Discovery of novel biphenyl-sulfonamide analogues as NLRP3 inflammasome inhibitors
Bioorg Chem. 2024 Mar 9;146:107263. doi: 10.1016/j.bioorg.2024.107263. Online ahead of print.ABSTRACTThe aberrant activation of NLRP3 inflammasome has been observed in various human diseases. Targeting the NLRP3 protein with small molecule inhibitors shows immense potential as an effective strategy for disease intervention. Herein, a series of novel biphenyl-sulfonamide NLRP3 inflammasome inhibitors were designed and synthesized. The representative compound H28 was identified as potent and specific NLRP3 inflammasome inhibitor with IC50 values of 0.57 μM. Preliminary mechanistic studies have revealed that compound H28 exh...
Source: Bioorganic Chemistry - March 16, 2024 Category: Chemistry Authors: Chao Huang Jinyu Liu Yuxin Chen Simin Sun Tongtong Kang Yuqi Jiang Xiaoyang Li Source Type: research
Engineering an (R)-selective transaminase for asymmetric synthesis of (R)-3-aminobutanol
This study provides a basis for the rational design of an active to creating variants that can accommodate novel substrates.PMID:38492494 | DOI:10.1016/j.bioorg.2024.107264 (Source: Bioorganic Chemistry)
Source: Bioorganic Chemistry - March 16, 2024 Category: Chemistry Authors: He Liu Shixi Wang Meng Xu Kaiyue Zhang Qian Gao Hualei Wang Dongzhi Wei Source Type: research
Discovery of novel biphenyl-sulfonamide analogues as NLRP3 inflammasome inhibitors
Bioorg Chem. 2024 Mar 9;146:107263. doi: 10.1016/j.bioorg.2024.107263. Online ahead of print.ABSTRACTThe aberrant activation of NLRP3 inflammasome has been observed in various human diseases. Targeting the NLRP3 protein with small molecule inhibitors shows immense potential as an effective strategy for disease intervention. Herein, a series of novel biphenyl-sulfonamide NLRP3 inflammasome inhibitors were designed and synthesized. The representative compound H28 was identified as potent and specific NLRP3 inflammasome inhibitor with IC50 values of 0.57 μM. Preliminary mechanistic studies have revealed that compound H28 exh...
Source: Bioorganic Chemistry - March 16, 2024 Category: Chemistry Authors: Chao Huang Jinyu Liu Yuxin Chen Simin Sun Tongtong Kang Yuqi Jiang Xiaoyang Li Source Type: research
Engineering an (R)-selective transaminase for asymmetric synthesis of (R)-3-aminobutanol
This study provides a basis for the rational design of an active to creating variants that can accommodate novel substrates.PMID:38492494 | DOI:10.1016/j.bioorg.2024.107264 (Source: Bioorganic Chemistry)
Source: Bioorganic Chemistry - March 16, 2024 Category: Chemistry Authors: He Liu Shixi Wang Meng Xu Kaiyue Zhang Qian Gao Hualei Wang Dongzhi Wei Source Type: research
Recent development of VEGFR small molecule inhibitors as anticancer agents: A patent review (2021-2023)
Bioorg Chem. 2024 Mar 9;146:107278. doi: 10.1016/j.bioorg.2024.107278. Online ahead of print.ABSTRACTVEGFR, a receptor tyrosine kinase inhibitor (TKI), is an important regulatory factor that promotes angiogenesis and vascular permeability. It plays a significant role in processes such as tumor angiogenesis, tumor cell invasion, and metastasis. VEGFR is mainly composed of three subtypes: VEGFR-1, VEGFR-2, and VEGFR-3. Among them, VEGFR-2 is the crucial signaling receptor for VEGF, which is involved in various pathological and physiological functions. At present, VEGFR-2 is closely related to a variety of cancers, such as no...
Source: Bioorganic Chemistry - March 14, 2024 Category: Chemistry Authors: Jing Zeng Qichuan Deng Zheng Chen Shuang Yan Qin Dong Yuyu Zhang Yuan Cui Ling Li Yuxin He Jianyou Shi Source Type: research
DEFB114 protein enhances host resistance to fungal infection through the NOD1/2-ATG16L1-NF- κB signaling pathway
In this study, a 210 bp long cDNA sequence of yak DEFB114 gene was amplified and successfully expressed in a prokaryotic system. The DEFB114 protein exhibited significant inhibitory effects on the growth of Aspergillus fumigatus in vitro. When co-cultured with yak macrophages, DEFB114 protein enhanced macrophage phagocytic activity and increased nucleic acid fluorescence intensity (P < 0.05). DEFB114 protein also enhanced the activity of yak macrophages stimulated by inactivated Aspergillus fumigatus spores, increased the release of nitric oxide (NO), and promoted the expression of genes such as γ-actin, Lgals, Man2b, ...
