The synthesis and antitumoral activity of ester and amide derivatives of 2-arylamino-6-trifluoromethyl-3-pyridinecarboxylic acids 8-58 is described. Trifluoromethylpyridine derivatives 8-58 were evaluated for their anticancer activity toward human tumoral cell lines by the National Cancer Institute (NCI). Most of them possess encouraging anticancer activity, having GI(50) values in the low micromolar to nanomolar concentration range. The 3,4,5-trimethoxyphenylamide 44 was the most active, and it is now under review by NCI Biological Evaluation Committee for possible further studies.
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http://dx.doi.org/10.1016/j.bmc.2007.11.069 | DOI Listing |
J Transl Med
January 2025
Department of Urology, First Affiliated Hospital of Xi'an Jiaotong University, Xi'an, Shaanxi Province, China.
Background: The progression of bladder cancer (BC) from non-muscle-invasive bladder cancer (NMIBC) to muscle-invasive bladder cancer (MIBC) significantly increases disease severity. Although the tumor microenvironment (TME) plays a pivotal role in this process, the heterogeneity of tumor cells and TME components remains underexplored.
Methods: We characterized the transcriptomes of single cells from 11 BC samples, including 4 NMIBC, 4 MIBC, and 3 adjacent normal tissues.
BMC Complement Med Ther
January 2025
Division of Pharmacology and Biopharmaceutical Sciences, Faculty of Pharmaceutical Sciences, Burapha University, Chonburi, Thailand.
Background: Plant flavonoids such as quercetin are useful for both the therapeutic and preventive care of a variety of illnesses. Nevertheless, their antitumor efficacy against KON oral cancer is still unknown. Therefore, the aim of this investigation was to examine quercetin's anti-growth, anti-migrative, and anti-invasive characteristics.
View Article and Find Full Text PDFNat Commun
January 2025
Department of Orthopaedic Surgery, Washington University School of Medicine, St. Louis, MO, USA.
Mechanisms related to tumor evasion from NK cell-mediated immune surveillance remain enigmatic. Dickkopf-1 (DKK1) is a Wnt/β-catenin inhibitor, whose levels correlate with breast cancer progression. We find DKK1 to be expressed by tumor cells and cancer-associated fibroblasts (CAFs) in patient samples and orthotopic breast tumors, and in bone.
View Article and Find Full Text PDFDiscov Oncol
January 2025
Department of Thoracic Surgery, Shanghai Public Health Clinical Center, Fudan University Shanghai, Caolang Highway 2901#, Jinshan District, Shanghai, People's Republic of China.
Background: Lung adenocarcinoma (LUAD) is a leading form of non-small cell lung cancer characterized by a complex tumor microenvironment (TME) that influences disease progression and therapeutic response. Tumor-associated macrophages (TAMs) within the TME promote tumorigenesis and evasion of immune surveillance, though their heterogeneity poses challenges in understanding their roles and therapeutic targeting. Additionally, traditional Chinese medicine (TCM) offers potential anti-cancer agents that could modulate the immune landscape.
View Article and Find Full Text PDFJ Med Chem
January 2025
Key Laboratory of Tropical Biological Resources of Ministry of Education, School of Pharmaceutical Sciences, Hainan University, Haikou 570228, China.
A highly selective ferroptosis inducer with drug-like properties can significantly advance the research on inducing ferroptosis for anticancer treatment. We previously reported a highly active GPX4 inhibitor , but its activity and stability need further improvement. In this work, a novel GPX4 inhibitor with more potent cytotoxicity (IC = 0.
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