- Wang, Xiaokui,Lin, Jian,Chen, Yao,Zhong, Wu,Zhao, Guoming,Liu, Hongying,Li, Site,Wang, Lili,Li, Song
-
experimental part
p. 1898 - 1904
(2009/05/26)
-
- Solvent free Stobbe condensation: A green approach
-
Solvent free Stobbe-condensation of methyl β benzoyl propionate 1c and methyl β-naphthoyl propionate 1d with benzaldehyde, anisaldehyde and furfural using dry solid potassium tertiary butoxide at room temperature and at 80°C gives β arylidene β benzoyl pr
- Banerjee, Shubhra,Tayde, Ravibabu A,Sharma, Bhagyashree D
-
experimental part
p. 882 - 885
(2009/12/24)
-
- Process for preparing alkylidene substituted succinic acid esters
-
A process for the preparation of alkylidene substituted succinates comprising a step (a) in which is carried out the reaction of a carbonilic compound, a succinic and a base in a reaction medium and a step (b) in which the alkylidene substituted product obtained in (a) is esterified, characterized in that the succinic ester is used in a molar amount substantially equal to, or lower than, the amount of compound carbonilic compound, (ii) the base is used in a molar amount substantially equal to the succinic ester and is selected from metal hydrides and metal and alkoxides, and (iii) the reaction medium comprises an aprotic liquid medium or a protic liquid medium having a Ka, measured in water, lower than that of iPrOH.
- -
-
-
- Conjugate addition of nitroalkanes to dimethyl maleate. Regioselective formation of both monoesters of 2-alkylsuccinic acids
-
Diesters of (E)-2-alkylidenesuccinic acids obtained by conjugate addition of nitroalkanes to dimethyl maleate can be selectively monohydrolyzed at the more reactive carboxyl group to the corresponding half-ester. Alternatively, total hydrolysis to the dia
- Ballini, Roberto,Bosica, Giovanna,Palmieri, Alessandro,Petrini, Marino,Pierantozzi, Claudio
-
p. 7283 - 7289
(2007/10/03)
-
- Hydroxamic acids as potent inhibitors of endothelin-converting enzyme from human bronchiolar smooth muscle
-
Hydroxamic acids 6a-h, derived from malonyl amino acids, and 25a-d, derived from succinyl amino acids, were synthesized as inhibitors of human bronchiolar smooth muscle endothelin-converting enzyme (HBSM ECE). Several unexpected side reactions were discov
- Bihovsky,Levinson,Loewi,Erhardt,Polokoff
-
p. 2119 - 2129
(2007/10/02)
-
- Preparation of (S)-2-Substituted Succinates by Stereospecific Reductions of Fumarate and Derivatives with Resting Cells of Clostridium formicoaceticum
-
Fumarate derivatives have been reduced to (S)-2-methylsuccinate 2a, (S)-2-ethylsuccinate 3a and (S)-2-chlorosuccinate 4a in up to 1 M concentrations with Clostridium formicoaceticum.Formate was the electron donor and viologens or anthraquinone-2,6-disulphonate acted as artificial electron mediators.Reductions with freeze-dried cells in 2H2O-buffers led to the (2R,3S)--dideuterated succinate derivatives.The productivity numbers ranged from 450 to 5000 and the enantiomeric excess of all (S)-2-substituted succinates was >/= 99percent.
- Eck, Richard,Simon, Helmut
-
p. 13631 - 13640
(2007/10/02)
-