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Total synthesis/semi-synthesis of natural isopentenyl flavonoids with inhibitory activity on NLRP3 inflammasome
Bioorg Med Chem Lett. 2024 Apr 29:129777. doi: 10.1016/j.bmcl.2024.129777. Online ahead of print.ABSTRACTInflammation is the body's defense response to stimuli. When the homeostatic balance is disturbed, disease may result. Flavonoids have clear anti-inflammatory effects and the isopentenyl group significantly enhances the pharmacological activity of flavonoids. Therefore, isopentenyl flavonoids have the potential to serve as lead compounds for the development of anti-inflammatory drugs. Throughout this research, eight natural compounds were synthesized, including 5,7-dihydroxy-4'-methoxy-8-prenylflavonoid (1), 4'-O-Methyl...
Source: Bioorganic and Medicinal Chemistry Letters - May 1, 2024 Category: Chemistry Authors: Yingjie Hu Mengjun Su Yichao Kong Caihong Jiang Yaxia Yuan Xiabin Chen Lei Ma Source Type: research

Design, synthesis and structure-activity relationship of 1,8-naphthalimide derivatives as highly potent hCYP1B1 inhibitors
This study aimed to develop novel efficacious hCYP1B1 inhibitors that worked well in living cells but without AhR agonist effects. For these purposes, a series of 1,8-naphthalimide derivatives were designed and synthesized, and their structure-activity relationships (SAR) as hCYP1B1 inhibitors were analyzed. Following three rounds SAR studies, several potent hCYP1B1 inhibitors were discovered, among which compound 3n was selected for further investigations owing to its extremely potent anti-hCYP1B1 activity (IC50 = 0.040 nM) and its blocking AhR transcription activity in living cells. Inhibition kinetic analyses showed tha...
Source: Bioorganic and Medicinal Chemistry Letters - May 1, 2024 Category: Chemistry Authors: Yueyue Wei Yuan Xiong Qingyi Liao Ya Yang Tian Tian Xiqian Guo Sanfeng Dong Jianming Zhu Yong Zhang Bo Li Zhijian Xu Weiliang Zhu Guangbo Ge Source Type: research

Synthesis and cytotoxicity of novel 6,8,9-trisubstituted purine analogs against liver cancer cells
Bioorg Med Chem Lett. 2024 Apr 28;106:129775. doi: 10.1016/j.bmcl.2024.129775. Online ahead of print.ABSTRACTA series of novel 6-(substituted phenyl piperazine)-8-(4-substituted phenyl)-9-cyclopentyl purines, 10-51, were synthesized by a four-step synthesis, achieving an overall yield of about 43 %. The reaction conditions were effectively optimized, and the final products were obtained with high purity and yield in all synthesis steps. The synthesized nucleobases were evaluated for their in vitro cytotoxic activities on selected human cancer cell lines (HUH7 (liver), HCT116 (colon), and MCF7 (breast)) using the Sulforhoda...
Source: Bioorganic and Medicinal Chemistry Letters - April 30, 2024 Category: Chemistry Authors: M Fatih Polat Irem Durmaz Şahin P ınar Kul Rengul Cetin Atalay Meral Tuncbilek Source Type: research

Fluorescence biosensor to detect microRNAs via integrating DNA hairpins transition mediated strand displacement amplification with primer exchange reaction
Bioorg Med Chem Lett. 2024 Apr 28;106:129774. doi: 10.1016/j.bmcl.2024.129774. Online ahead of print.ABSTRACTHerein, we constructed a fluorescence biosensor for the ultra-sensitive analysis of microRNAs (miRNAs) by combining DNA hairpins transition triggered strand displacement amplification (DHT-SDA) with primer exchange reaction (PER). Target miRNA initiated DHT-SDA to facilitate the generation of multiple single-stranded DNA (ssDNA) as PER primer, which was extended into a long ssDNA. The biosensor is successfully utilized in detecting miRNAs with high sensitivity (limit of detection for miRNA-21 was 58 fM) and a good l...
Source: Bioorganic and Medicinal Chemistry Letters - April 30, 2024 Category: Chemistry Authors: Xiaoyu Liu Shengjun Bu Hongyu Zhou Yao Xu Zhuo Hao Zehong Li Jiayu Wan Source Type: research

