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Total 18223 results found since Jan 2013.
Iridium(III) complex induces apoptosis in HeLa cells by regulating mitochondrial and PI3K/AKT signaling pathways: In vitro and in vivo experiments
Bioorg Chem. 2023 Sep 16;141:106867. doi: 10.1016/j.bioorg.2023.106867. Online ahead of print.ABSTRACTCyclometalated iridium complexes with mitochondrial targeting show great potential as substitutes for platinum-based complexes because of their strong anti-cancer properties. Three novel cyclometalated iridium(III) compounds were synthesized and evaluated in five different cell lines as part of the ongoing systematic investigations of these compounds. The complexes were prepared using 4,7-dichloro-1,10-phenanthroline ligands. The cytotoxicity of complexes Ir1-Ir3 towards HeLa cells was shown to be high, with IC50 values of...
Source: Bioorganic Chemistry - September 21, 2023 Category: Chemistry Authors: Shu-Fen He Wei-Chao Han Ying-Ying Shao Han-Bin Zhang Wen-Xin Hong Qiu-Hong Yang Yu-Qing Zhang Rui-Rong He Jing Sun Source Type: research
The active phthalate metabolite, DHEP, induces proliferation and metastasis of prostate cancer cells via upregulation of β-catenin and downregulation of KLF7
Bioorg Chem. 2023 Sep 15;141:106864. doi: 10.1016/j.bioorg.2023.106864. Online ahead of print.ABSTRACTPhthalates such as DHEP are among the widely used compounds in industry. It has been shown that DHEP can convey various biological consequences in mammalian cells, among them, the carcinogenic effects of DHEP are emphasized. The present study aimed to assess the impact of DHEP exposure on the proliferation and invasiveness of DU145 prostate cancer cells through in vitro and in vivo models. The DU145 cells were treated with increasing concentrations of DHEP and the tumorigenic parameters were analyzed. KLF7 as a probable me...
Source: Bioorganic Chemistry - September 21, 2023 Category: Chemistry Authors: Hecheng Li Jianping Li Yubo Ma Ziming Wang Zihe Peng Hang Xu Hang Bi Shaik Althaf Hussain Zhaolun Li Source Type: research
Indoloquinazoline alkaloids suppress angiogenesis and inhibit metastasis of melanoma cells
Bioorg Chem. 2023 Sep 18;141:106873. doi: 10.1016/j.bioorg.2023.106873. Online ahead of print.ABSTRACTMetastasis is the leading cause of cancer-related mortality, targeting angiogenesis emerges as a therapeutic strategy for the treatment of melanoma metastasis. Discovery of new antiangiogenic compounds with specific mechanism of action is still desired. In present study, a bioassay-guidance uncovers the EtOAc extract of a marine-derived fungus Aspergillus clavutus LZD32-24 with significant inhibitory activity against the angiogenesis in Tg (fli1a: EGFP) zebrafish model. Extensive chromatographic fractionation led to the is...
Source: Bioorganic Chemistry - September 21, 2023 Category: Chemistry Authors: Xingchen Guo Aili Fan Xinyi Qi Dong Liu Jian Huang Wenhan Lin Source Type: research
Effect of cycloastragenol and punicalagin on Prp(106-126) and A β(25-35) oligomerization and fibrillizaton
In this study, we have examined the effect of two NPs, cycloastragenol (CAG) and punicalagin (PCG), on the metal-induced oligomerization and aggregation of Aβ25-35 and PrP106-126 peptides. The peptide aggregation and inhibitory properties of both NPs were examined by the thioflavin-T (ThT) assay, MALDI-TOF, circular dichroism (CD) spectroscopy, and transmission electron microscopy (TEM). Among the two NPs, PCG significantly binds to the peptides, chelates metal ions (Cu2+ and Zn2+), inhibits peptide aggregation, substantially reduces oxidative stress, and controls the production of reactive oxygen species (ROS). Both NPs ...
