Histone deacetylases (HDACs) are enzymes involved in tumor genesis and development. Herein, we report a novel series of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives as HDACs inhibitors. The preliminary biological screening showed that most of our compounds exhibited potent inhibi...

Histone deacetylase inhibitors with desirable pharmacokinetic profiles which can be delivered to solid tumor tissues in large amount might be promising to treat solid tumor effectively. Herein, structural modification of a previously reported tetrahydroisoquinoline-based HDAC inhibitor 1 was car...

Conformationally constrained amino acids were synthesized in chiral or racemic forms: d- amd l-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (Tic), the erythro-d,l-4-methyl analogue, d- and l-7-hydroxy-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid, d- and l-7-hydroxy-6,8-diiodo-1,2,3,4-tet...

Tribo-electrification is a common occurrence within the pharmaceutical industry where solid dosage forms constitute majority of pharmaceutical formulations. Tribo-electrification of powders leads to a range of complications such as adhesion of particulate material to the processing equipment res...

In the synthesis of chiral molecules, the incorporation of enantioselective enzymatic conversions within the synthetic route often presents a useful approach. For the substitution of a chemical step with an enzymatic reaction, however, the complete synthetic route leading to and from this reacti...

A new route allowing the one-step synthesis of (2-heteroarylphenyl)tetrazole and fluorinated biphenyltetrazole derivatives is disclosed. By using 2 mol% of an air-stable diphosphine-palladium catalyst [PdCl(C3H5)(dppb)], potassium pivalate as base and dimethylacetamide as solvent, a wide range o...

Upon hemideprotonation of 8-bromoguanosine (8-BrG) at the N1 position, induced by DBU, the adduct [8-BrG][8-BrG]−[DBU–H]+ was formed. Slow evaporation of the 8-BrG methanol solution, in the presence of 0.5 equiv of DBU, yielded two polymorphic structures (1 and 2), where a neutral [8-BrG] (A) a...

The present work deals with the synthesis and characterization of novel multiblock copolymers containing poly(lactide) (PLA) and fatty acid dimer-based polyols. Notably, both blocks are bio-renewable. PLA segments are rigid and crystallizable, while the polyol-blocks are amorphous and possess lo...

Telechelic macromers end-capped with (meth)acrylic functionalities are the most commonly used materials in rigid, dental formulations. In order to provide higher flexibility to the final product (not necessarily for dental applications), long chain aliphatic fatty acid derivatives may be chosen....

The elongases of very long-chain fatty acids (Elovl) account for the rate-limiting condensation step of the elongation process in fatty acid (FA) biosynthesis in vertebrates. One member of the Elovl family, Elovl4, has been regarded as a critical enzyme in vertebrates in the production of the so...

Reactive polyamides with amine values ranging from 310 to 389 were prepared by reacting C21 cycloaliphatic dicarboxylic acid, prepared from acrylic acid and dehydrated castor oil fatty acids, with various polyamines, namely diethylenetriamine, triethylenetetramine and tetraethylenepentamine. Som...

Sinapic acid (SNP) is a nutraceutical compound of hydroxybenzoic acid derivative which possesses anti-oxidant, anti-microbial, anti-inflammatory, anti-cancer, and anti-anxiety activity properties. In the present work, two cocrystals of SNP with two active drug ingredients such as Ethenzamide (ET...

A green, simple and efficient protocol for the synthesis of the two new barbituric acid derivatives; 4 and 5 is described. One pot fashion of 2 mol of barbituric acid derivatives with 3-fluorobenzaldehyde in green solvent (H2O) providing compound 4. Reaction of equimolar of barbituric acid deriv...

The polymerization products of C18 fatty acids are complex mixtures of high dimeric, trimeric and higher molecular weight liquid acids. The current separation method for these mixtures involves a lengthy normal-phase HPLC gradient and the use of primary standards that are prepared via a semi-pre...

In this work, a rosin-derived diacid and a dimer fatty acid were converted into diglycidyl ester type epoxies, respectively, and the chemical structures of the products were confirmed by 1H NMR, FT-IR and ESI-MS. A novel modification was introduced to the two-step synthesis of diglycidyl ester b...

Non-reactive polyamides were prepared by reacting a mixture comprising polymeric fatty acids, diamines such as ethylenediamine and hexamethylenediamine and an aliphatic monobasic acid or amine, to obtain a product of the desired extent of reaction, degree of polymerization, number average molecu...

We synthesized new alternating conjugated polymers, PCDTFMMBI and PBDTDTFMMBI, which consist of trifluoromethyl substituted dimethyl-2H-benzimidazole (FMMBI) as new electron deficient unit, by palladium(0)-catalyzed Suzuki or Stille polymerization. Trifluoromethyl group has attractive features s...

Formycin B (FB), a moderate inhibitor (Ki ∼ 100 μM) of mammalian purine nucleoside phosphorylase (PNP), and formycin A (FA), which is totally inactive vs. the mammalian enzyme, are both effective inhibitors of the bacterial (Escherichia coli) enzyme (Ki ∼ 5 μM). Examination of a series of N-...

Previous research has demonstrated that acute and chronic opiate treatment alters receptor- and postreceptor-mediated adenylyl cyclase activity. This study examined the regulation of G protein- and forskolin-mediated adenylyl cyclase activity in mouse striatum and cortex after short- and long-te...

Primary amines react with pyrylium cations to give pyridiniums which transfer the N-substituent to a wide range of halide, O-, S-, N-, C- and H-nucleophiles and undergo elimination and rearrangement reactions.Kinetic study of the formation and displacement steps has enabled the selection of subs...