Source: Bioorganic Chemistry - March 14, 2024 Category: Chemistry Authors: Jingyun Chen Qundi Mei Li Wang Yong Wei Source Type: research
Indole-based NNN donor Schiff base ligand and its complexes: Sonication-assisted synthesis, characterization, DNA binding, anti-cancer evaluation and in-vitro biological assay
Bioorg Chem. 2024 Mar 11;146:107281. doi: 10.1016/j.bioorg.2024.107281. Online ahead of print.ABSTRACTA novel indole based NNN donor Schiff base ligand and its Ni(II), Zn(II) and Cd(II) complexes have been synthesized using sonication-assisted method which is a highly efficient eco-friendly mechanism. The synthesized complexes have been characterized using elemental analysis, UV-Vis spectroscopy, mass spectrometry, FT-IR, and NMR and are optimized using DFT approach, which provided their theoretical framework. The stoichiometry between the ligand and the metal ions was also determined using Job's method. The thermogravimet...
Source: Bioorganic Chemistry - March 14, 2024 Category: Chemistry Authors: Thangjam Sanjurani Sneha Paul Pranjit Barman Source Type: research
Recent development of VEGFR small molecule inhibitors as anticancer agents: A patent review (2021-2023)
Bioorg Chem. 2024 Mar 9;146:107278. doi: 10.1016/j.bioorg.2024.107278. Online ahead of print.ABSTRACTVEGFR, a receptor tyrosine kinase inhibitor (TKI), is an important regulatory factor that promotes angiogenesis and vascular permeability. It plays a significant role in processes such as tumor angiogenesis, tumor cell invasion, and metastasis. VEGFR is mainly composed of three subtypes: VEGFR-1, VEGFR-2, and VEGFR-3. Among them, VEGFR-2 is the crucial signaling receptor for VEGF, which is involved in various pathological and physiological functions. At present, VEGFR-2 is closely related to a variety of cancers, such as no...
Source: Bioorganic Chemistry - March 14, 2024 Category: Chemistry Authors: Jing Zeng Qichuan Deng Zheng Chen Shuang Yan Qin Dong Yuyu Zhang Yuan Cui Ling Li Yuxin He Jianyou Shi Source Type: research
DEFB114 protein enhances host resistance to fungal infection through the NOD1/2-ATG16L1-NF- κB signaling pathway
In this study, a 210 bp long cDNA sequence of yak DEFB114 gene was amplified and successfully expressed in a prokaryotic system. The DEFB114 protein exhibited significant inhibitory effects on the growth of Aspergillus fumigatus in vitro. When co-cultured with yak macrophages, DEFB114 protein enhanced macrophage phagocytic activity and increased nucleic acid fluorescence intensity (P < 0.05). DEFB114 protein also enhanced the activity of yak macrophages stimulated by inactivated Aspergillus fumigatus spores, increased the release of nitric oxide (NO), and promoted the expression of genes such as γ-actin, Lgals, Man2b, ...
Source: Bioorganic Chemistry - March 14, 2024 Category: Chemistry Authors: Jingyun Chen Qundi Mei Li Wang Yong Wei Source Type: research
Indole-based NNN donor Schiff base ligand and its complexes: Sonication-assisted synthesis, characterization, DNA binding, anti-cancer evaluation and in-vitro biological assay
Bioorg Chem. 2024 Mar 11;146:107281. doi: 10.1016/j.bioorg.2024.107281. Online ahead of print.ABSTRACTA novel indole based NNN donor Schiff base ligand and its Ni(II), Zn(II) and Cd(II) complexes have been synthesized using sonication-assisted method which is a highly efficient eco-friendly mechanism. The synthesized complexes have been characterized using elemental analysis, UV-Vis spectroscopy, mass spectrometry, FT-IR, and NMR and are optimized using DFT approach, which provided their theoretical framework. The stoichiometry between the ligand and the metal ions was also determined using Job's method. The thermogravimet...
Source: Bioorganic Chemistry - March 14, 2024 Category: Chemistry Authors: Thangjam Sanjurani Sneha Paul Pranjit Barman Source Type: research
New diarylcyclopentenone enantiomers and biphenyl derivatives from the fungus Talaromyces adpressus
Bioorg Chem. 2024 Mar 9;146:107280. doi: 10.1016/j.bioorg.2024.107280. Online ahead of print.ABSTRACTTen new compounds, including three pairs of diarylcyclopentenone enantiomers (±) talaromycesins A-C (1-3) and four biphenyl derivatives talaromycesins D-G (4-7), along with four known compounds (8-11), were isolated from the fungus Talaromyces adpressus. Their structures were determined by analyses of extensive NMR spectroscopic and HRESIMS data, and their absolute configurations were elucidated by the dimolybdenum tetraacetate [Mo2(AcO)4]-induced ECD spectra, X-ray crystallographic studies, and ECD calculations. These new...