Source: Biophysical Chemistry - September 21, 2023 Category: Chemistry Authors: Govinda R Navale Rahul Chauhan Saakshi Saini Partha Roy Kaushik Ghosh Source Type: research
Medicinal Chemistry-driven Approach to Novel 2-Substituted Benzoxazole - Estradiol Chimeras: Synthesis, Anticancer Activity and Early ADME Profile
ChemMedChem. 2023 Sep 20:e202300352. doi: 10.1002/cmdc.202300352. Online ahead of print.ABSTRACTThe efficient synthesis of novel estradiol-based A-ring-fused oxazole derivatives, which can be considered as benzoxazole-steroid domain-integrated hybrids containing a common benzene structural motif, is described. The target compounds were prepared from steroidal 2-aminophenol precursors by heterocycle formation or functional group interconversion (FGI) strategies. According to 2D projection-based t-distributed stochastic neighbor embedding (t-SNE), the novel molecules were proved to represent a new chemical space among steroi...
Source: ChemMedChem - September 20, 2023 Category: Chemistry Authors: Ferenc Kov ács Ildik ó Huliák H édi Árva M ónika Kiricsi D óra Erdős Marianna Kocsis Gergely Tak ács Gy örgy T Balogh Éva Frank Source Type: research
Flower-like porous BCN assembled by nanosheets for paclitaxel delivery
This study presents a novel template method for preparing porous BCN nanomaterials, offering a promising platform for high-performance anticancer drug delivery.PMID:37727129 | DOI:10.1039/d3cc03320a
Source: Chemical Communications - September 20, 2023 Category: Chemistry Authors: Haiyan Wang Congling Wang Yuxian Deng Yuxin Han Shuo Xiang Hanning Xiao Qunhong Weng Source Type: research
Synthesis, cytotoxic activity evaluation and mechanistic investigation of novel 3,7-diarylsubstituted 6-azaindoles
Eur J Med Chem. 2023 Sep 13;261:115804. doi: 10.1016/j.ejmech.2023.115804. Online ahead of print.ABSTRACTA number of new disubstituted 6-azaindoles have been designed and synthesized bearing a crucial structural modification in respect to an analogous antiproliferative hit compound. The synthesis was performed using 2-amino-3-nitro-4-picoline, that was suitably modified and converted to 7-chloro-3-iodo-6-azaindole and this central scaffold was used for successive Suzuki-type couplings, to result in the target compounds. The evaluation of the cytotoxic activity was performed against four human cancer cell lines, as well as ...
Source: European Journal of Medicinal Chemistry - September 20, 2023 Category: Chemistry Authors: Nikolaos Lougiakis Nikolaos Sakalis Maria Georgiou Panagiotis Marakos Nicole Pouli Alexios-Leandros Skaltsounis Eleni Mavrogonatou Harris Pratsinis Dimitris Kletsas Source Type: research
Flower-like porous BCN assembled by nanosheets for paclitaxel delivery
This study presents a novel template method for preparing porous BCN nanomaterials, offering a promising platform for high-performance anticancer drug delivery.PMID:37727129 | DOI:10.1039/d3cc03320a
Source: Chemical Communications - September 20, 2023 Category: Chemistry Authors: Haiyan Wang Congling Wang Yuxian Deng Yuxin Han Shuo Xiang Hanning Xiao Qunhong Weng Source Type: research
Medicinal Chemistry-driven Approach to Novel 2-Substituted Benzoxazole - Estradiol Chimeras: Synthesis, Anticancer Activity and Early ADME Profile
ChemMedChem. 2023 Sep 20:e202300352. doi: 10.1002/cmdc.202300352. Online ahead of print.ABSTRACTThe efficient synthesis of novel estradiol-based A-ring-fused oxazole derivatives, which can be considered as benzoxazole-steroid domain-integrated hybrids containing a common benzene structural motif, is described. The target compounds were prepared from steroidal 2-aminophenol precursors by heterocycle formation or functional group interconversion (FGI) strategies. According to 2D projection-based t-distributed stochastic neighbor embedding (t-SNE), the novel molecules were proved to represent a new chemical space among steroi...
