A series of thiomorpholine sulfonamide hydroxamate TACE inhibitors, all bearing propargylic ether P1' groups, was explored. In particular, compound 5h has excellent in vitro potency against isolated TACE enzyme and in cells, oral activity in a model of TNF-alpha production and a collagen-induced arthritis model, was selected as a clinical candidate for the treatment of RA.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2005.12.020 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Dual-drug loaded chondroitin sulfate embolization beads enhance TACE therapy for HCC by integrating embolization, chemotherapy, and anti-angiogenesis.
Mater Today Bio
February 2025
State Key Laboratory of Digital Medical Engineering, Jiangsu Key Laboratory for Biomaterials and Devices, School of Biological Sciences & Medical Engineering, Southeast University, Nanjing, 210009, China.
Hepatocellular carcinoma (HCC) is a major public health threat due to its high incidence and mortality rates. Transcatheter arterial chemoembolization (TACE), the primary treatment for intermediate-to-advanced hepatocellular carcinoma (HCC), commonly utilizes embolic agents loaded with anthracycline-based cytotoxic drugs. Post-TACE, the hypoxic microenvironment in the tumor induced by embolization stimulates the formation of new blood vessels, potentially leading to revascularization and diminishing TACE's efficacy.
View Article and Find Full Text PDFDeep learning-based CT radiomics predicts prognosis of unresectable hepatocellular carcinoma treated with TACE-HAIC combined with PD-1 inhibitors and tyrosine kinase inhibitors.
BMC Gastroenterol
January 2025
Department of Interventional Radiology, Harbin Medical University Cancer Hospital, No. 150 Haping Road, Nangang District, Harbin, Heilongjiang Province, 150081, China.
Objective: To develop and validate a computed tomography (CT)-based deep learning radiomics model to predict treatment response and progression-free survival (PFS) in patients with unresectable hepatocellular carcinoma (uHCC) treated with transarterial chemoembolization (TACE)-hepatic arterial infusion chemotherapy (HAIC) combined with PD-1 inhibitors and tyrosine kinase inhibitors (TKIs).
Methods: This retrospective study included 172 patients with uHCC who underwent combination therapy of TACE-HAIC with TKIs and PD-1 inhibitors. Among them, 122 were from the Interventional Department of the Harbin Medical University Cancer Hospital, with 92 randomly assigned to the training cohort and 30 cases randomly assigned to the testing cohort.
Comparative Efficacy of Lenvatinib Plus Immunotherapy and Regorafenib Plus Immunotherapy After Lenvatinib Failure for Advanced Hepatocellular Carcinoma: A Retrospective Study.
Drugs Real World Outcomes
January 2025
Interventional Radiology Department, Jiangsu Cancer Hospital and Jiangsu Institute of Cancer Research and The Affiliated Cancer Hospital of Nanjing Medical University, Nanjing, Jiangsu, China.
Background: The combination of regorafenib and immune checkpoint inhibitor (ICI) has been the most popular second-line systemic therapy for advanced hepatocellular carcinoma (HCC). However, considering the good anti-tumor performance of lenvatinib, combined immunotherapy on the basis of lenvatinib after first-line lenvatinib failure is also popular in clinical practice. This study aimed to compare the efficacy and safety of regorafenib plus ICI (TACE-R-I) versus lenvatinib plus ICI (TACE-L-I) in patients with advanced HCC after lenvatinib failure.
View Article and Find Full Text PDFNeoadjuvant therapy with triple therapy for centrally located hepatocellular carcinoma.
Eur J Surg Oncol
January 2025
Department of Hepatopancreatobiliary Surgery, Sichuan Clinical Research Center for Cancer, Sichuan Cancer Hospital and Institute, Affiliated Cancer Hospital of University of Electronic Science and Technology of China, Chengdu, China. Electronic address:
Background: Centrally located hepatocellular carcinoma (HCC) is a subtype HCC with special location adjoined hepatic portals. It is difficult to be radically resected with sufficient surgical margin. We discussed whether neoadjuvant therapy could increase surgical margin and reduce recurrence.
View Article and Find Full Text PDFSafety and efficacy of PD-1 inhibitor (sintilimab) combined with transarterial chemoembolization as the initial treatment in patients with intermediate-stage hepatocellular carcinoma beyond up-to-seven criteria.
J Immunother Cancer
January 2025
Department of Liver Surgery and Transplantation, Liver Cancer Institute, Zhongshan Hospital, Fudan University, Shanghai, China
Background: Numerous studies have demonstrated limited survival benefits of transarterial chemoembolization (TACE) alone in the treatment of intermediate-stage hepatocellular carcinoma (HCC) beyond up-to-seven criteria. The advent of immunotherapy, particularly immune checkpoint inhibitors (ICIs), has opened new avenues for HCC treatment. However, TACE combined with ICIs has not been investigated for patients with intermediate-stage HCC beyond the up-to-seven criteria.
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!