Antitumor activity and toxicity to host of newly synthesized disulfide derivatives of 6-mercaptopurine (6-MP) and 6-thioguanine (6-TG) were examined in murine ascites sarcoma-180 system (total packed cell volume method) by parenteral administration. The compounds tested were 6-alkyl disulfides (carbon number of alkyl group: 2, 3, 4, 5, 6, 7, 8, 10, and 14), 6-branched-alkyl disulfides (iso-propyl, sec-butyl, and tert-butyl), and 6-aralkyl disulfide (naphthyryl). Most disulfide derivatives of 6-MP and 6-TG showed higher antitumor activity (lower ED50) and higher toxicity to host (lower LD50) than parent compounds, but ratios of increase in activity and toxicity were different with each other. The compounds with higher chemotherapeutic index (LD50/ED50) than parent compounds were alpha-naphthyryl (8.7) disulfide in a series of 6-MP (7.5) derivatives; and sec-butyl (27), tert-butyl (24), octyl (23), decyl (26), and alpha-naphthyryl (28) disulfides in a series of 6-TG (14) derivatives. These 6-TG derivatives were promising for antitumor agents.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1248/bpb1978.4.58 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Stroma-derived Dickkopf-1 contributes to the suppression of NK cell cytotoxicity in breast cancer.
Nat 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 PDFNanoparticle-based Drug Delivery Systems to Modulate Tumor Immune Response for Glioblastoma Treatment.
Acta Biomater
January 2025
School of Materials and Energy, Southwest University, Chongqing 400715, China; Yibin Academy of Southwest University, Yibin 644005, China. Electronic address:
Glioblastoma (GBM) is a primary central nervous system neoplasm, characterized by a grim prognosis and low survival rates. This unfavorable therapeutic outcome is partially attributed to the inadequate immune infiltration and an immunosuppressive microenvironment, which compromises the effectiveness of conventional radiotherapy and chemotherapy. To this end, precise modulation of cellular dynamics in the immune system has emerged as a promising approach for therapeutic intervention.
View Article and Find Full Text PDFEpithelial cell diversity and immune remodeling in bladder cancer progression: insights from single-cell transcriptomics.
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.
Quercetin triggers cell apoptosis-associated ROS-mediated cell death and induces S and G2/M-phase cell cycle arrest in KON oral cancer cells.
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 PDFDissecting macrophage heterogeneity and kaempferol in lung adenocarcinoma: a single-cell transcriptomic approach and network pharmacology.
Discov 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 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!