Source: ChemMedChem - September 20, 2023 Category: Chemistry Authors: Ferenc Kov ács Ildik ó Huliák H édi Árva M ónika Kiricsi D óra Erdős Marianna Kocsis Gergely Tak ács Gy örgy T Balogh Éva Frank Source Type: research
Enantioselective De Novo Synthesis of α,α-Diaryl Ketones from Alkynes
Angew Chem Int Ed Engl. 2023 Sep 19:e202310078. doi: 10.1002/anie.202310078. Online ahead of print.ABSTRACTChiral α,α-diaryl ketones are structural motifs commonly present in bioactive molecules, and they are also valuable building blocks in synthetic organic chemistry. However, catalytic asymmetric synthesis of α,α-diaryl ketones bearing a tertiary stereogenic center remains largely unsolved. Herein, we report a catalytic de novo enantioselective synthesis of α,α-diaryl ketones from simple alkynes via chiral phosphoric acid (CPA) catalysis. A broad range of enolizable α,α-diaryl ketones are prepared in good yields...
Source: Angewandte Chemie - September 19, 2023 Category: Chemistry Authors: Xueting Zhou Qingqin Huang Jiami Guo Lei Dai Yixin Lu Source Type: research
Design and Synthesis of New bis-oxindole and Spiro(triazole-oxindole) as CDK4 Inhibitors with Potent Anti-breast Cancer Activity
CONCLUSION: According to all of the findings, bis-oxindole 3c shows promise as a cancer treatment targeting CDK4.PMID:37723960 | DOI:10.2174/1573406419666230810124855
Source: Medicinal Chemistry - September 19, 2023 Category: Chemistry Authors: Thoraya A Farghaly Rami Adel Pashameah Abrar Bayazeed Amerah M Al-Soliemy Amani M R Alsaedi Marwa F Harras Source Type: research
Recent Advances in Nanobiotechnology for the Treatment of Non-Hodgkin's Lymphoma
Mini Rev Med Chem. 2023 Sep 15. doi: 10.2174/1389557523666230915103121. Online ahead of print.ABSTRACTLymphoma is the eighth most common type of cancer worldwide. Currently, lymphoma is mainly classified into two main groups: Hodgkin's lymphoma (HL) and non-Hodgkin's lymphoma (NHL), with NHL accounting for 80% to 90% of the cases. NHL is primarily divided into B, T, and natural killer (NK) cell lymphoma. Nanotechnology is developing rapidly and has made significant contributions to the field of medicine. This review summarizes the advancements of nanobiotechnology in recent years and its applications in the treatment of NH...
Source: Mini Reviews in Medicinal Chemistry - September 19, 2023 Category: Chemistry Authors: Shuxian Liu Minghao Xu Lei Zhong Xiangmin Tong Suying Qian Source Type: research
In silico Strategy: A Promising Implement in the Development of Multitarget Drugs against Neurodegenerative Diseases
Curr Top Med Chem. 2023 Aug 31. doi: 10.2174/1568026623666230811113231. Online ahead of print.ABSTRACTMulti-target drug development (MTDD) is the demand of the recent era, especially in the case of multi-factorial conditions such as cancer, depression, neurodegenerative diseases (NDs), etc. The MTDD approaches have many advantages; avoidance of drug-drug interactions, predictable pharmacokinetic profile, and less drug resistance. The wet lab practice in MTDD is very challenging for the researchers, and the chances of late-stage failure are obvious. Identification of an appropriate target (Target fishing) is another challen...
Source: Current Topics in Medicinal Chemistry - September 19, 2023 Category: Chemistry Authors: Purusottam Banjare Balaji Wamanrao Matore Anjali Murmu Vikash Kumar Jagadish Singh Partha Pratim Roy Source Type: research
