Background & Objective: A new series of thiazoles substituted on the chromene scaffold were prepared by facial approaches starting from (E)-1-(2,3-Dihydrochromen-4-ylidene)thiosemicarbazide derivatives (2a,b). The thiosemicarbazides (2a,b) were reacted with a series of α-halo carbonyl compounds to give the corresponding rhodanine analogues and reacted also with C-acetyl-or Cethoxy- N-hydrazonoyl chlorides to afford the corresponding tri- and tetra-substituted hybrid hydrazinyl thiazole substituted chromenes.
Methods: The newly synthesized compounds were screened for their in vitro antimicrobial and antitumor activities by agar diffusion method and MTT assay, respectively.
Results: The results of the antimicrobial activity revealed that some of the new compounds exhibited excellent activity against pathogenic microorganism; Candida albicans compared with Ciprofloxacin and nystatin, as the reference drugs. All of the tested compounds exhibited significant cytotoxic activities comparable to that of the reference drug; Doxorubicin® (on HCT116 (colorectal carcinoma human cell line).
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http://dx.doi.org/10.2174/1389557519666190722123422 | DOI Listing |
Sci Rep
December 2024
Department of Life Sciences, College of Life Sciences, National Chung Hsing University, Kuo Kuang Rd., Taichung, 402, Taiwan.
Hepatocellular carcinoma (HCC) constitutes 90% of liver cancer cases and ranks as the third leading cause of cancer-related mortality, necessitating urgent development of alternative therapies. Lactoferrin (LF), a natural iron-binding glycoprotein with reported anticancer effects, is investigated for its potential in liver cancer treatment, an area with limited existing studies. This study focuses on evaluating LF's anti-liver cancer effects on HCC cells and assessing the preventive efficacy of oral LF administration in a murine model.
View Article and Find Full Text PDFPLoS One
December 2024
Hangzhou Institute of Medicine (HIM), Zhejiang Cancer Hospital, Zhejiang, Hangzhou, China.
Purpose: Approximately 20% of all breast cancer cases are classified as triple-negative breast cancer (TNBC), which represents the most challenging subtype due to its poor prognosis and high metastatic rate. Caffeic acid phenethyl ester (CAPE), the main component extracted from propolis, has been reported to exhibit anticancer activity across various tumor cell types. This study aimed to investigate the effects and mechanisms of CAPE on TNBC.
View Article and Find Full Text PDFInt J Biol Macromol
December 2024
State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources, School of Chemistry and Pharmaceutical Science, Guangxi Normal University, Guilin 541001, PR China.
High locoregional recurrence rates and potential wound infections remain a significant challenge for postoperative breast cancer patients. Herein, we developed a dual-network hyaluronic acid (HA) nanocomposite hydrogel composed of herring sperm DNA (hsDNA) bridged methacrylated HA (HAMA) and FeMg-LDH-ppsa nanohybrid chelated catechol-modified HA (HADA) for the prevention of breast cancer recurrent, anti-infection, and promoting wound healing. Dynamic reversible hsDNA cross-linking combined with metal-catechol chelating renders the hydrogel injectability, rapid self-healing ability, and enhanced mechanical properties.
View Article and Find Full Text PDFJ Cancer Res Clin Oncol
December 2024
Zhuhai Tengbai Pharmaceutical Co., Ltd, Zhuhai, 519031, China.
Background: Colorectal cancer (CRC) is the third most common cancer globally, with advanced stages presenting significant treatment challenges. Recently years, drug combination therapy has become a promising strategy for cancer treatment.
Objective: To evaluate the therapeutic efficacy of the combination of the anti-angiogenic drug PEP06 (TB01) and the cytotoxic drug Trifluridine/Tipiracil (TAS-102) in human CRC HCT-116 xenograft mouse model.
Int J Nanomedicine
December 2024
Department of Dermatology, Affiliated Hospital of Shandong Second Medical University, School of Clinical Medicine, Shandong Second Medical University, Weifang, 261031, People's Republic of China.
Background: Melanoma is an aggressive skin tumor with limited therapeutic options due to rapid proliferation, early metastasis, and poor prognosis. Baicalin (BA), a natural flavonoid, shows promise in inducing ferroptosis and apoptosis but faces challenges of poor solubility and bioavailability. To address these issues, we developed a multifunctional drug delivery system: manganese-doped ZIF-8 nanoparticles (ZIF(Mn)) loaded with BA and modified with folic acid (FA) and polyethylene glycol (PEG).
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