Addition of alkynes and osmium carbynes towards functionalized dπ-pπ conjugated systems

碳-碳三键和碳-金属三键是两类高度不饱和的化学键。该工作发现了这两类三键之间的全新反应模式。利用该反应能把金属和有机π共轭体系有效结合，得到一类金属d轨道参与π共轭的全新大π共轭体系。化学化工学院夏海平教授课题组碳龙化学研究取得新进展，利用金属卡拜与炔烃的新反应，成功地合成了一类金属d轨道参与π共轭的全新共轭体系并在有机太阳能电池领域得到应用。该工作是在夏海平教授和南方科技大学何凤副教授共同指导下完成的。化学化工学院2016级iChEM博士生陈仕焰和南科大博士生刘龙珠为论文的共同第一作者。该工作充分体现了多学科协同创新研究优势：相关化合物合成、表征由陈仕焰、高翔、彭丽霞、张颖等完成；光电测试由刘龙珠完成；理论计算由陈仕焰、华煜晖完成。化学化工学院杨柳林副教授、谭元植教授等对研究工作给予了大力支持。【Abstract】The metal-carbon triple bonds and carbon-carbon triple bonds are both highly unsaturated bonds. As a result, their reactions tend to afford cycloaddition intermediates or products. Herein, we report a reaction of M≡C and C≡C bonds that affords acyclic addition products. These newly discovered reactions are highly efficient, regio- and stereospecific, with good functional group tolerance, and are robust under air at room temperature. The isotope labeling NMR experiments and theoretical calculations reveal the reaction mechanism. Employing these reactions, functionalized dπ-pπ conjugated systems can be easily constructed and modified. The resulting dπ-pπ conjugated systems were found to be good electron transport layer materials in organic solar cells, with power conversion efficiency up to 16.28% based on the PM6: Y6 non-fullerene system. This work provides a facile, efficient methodology for the preparation of dπ-pπ conjugated systems for use in functional materials.This research was supported by the National Natural Science Foundation of China (Nos. U1705254, 21931002, and 21975115), Guangdong Provincial Key Laboratory of Catalysis (No. 2020B121201002), Shenzhen Nobel Prize Scientists Laboratory Project (no.C17783101), and the National Key R&D Program of China (2017YFA0204902). We thank the SUSTech Core Research Facilities for the Holiba-UVISEL measurements. 研究工作得到了国家自然科学基金(U1705254、21931002、21975115)，广东省催化化学重点实验室(No. 2020B121201002)，国家重点研发计划(2017YFA0204902)，及深圳诺贝尔奖科学家实验室(C17783101)等项目资助

一种新型靶向性抗肿瘤药物及其制备方法与应用

物理化学带填

葡萄糖醛酸转移酶UGT1A3的特异性探针底物及其应用

带填

生殖毒性替代试验在中药安全性评价中的应用研究进展

中药应用历史悠久，而多数中药，即使是毒性中药，在应用于人体之前并未进行严格的生殖毒性评价。随着中药新药研发工作的全力推进，中药生殖毒性应得到充分重视。体外替代试验是生殖毒性常规评价试验的一种补充，在药物研发的早期阶段能有效降低研发风险，减少研发费用，缩短研发时间，并预警早期毒性。小鼠胚胎干细胞试验、大鼠胚胎细胞微团培养和全胚胎培养试验为欧洲替代方法验证中心验证并推荐的方法，斑马鱼胚胎发育毒性模型是近年来研究并验证的替代试验。近年来，上述试验陆续有在中药生殖毒性研究中应用的报道。根据中药的特点，采用系列替代模型组合策略能更准确预测受试中药的毒性。替代试验优势明显，而中药生殖毒性的评价又需要快捷有效的方法，相信在不久的将来，替代试验将在中药生殖毒性评价中发挥不可或缺的作用。The application of traditional Chinese medicines (TCMs) has a long history. However, most of TCMs, even "toxic medicines", have not had their safety evaluated before being applied to humans. With the development of new TCMs, the reproductive toxicity deserves more attention. Repro¬ductive toxicity in vitro alternative tests can filter drug toxicity rapidly, which is a supplement to the rou¬tine evaluation test of reproductive toxicity. In the early stage, alternative tests can effectively reduce the risk and cost of drug research and development, shorten the cycle of development and warn early toxicity. The reproductive toxicity alternative tests validated and recommended by the European Centre for the Validation of Alternative Method (ECVAM) include the embryonic stem cell test (EST), the rat embryonic cell micromass culture (MM) test and whole embryo culture (WEC) test. The zebrafish embryo model is considered a new developmental toxicity alternative model. In recent years, the tests men¬tioned above have been applied in the evaluation of reproductive toxicity of TCMs. According to the characteristics and application of TCMs, integrated testing strategies from various alternative tests can help to predict reproductive toxicity accurately. The advantages of alternative tests are obvious, and the evaluation of reproductive toxicity of TCMs needs to be done quickly. It is believed that in the near future, alternative tests will play an indispensable role in the evaluation of reproductive toxicity of TCMs. © 2021 Chinese Journal of Pharmacology and Toxicology. All rights reserved