Ferulic acid-carbazole hybrid compounds: Combination of cholinesterase inhibition, antioxidant and neuroprotection as multifunctional anti-Alzheimer agents.

In order to search for novel multifunctional anti-Alzheimer agents, a series of ferulic acid-carbazole hybrid compounds were designed and synthesized. Ellman's assay revealed that the hybrid compounds showed moderate to potent inhibitory activity against the cholinesterases. Particularly, the AChE inhibition potency of compound 5k (IC50 1.

Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents.

Facing the multifactorial nature of Alzheimer's disease, twelve dibenzofuran/carbazole derivatives, which can be considered as the D-ring opened analogs of galantamine, have been designed and synthesized as multifunctional anti-Alzheimer agents. In vitro tests revealed that compounds 3 and 5, which bear a nitrate moiety in the molecule, showed a potent inhibition activity towards AChE and compound 3 showed a good Aβ42 aggregation inhibitory activity. Moreover, 3 and 5 could also release a relative low concentration of NO in vitro and they did not show toxicity to neuronal cells, while exerted a neuroprotective effect against the Aβ-induced toxicity.

Synthesis and anticancer activity of some novel 2-phenazinamine derivatives.

In this study, we report the synthesis and spectral characterization of a novel series of 2-phenazinamine derivatives. In vitro evaluation for their anticancer activity toward cultured K562 (human chronic myelogenous leukemia), HepG2 (human hepatocellular carcinoma), MGC803 (human gastric carcinoma), HCT116 (human colorectal carcinoma), MCF7 (human breast adenocarcinoma) cell lines, as well as 293T (epithelial cells from human embryo kidney) non-cancer cell was carried out. The compounds 4, 7, 16 and 19 showed good positive anticancer activity in vitro.

Design and synthesis of dimethylaminomethyl-substituted curcumin derivatives/analogues: potent antitumor and antioxidant activity, improved stability and aqueous solubility compared with curcumin.

A series of dimethylaminomethyl-substituted curcumin derivatives/analogues were designed and synthesized. All compounds effectively inhibited HepG2, SGC-7901, A549 and HCT-116 tumor cell lines proliferation in MTT assay. Particularly, compounds 2a and 3d showed much better activity than curcumin against all of the four tumor cell lines.

Current progresses of novel natural products and their derivatives/ analogs as anti-Alzheimer candidates: an update.

Alzheimer's disease (AD) is one of the most threatening diseases affecting the aged with high incidence. Though AD has been defined for more than 100 years, it is still incurable. The drugs clinically used for the treatment of this disease, such as acetylcholinesterase inhibitors (AChEIs) and N-methyl-D-aspartate (NMDA) receptor antagonist, can only provide a limited therapeutic effect.

6-Meth-oxy-2-methyl-1-m-tolyl-1H-benzimidazole hemihydrate.

The title compound, C(16)H(16)N(2)O·0.5H(2)O, is a substituted 1-phenyl-benzimidazole, which belongs to the class of ATP-site inhibitors of the platelet-derived growth-factor receptor. In the crystal, the components are linked by an O-H⋯N hydrogen bond.

(3aR*,7aS*)-1-(p-Tolyl-sulfon-yl)perhydro-indol-2-one.

In the racemic title compound, C(15)H(19)NO(3)S, the dihedral angle between the planes of the benzene ring and the O=S=O group is 56.92 (7)° and the cyclo-hexane ring adopts a chair conformation.