The study delves into the binding properties of acridine-9-amine and its selected, mainly N-substituted derivatives (A9As), with calf thymus deoxyribonucleic acid (CT-DNA). This investigation, conducted using UV-Vis spectrophotometry, steady-state fluorescence spectroscopy and isothermal titration calorimetry, provides insights into the relationship between their structure and activity. The absorption spectra of the A9As exhibited a slight red shift and significant hypochromic effects, while the fluorescence emission intensities decreased in the presence of CT-DNA. These results suggest that all fluorescent substrates intercalate into the double helix of native DNA to varying degrees. The binding constants for the A9As/CT-DNA complexes (log(K_A) were determined using various techniques in the range from 2.59 to 5.50). The thermodynamic parameters of A9As binding to DNA were obtained from ITC measurements (ΔG from - 7.51 to - 6.75 kcal·mol^-1, ΔH from - 11.58 to - 3.83 kcal·mol^-1, and TΔS from - 4.83 to 3.68 kcal·mol^-1) and indicated that the formation of all the investigated A9As-DNA complexes is an enthalpy-driven process. The study also discusses the influence of the emitters' structure and electronic properties of substituents on intercalation efficiency. This knowledge serves as a guide for further research and offers directions for functionalising new acridines as potential reagents. It also provides the latest information on the ability of intercalation to DNA, which can be instrumental in studies on the mechanism of binding small aromatic molecules to DNA and can potentially contribute to new anticancer drug designs.

2025-01-23·Energy & Fuels

Molecular Design of Bipolar Redox-Active Molecules with Extended p–n Fusion for Symmetric Redox Flow Batteries

作者: Lu, Zonglong ; Wu, Tingting ; Feng, Shunan ; Cao, Yunjie ; Dai, Gaole ; He, Wei ; Liu, Yue ; Zhao, Yu ; Li, Qin ; Chen, Limiao

Most nonaqueous redox flow batteries (RFBs) encounter the issue of irreversible capacity loss due to the crossover of redox-active materials.To mitigate this, an innovative approach is to construct sym. RFBs with bipolar redox-active mols. (BRMs).Merging established p- and n-type redox-active moieties within a single mol. through fused conjugation has proven to be a practical and effective strategy for the preparation of BRMs.Nonetheless, this strategy presents significant challenges, primarily involving the destabilization of redox intermediates caused by direct and excessive electronic perturbation as well as the inherently deleterious interactions between the two types of redox-active centers.This study proposes a robust design strategy for BRMs that incorporate addnl. p- and n-type redox moieties within the same conjugated structure to enhance redox stability.As a demonstrator, we designed and synthesized a novel class of BRMs, merging two sets of pyrrolic nitrogen and ketone redox-active moieties.The potential and efficacy of these mols. as BRMs for RFBs were evaluated in static cells as a proof of concept.A sym. static cell based on one of these mols. achieves a cell voltage of 2.6 V and demonstrates satisfactory Coulombic and energy efficiencies as well as capacity retention over long-term charge-discharge cycles.Our study provides innovative structures and an effective strategy for developing high-performance BRMs.

2025-01-17·Organic Letters

Metal- and Light-Free Decarboxylative Giese Addition Reaction Facilitated by Hantzsch Ester

Article

作者: Niu, Hong-Ying ; Yuan, Shuai ; Wang, Jing ; Deng, Xiao-Shan ; Jia, Ming ; Wang, Song-Lin ; Zhu, Xing-Yu ; Zhang, Yong ; Guo, Hai-Ming ; Liang, Lei

We have developed a novel strategy for decarboxylative radical addition reactions that employs ground-state reduced nicotinamide adenine dinucleotide (NADH) analogues under ambient and open-air conditions, facilitating the efficient formation of Csp³-Csp³ bonds in a variety of substrates. This protocol is distinguished by its operational simplicity, mild reaction conditions, high efficiency, and the use of cost-effective starting materials. Furthermore, experimental studies have provided valuable insights into the reaction mechanism, elucidating the light-independent pathways that promote these transformations.

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适应症	最高研发状态	国家/地区	公司	日期
实体瘤	临床3期	-	Jubilant Biosys Ltd.	2020-08-02
实体瘤	临床3期	美国	Checkpoint Therapeutics, Inc.	2020-08-02
肿瘤	临床申请	美国	Jubilant Therapeutics, Inc.初创企业	2024-06-15