Synthesis and cytotoxicity of novel 6,8,9-Trisubstituted purine analogs against liver cancer cells
Bioorg Med Chem Lett. 2024 Apr 28:129775. doi: 10.1016/j.bmcl.2024.129775. Online ahead of print.ABSTRACTA series of novel 6-(substituted phenyl piperazine)-8-(4-substituted phenyl)-9-cyclopentyl purines, 10-51, were synthesized by a four-step synthesis, achieving an overall yield of about 43 %. The reaction conditions were effectively optimized, and the final products were obtained with high purity and yield in all synthesis steps. The synthesized nucleobases were evaluated for their in vitro cytotoxic activities on selected human cancer cell lines (HUH7 (liver), HCT116 (colon), and MCF7 (breast)) using the Sulforhodamine...
Source: Bioorganic and Medicinal Chemistry Letters - April 30, 2024 Category: Chemistry Authors: M Fatih Polat Irem Durmaz Şahin P ınar Kul Rengul Cetin Atalay Meral Tuncbilek Source Type: research

Fluorescence biosensor to detect microRNAs via integrating DNA hairpins transition mediated strand displacement amplification with primer exchange reaction
Bioorg Med Chem Lett. 2024 Apr 28:129774. doi: 10.1016/j.bmcl.2024.129774. Online ahead of print.ABSTRACTHerein, we constructed a fluorescence biosensor for the ultra-sensitive analysis of microRNAs (miRNAs) by combining DNA hairpins transition triggered strand displacement amplification (DHT-SDA) with primer exchange reaction (PER). Target miRNA initiated DHT-SDA to facilitate the generation of multiple single-stranded DNA (ssDNA) as PER primer, which was extended into a long ssDNA. The biosensor is successfully utilized in detecting miRNAs with high sensitivity (limit of detection for miRNA-21 was 58 fM) and a good linea...
Source: Bioorganic and Medicinal Chemistry Letters - April 30, 2024 Category: Chemistry Authors: Xiaoyu Liu Shengjun Bu Hongyu Zhou Yao Xu Zhuo Hao Zehong Li Jiayu Wan Source Type: research

Synthesis of a new 2-prenylated quinoline as potential drug for metabolic syndrome with pan-PPAR activity and anti-inflammatory effects
Bioorg Med Chem Lett. 2024 Apr 26;106:129770. doi: 10.1016/j.bmcl.2024.129770. Online ahead of print.ABSTRACTWe have previously reported the total synthesis and structure-activity relationships (SAR) of 2-prenylated benzopyrans with PPAR agonist activity. Herein, we have described the synthesis and PPAR activity of 2-prenylated benzopyrans and 2-prenylated quinolines. The benzopyran nucleus was generated via enamine-catalyzed Kabbe condensation, and the quinoline nucleus via Friedländer condensation. Results demonstrated that both benzopyran (5a) and quinoline (4b) derivatives bearing a γ,δ-unsaturated ester displayed a...
Source: Bioorganic and Medicinal Chemistry Letters - April 27, 2024 Category: Chemistry Authors: Carlos Villarroel-Vicente Ainhoa Garc ía Khamis Zibar Mar ía Ayelén Schiel Jordi Ferri Nathalie Hennuyer Ricardo D Enriz Bart Staels Diego Cortes Nuria Cabedo Source Type: research

Preparation and bioevaluation of a novel < sup > 99m < /sup > Tc-labelled propylene amine oxime (PnAO) containing two 4-methyl-2-nitroimidazole groups as a promising tumor hypoxia imaging agent
Bioorg Med Chem Lett. 2024 Apr 25;106:129773. doi: 10.1016/j.bmcl.2024.129773. Online ahead of print.ABSTRACTHypoxia is a common phenomenon in solid tumors, and its presence inhibits the efficacy of tumor chemotherapy and radiotherapy. Accurate measurement of hypoxia before tumor treatment is essential. Three propylene amine oxime (PnAO) derivatives with different substituents attached to 2-nitroimidazole were synthesized in the work, they are 3,3,9,9-tetramethyl-1,11-bis(4-bromo-2-nitro-1H-imidazol-1-yl)-4,8-diazaundecane-2,10-dione dioxime (Br2P2), 3,3,9,9-tetramethyl-1,11-bis(4-methyl-2-nitro-1H-imidazol-1-yl)-4,8-diaza...
Source: Bioorganic and Medicinal Chemistry Letters - April 27, 2024 Category: Chemistry Authors: Shuo Li Taiwei Chu Source Type: research

