No abstract

A series of novel 2-aryl-benzimidazole derivatives of dehydroabietic acid were synthesized. Among them, compound 6j was found to be a potent tubulin polymerization inhibitor.

Flavonoids are secondary metabolites of plants. In general，most flavonoids are combined with glucosides and have extremely complex molecular structures. In the nature，these flavonoids have a variety of biological activities，such as anti-oxidation，anti-virus，anti-tumor，scavenging free radicals and so on，however，due to poor solubility and stability of flavonoids，their bioavailability is limited. The method of drug design is used to modify the structure of flavonoids to give them special functions. At present, flavonoids have broad application prospects in the treatment of tumors. It has inhibited the proliferation, migration, invasion, angiogenesis and multi-drug resistance of tumors and has become a research hotspot.

Chemical space is defined as all possible small organic molecules, including those present in biological systems, which is so vast that so far only a tiny fraction of it has been explored. Indeed, a thorough examination of all "chemical space" is practically impossible. The success of three EGFR inhibitors (Gefitnib, Erlotinib, Lapatinib) suggests that 4-anilinoquinazoline scaffold is still worth developing in the future. To date hundreds of this sort of derivatives have been synthesized and show potent anticancer activities. Most of the compounds have been proved to be EGFR/HER2 kinase inhibitors, binding at the hinge region of the ATP site and some lead compounds have been optimized against a number of different kinases, including VEGFR-2, Src, Aurora A/B, Tpl, Clk and PDE10A. Now there is now a rich pipeline of novel anticancer agents based on 4-anilinoquinazoline in early phase clinical trials. This review will highlight the exploration of chemical space of 4-anilinoquinazoline in the past ten years and we hope that increasing knowledge of the SAR and cellular processes underlying the antitumor-activity of anilinoquinazoline derivatives will be beneficial to the rational design of new generation of small molecule anticancer drugs.

Flexible artificial skin sensors have been a hot research topic over the past 20 years due to their remarkable prospects in the fabrication of smart wearable devices. Normally, electronic skin sensors transmit signals via stretchy electrical conductors, and the manufacturing processes are more complicated, involving multiple steps. For the first time, this work reports a facile one-step fabrication of poly(sodium methacrylate-covinylimidazole)-Co 2+ hydrogels with high mechanical strength, good elasticity, and excellent sensitivity that can be used as ionic skins (I-skins). In addition, mechanical analysis indicates that the designed hydrogels have enhanced strain and tensile strength due to hydrogen bonding and metal−ligand bonding interactions, and these two types of dynamic noncovalent interactions are explored in detail. Simultaneously, the developed hydrogels also display superior conductivity and self-healing qualities with restored sensing properties. Furthermore, the proposed hydrogel with good sensitivity and stable strain range is suitable to fabricate a wearable strain sensor, and this hydrogel sensor was demonstrated to be effective in monitoring human motion, including joint flexion, pulse, vocal cord vibration, and respiration. In addition, a pressure distribution sensor array was developed by this hydrogel and was used to construct the model of plantar pressure distribution in normal subjects and flatfoot patients, offering a strategy for the early detection and clinical diagnosis of numerous foot-related disorders. Hence, this research may offer a promising approach for generating biocompatible hydrogels with integrated mechanical characteristics, and these hydrogels present development potentials in multifunctional ionic skins.