The first total synthesis for large-scale production and anticancer activity of novel aminophenylpyridinium-5-(hydroxybenzoyl)hydrazonomethyl-2-oxothiazol-3-ide (PBHT) (1) and its derivatives are reported. The chemical structure of PBHT was unambiguously determined by utilization of the two-dimensional nuclear Overhauser effect (NOE) technique. The anticancer activity against human colon adenocarcinoma (HCT15) cells of all synthesized compounds was approximately four-fold greater than that of 5-fluorouracil, with IC50 values ranging from 10.1 to 14.2 µM. The three structural determinants of hydroxybenzoyl, hydrazinylidene, and pyridinium oxothiazole in the synthesized compounds could be indispensable for exhibiting anticancer activity.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1248/cpb.c15-00441 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Natural products and long non-coding RNAs in prostate cancer: insights into etiology and treatment resistance.
Naunyn Schmiedebergs Arch Pharmacol
January 2025
Department of Biochemistry, Faculty of Pharmacy, Badr University in Cairo (BUC), Badr City, , 11829, Cairo, Egypt.
Globally, the incidence and death rates associated with cancer persist in rising, despite considerable advancements in cancer therapy. Although some malignancies are manageable by a mix of chemotherapy, surgery, radiation, and targeted therapy, most malignant tumors either exhibit poor responsiveness to early identification or endure post-treatment survival. The prognosis for prostate cancer (PCa) is unfavorable since it is a perilous and lethal malignancy.
View Article and Find Full Text PDFConstruction of Escherichia coli cell factory for efficient synthesis of indigo.
Chembiochem
January 2025
Jiangnan University, State Key Laboratory of Food Science and Technology, 1800 Lihu Road, Wuxi, China, 214122, Wuxi, CHINA.
Indigo is widely used in dyes, medicines and semiconductors materials due to its excellent dyeing efficiency, antibacterial, antiviral, anticancer, anti-corrosion, and thermostability properties. Here, a biosynthetic pathway for indigo was designed, integrating two enzymes (EcTnaA, MaFMO) into a higher L-tryptophan-producing the strain Escherichia coli TRP. However, the lower catalytic activity of MaFMO was a bottleneck for increasing indigo titers.
View Article and Find Full Text PDFTransforming Bacterial Pathogens into Wonder Tools in Cancer Immunotherapy.
Mol Ther
January 2025
College of Veterinary Medicine, Jeonbuk National University, 79 Gobong-ro, Iksan City, Jeollabuk-do, 54596, Republic of Korea. Electronic address:
Cancer immunotherapy has revolutionized cancer treatment due to its precise, target-specific approach compared to conventional therapies. However, treating solid tumors remains challenging as these tumors are inherently immunosuppressive, and their tumor microenvironment (TME) often limits therapeutic efficacy. Interestingly, certain bacterial species offer a promising alternative by exhibiting an innate ability to target and proliferate within tumor environments.
View Article and Find Full Text PDFThe important role of the histone acetyltransferases p300/CBP in cancer and the promising anticancer effects of p300/CBP inhibitors.
Cell Biol Toxicol
January 2025
Department of Ultrasound, Shengjing Hospital of China Medical University, 110004, Shenyang, Liaoning, China.
Histone acetyltransferases p300 (E1A-associated protein p300) and CBP (CREB binding protein), collectively known as p300/CBP due to shared sequence and functional synergy, catalyze histone H3K27 acetylation and consequently induce gene transcription. p300/CBP over-expression or over-activity activates the transcription of oncogenes, leading to cancer cell growth, resistance to apoptosis, tumor initiation and development. The discovery of small molecule inhibitors targeting p300/CBP histone acetyltransferase activity, bromodomains, dual inhibitors of p300/CBP and BRD4 bromodomains, as well as proteolysis-targeted-chimaera p300/CBP protein degraders, marks significant progress in cancer therapeutics.
View Article and Find Full Text PDFAn In Vitro Study of the Effects of Methotrexate Loaded Biocomposite Beads on MG63 Osteoblast Cells.
Sci Rep
January 2025
Physics Department, Faculty of Science, Al-Azhar University, Nasr City, Cairo, 11884, Egypt.
This study aims to synthesize a new localized drug delivery system of bioglass, polyvinyl alcohol (PVA), cellulose (CNC), and sodium alginate (SA) beads as a carrier for methotrexate (MTX) drugs for the treatment of osteosarcoma. Methotrexate /Bioglass-loaded Polyvinyl/Cellulose/Sodium alginate biocomposite beads were prepared via the dropwise method with different concentrations of (65%SiO-30%CaO- 5%PO) bioglass. Samples were named B0, S0, S1, S2, and S3, respectively.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!