Source: Bioorganic Chemistry - March 13, 2024 Category: Chemistry Authors: Meijia Zheng Yongqi Li Hong Liao Chenxi Zhou Qin Li Chunmei Chen Weiguang Sun Yonghui Zhang Hucheng Zhu Source Type: research
Novel chiral matrine derivatives as potential antitumor agents: Design, synthesis and biological evaluation
In this study, we designed and synthesized a novel chiral matrine derivative. Their cytotoxicity against three types of tumor cells was assessed. Comparing the newly synthesized derivatives to the parent matrine, most compounds exhibited significantly enhanced inhibitory effects on cancer cells. Among them, Q12 exhibited the highest activity, with IC50 values of 8.31 μM against rat glioma cells C6, 6.3 μM against human liver cancer cells HepG2 and 7.14 μM against human gastric cancer cells HGC-27, meanwhile showing low toxicity. Based on IC50 values, we constructed a preliminary structure-activity relationship (SAR). Co...
Source: Bioorganic Chemistry - March 13, 2024 Category: Chemistry Authors: Gan Qiu Fan Li Jamal A H Kowah Junwei Xie Qingfeng Long Lisheng Wang Xu Liu Source Type: research
New diarylcyclopentenone enantiomers and biphenyl derivatives from the fungus Talaromyces adpressus
Bioorg Chem. 2024 Mar 9;146:107280. doi: 10.1016/j.bioorg.2024.107280. Online ahead of print.ABSTRACTTen new compounds, including three pairs of diarylcyclopentenone enantiomers (±) talaromycesins A-C (1-3) and four biphenyl derivatives talaromycesins D-G (4-7), along with four known compounds (8-11), were isolated from the fungus Talaromyces adpressus. Their structures were determined by analyses of extensive NMR spectroscopic and HRESIMS data, and their absolute configurations were elucidated by the dimolybdenum tetraacetate [Mo2(AcO)4]-induced ECD spectra, X-ray crystallographic studies, and ECD calculations. These new...
Source: Bioorganic Chemistry - March 13, 2024 Category: Chemistry Authors: Meijia Zheng Yongqi Li Hong Liao Chenxi Zhou Qin Li Chunmei Chen Weiguang Sun Yonghui Zhang Hucheng Zhu Source Type: research
Novel chiral matrine derivatives as potential antitumor agents: Design, synthesis and biological evaluation
In this study, we designed and synthesized a novel chiral matrine derivative. Their cytotoxicity against three types of tumor cells was assessed. Comparing the newly synthesized derivatives to the parent matrine, most compounds exhibited significantly enhanced inhibitory effects on cancer cells. Among them, Q12 exhibited the highest activity, with IC50 values of 8.31 μM against rat glioma cells C6, 6.3 μM against human liver cancer cells HepG2 and 7.14 μM against human gastric cancer cells HGC-27, meanwhile showing low toxicity. Based on IC50 values, we constructed a preliminary structure-activity relationship (SAR). Co...
Source: Bioorganic Chemistry - March 13, 2024 Category: Chemistry Authors: Gan Qiu Fan Li Jamal A H Kowah Junwei Xie Qingfeng Long Lisheng Wang Xu Liu Source Type: research
Antimicrobial properties of triazolato terpyridine Pd(II) and Pt(II) complexes formed by [3+2] cycloaddition coupling reaction
Bioorg Chem. 2024 Mar 6;146:107262. doi: 10.1016/j.bioorg.2024.107262. Online ahead of print.ABSTRACTModern classes of antimicrobials are crucial because most drugs in development today are basically antibiotic derivatives. Even though a large number of metal-based compounds have been studied as antimicrobial agents, relatively few studies have examined the antimicrobial properties of Pd(II) and Pt(II) compounds. The [3+2] cycloaddition reactions of [M(N3)L]PF6 (M = Pd(II) and Pt(II); L = 4'-(2-pyridyl)-2,2':6',2″-terpyridine) with 4,4,4-trifluoro-2-butynoic acid ethyl ester gave the corresponding triazolate complexes. T...
Source: Bioorganic Chemistry - March 11, 2024 Category: Chemistry Authors: Ahmed M Mansour Krzysztof Radacki Gamal A E Mostafa Essam A Ali Ola R Shehab Source Type: research