Synthesis of a new 2-prenylated quinoline as potential drug for metabolic syndrome with pan-PPAR activity and anti-inflammatory effects
Bioorg Med Chem Lett. 2024 Apr 25:129770. doi: 10.1016/j.bmcl.2024.129770. Online ahead of print.ABSTRACTWe have previously reported the total synthesis and structure-activity relationships (SAR) of 2-prenylated benzopyrans with PPAR agonist activity. Herein, we have described the synthesis and PPAR activity of 2-prenylated benzopyrans and 2-prenylated quinolines. The benzopyran nucleus was generated via enamine-catalyzed Kabbe condensation, and the quinoline nucleus via Friedländer condensation. Results demonstrated that both benzopyran (5a) and quinoline (4b) derivatives bearing a γ,δ-unsaturated ester displayed a pan...
Source: Bioorganic and Medicinal Chemistry Letters - April 27, 2024 Category: Chemistry Authors: Carlos Villarroel-Vicente Ainhoa Garc ía Khamis Zibar Mar ía Ayelén Schield Jordi Ferri Nathalie Hennuyer Ricardo D Enriz Bart Staels Diego Cortes Nuria Cabedo Source Type: research

Preparation and bioevaluation of a novel < sup > 99m < /sup > Tc-labelled propylene amine oxime (PnAO) containing two 4-methyl-2-nitroimidazole groups as a promising tumor hypoxia imaging agent
Bioorg Med Chem Lett. 2024 Apr 25:129773. doi: 10.1016/j.bmcl.2024.129773. Online ahead of print.ABSTRACTHypoxia is a common phenomenon in solid tumors, and its presence inhibits the efficacy of tumor chemotherapy and radiotherapy. Accurate measurement of hypoxia before tumor treatment is essential. Three propylene amine oxime (PnAO) derivatives with different substituents attached to 2-nitroimidazole were synthesized in the work, they are 3,3,9,9-tetramethyl-1,11-bis(4-bromo-2-nitro-1H-imidazol-1-yl)-4,8-diazaundecane-2,10-dione dioxime (Br2P2), 3,3,9,9-tetramethyl-1,11-bis(4-methyl-2-nitro-1H-imidazol-1-yl)-4,8-diazaunde...
Source: Bioorganic and Medicinal Chemistry Letters - April 27, 2024 Category: Chemistry Authors: Shuo Li Taiwei Chu Source Type: research

Discovery and preclinical evaluations of TQB3616, a novel CDK4-biased inhibitor
Bioorg Med Chem Lett. 2024 Apr 24:129769. doi: 10.1016/j.bmcl.2024.129769. Online ahead of print.ABSTRACTAmong small-molecule CDK4/6 inhibitors (palbociclib, ribociclib, and abemaciclib) approved for metastatic breast cancers, abemaciclib has a more tolerable adverse effects in clinic. This is attributable to preferential inhibition of CDK4 over CDK6. In our search for a biased CDK4 inhibitor, we discovered a series of pyrimidine-indazole inhibitors. SAR studies led us to TQB3616 as a preferential CDK4 inhibitor. TQB3616 exhibited improvements in both enzymatic and cellular proliferation inhibitory potency when tested side...
Source: Bioorganic and Medicinal Chemistry Letters - April 26, 2024 Category: Chemistry Authors: Zhaobing Xu Yingchun Liu Baohui Song Bingjie Ren Xiongbin Xu Ruibin Lin Xiaoyu Zhu Chen Chen Shuqun Yang Yusong Zhu Wen Jiang Wei Li Yuanfeng Xia Lihong Hu Shuhui Chen Chi-Chung Chan Jian Li Xiquan Zhang Ling Yang Xin Tian Charles Z Ding Source Type: research

The association between oxidized low-density lipoprotein and cancer: An emerging targeted therapeutic approach?
Bioorg Med Chem Lett. 2024 Apr 20:129762. doi: 10.1016/j.bmcl.2024.129762. Online ahead of print.ABSTRACTLipids play an important role in varying vital cellular processes including cell growth and division. Elevated levels of low-density lipoprotein (LDL) and oxidized-LDL (ox-LDL), and overexpression of the corresponding receptors including LDL receptor (LDLR), lectin-like oxidized low-density lipoprotein receptor-1 (LOX-1), and cluster of differentiation 36 (CD36), have shown strong correlations with different facets of carcinogenesis including proliferation, invasion, and angiogenesis. Furthermore, a high serum level of ...
Source: Bioorganic and Medicinal Chemistry Letters - April 22, 2024 Category: Chemistry Authors: Samin Ghorbani Moghadam Mehrshad Ebrahim Pour Seyedeh Hoda Alavizadeh Prashant Kesharwani Amirhossein Sahebkar Source Type: research