A convenient and efficient Ni-catalyzed reaction has been developed for synthesis of mono-substituted o-carboranes, involving cross-coupling of readily available and sterically hindered 1-bromomethyl-o-carborane with various alkyl and aryl Grignard reagents under mild conditions, and the corresp...

The water-soluble titanium-oxide structures covered in this review span a continuum from molecular clusters to colloidal nanocrystals. Here, a deliberate distinction is made between titanium clusters and nanoparticles with organic ligands, soluble in organic solvents, and related structures prep...

Recent zircon supply disruptions and the increasing demand for TiO2 in pigments has focused attention on the adequacy of known and anticipated resources, and the ability of current suppliers to meet future demand. Additionally, there is now a greater focus on the environmental impact of sulfate-...

This study explored the efficacy and efficiency of a simultaneous UV-catalyzed oxidation–coagulation process of titanium sulfate (UV/Ti(SO4)2) for efficient removal of As(III) from water. It revealed that, As(III) could be oxidized to As(V) during the UV catalyzed coagulation of Ti(SO4)2 with h...

Despite its natural abundance and widespread use as food, paint additive, and in bone implants, no specific biological function of titanium is known in the human body. High concentrations of Ti(IV) could result in cellular toxicity, however, the absence of Ti toxicity in the blood of patients wi...

A convenient gold-catalyzed asymmetric synthesis of polysubstituted furfurylamines starting from amino acids has been achieved. The cyclization proceeded under mild conditions and generally provided the furan or iodofuran derivatives in good to excellent yields and with high enantiomeric excess....

A screening program aimed at discovering novel anticancer agents based on natural products led to the selection of koningic acid (KA), known as a potent inhibitor of glycolysis. A method was set up to produce this fungal sesquiterpene lactone in large quantities by fermentation, thus allowing (i...

A series of 9-benzylamino acridine derivatives were synthesized as an extension of our discovery of acridine antitumor agents. Most of these acridine compounds displayed good antiproliferative activity with IC50 values in low micromole range and structure-activity relationships were studied. Top...

A straightforward route for preparing derivatives of ethyl 5-trichloromethyl-1,2,4-oxadiazole-3-carboxylate, in which the 5-trichloromethyl and/or the ester functionalities are displaced by various nucleophiles, has been designed. Mild reaction conditions were chosen to enable the formation of p...

A series of benzyl-[3-(benzylamino-methyl)-cyclohexylmethyl]-amine derivatives with different substitution pattern on the aromatic ring have been prepared and evaluated for their antibacterial activity against Gram-positive and Gram-negative bacterial strains. Most of the compounds exhibit poten...

We synthesized 47 kinds of 3-amino- or 3-benzylamino-β-carboline derivatives with a substituent on the 6-, 8-, or 6,8-carbon atoms and evaluated their antitumor activities for Hela S-3 and Sarcoma 180 cell lines using a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Consequ...

Despite the wide use of 1,2,4,5- tetrazines in biomaterials and materials science, currently there does not exist synthetic method(s) that can yield significant amount of 1,2,4,5- tetrazines without the use of potentially toxic metal catalysts. Here, we report a less energy intensive and more ef...

Pursuing our chemical and biological studies in this field, we described the multistep preparation of the new 5-, 6-, or 7-alkoxy and 7-alkoxy-8-methyl substituted 4-(1-piperazinyl)coumarins 5d-v, as well as the in vitro evaluation of their inhibitory activity on human platelet aggregation induc...

A series of 1-Sulfonyl-6-Piperazinyl-7-Azaindoles, showing strong antagonistic activity to 5-HT6 receptor (5-HT6R) was synthesized and characterized. The series was optimized to reduce activity on D2 receptor. Based on the selectivity against this off-target and the analysis of the ADME-tox prof...

BTK and PI3Kδ play crucial roles in the progression of leukemia, and studies confirmed that the dual inhibition against BTK and PI3Kδ could provide superior anticancer agents to single targeted therapies. Herein, a new series of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives were optimize...

5-{2-[4-(2-Methyl-5-quinolinyl)-1-piperazinyl]ethyl}-2(1H)-quinolinones and 3,4-dihydro-2(1H)-quinolinones have been identified with different combinations of 5-HT1 autoreceptor antagonist and hSerT potencies and excellent rat PK profiles. The availability of tool compounds with a range of profi...

New 2-(1-Piperazinyl)- and 2-(hexahydro-1H-1,4-diazepin-1-yl)benzothiazoles were prepared and tested as H1- and H3-receptor antagonists. A number of compounds showed weak H1-antagonistic activity, with pA2 values ranging from 5.5 to 6.1. The simple alkyl substituted, 2-[1-(4-methyl and 4-ethyl)p...

Btk inhibitors and PI3Kδ inhibitors play crucial roles in the treatment of leukemia, and studies confirmed that the synergetic inhibition against Btk and PI3Kδ could gain an optimal response. Herein, a series of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives were designed and synthesized ...

A series of novel dispiro piperazinyl-quinolinyl-thioxothiazolidin-2, 4-dione derivatives were synthesised and characterised by FT-IR 1H, 13C, 2D NMR and HRMS spectroscopic techniques. A representative compound 1'-(2-(4-methylpiperazin-1-yl)quinolin-3-yl)-2″-thioxo-5′,6′,7′,7a'-tet...

The multistep preparation of the new 10-substituted 2-(1-piperazinyl)pyrimido[1,2-a]benzimidazol-4(10H)-ones 6a–o, and of the two isomers 10-ethyl-2-(diethylamino)pyrimido[1,2-a]benzimidazol-4(10H)-one 6p and 10-ethyl-4-(diethylamino)pyrimido[1,2-a]benzimidazol-2(10H)-one 13, as well as the in ...