Rhodanine as a scaffold in drug discovery: a critical review of its biological activities and mechanisms of target modulation

T Tomašić, L Peterlin Mašič - Expert opinion on drug discovery, 2012‏ - Taylor & Francis
Introduction: Rhodanine-based compounds have been associated with numerous biological
activities. After many years of research in drug discovery, they have gained a reputation as …

[HTML][HTML] Regulation and involvement of matrix metalloproteinases in vascular diseases

M Amin, S Pushpakumar, N Muradashvili… - Frontiers in …, 2016‏ - ncbi.nlm.nih.gov
Matrix metalloproteinases (MMPs) are a family of zinc dependent endopeptidases whose
main function is to degrade and deposit structural proteins within the extracellular matrix …

Discovery and Mechanistic Studies of Dual-Target Hits for Carbonic Anhydrase IX and VEGFR-2 as Potential Agents for Solid Tumors: X-ray, In Vitro, In Vivo, and In …

SM Hefny, TF El-Moselhy, N El-Din… - Journal of Medicinal …, 2024‏ - ACS Publications
A dual-targeting approach is predicted to yield better cancer therapy outcomes.
Consequently, a series of coumarin-based thiazoles (5a–h, 6, and 7a–e) were designed and …

[HTML][HTML] Structure-based molecular modeling in SAR analysis and lead optimization

V Temml, Z Kutil - Computational and structural biotechnology journal, 2021‏ - Elsevier
In silico methods like molecular docking and pharmacophore modeling are established
strategies in lead identification. Their successful application for finding new active molecules …

Recent research advances in selective matrix metalloproteinase‐13 inhibitors as anti‐osteoarthritis agents

XW **e, RZ Wan, ZP Liu - ChemMedChem, 2017‏ - Wiley Online Library
Abstract Matrix metalloproteinase‐13 (MMP‐13) plays a key role in the degradation of type II
collagen in cartilage and bone in osteoarthritis (OA). The subtle differences between the …

Selective MMP-13 inhibitors: promising agents for the therapy of osteoarthritis

Y Wan, W Li, Z Liao, M Yan, X Chen… - Current medicinal …, 2020‏ - ingentaconnect.com
Osteoarthritis (OA) is an age-related degenerative disease, which is characterized by
chronic joint pain, inflammation and the damage of joint cartilage. At present, steroidal drugs …

Fragment-based design and synthesis of coumarin-based thiazoles as dual c-MET/STAT-3 inhibitors for potential antitumor agents

BH Naguib, HA Elsebaie, MS Nafie, S Mohamady… - Bioorganic …, 2024‏ - Elsevier
Abstract c-MET and STAT-3 are significant targets for cancer treatments. Here, we describe
a class of very effective dual STAT-3 and c-MET inhibitors with coumarin-based thiazoles …

3-(Bromoacetyl) coumarins: unraveling their synthesis, chemistry, and applications

MM Abdou, A Abu-Rayyan, AG Bedir, S Abdel-Fattah… - RSC …, 2021‏ - pubs.rsc.org
This review emphasizes recent developments in synthetic routes of 3-(bromoacetyl)
coumarin derivatives. Also, chemical reactions of 3-(bromoacetyl) coumarins as versatile …

In vitro and in vivo trypanocidal activities of 8‐methoxy‐3‐(4‐nitrobenzoyl)‐6‐propyl‐2H‐cromen‐2‐one, a new synthetic coumarin of low cytotoxicity against …

GA Brancaglion, AE Toyota… - Chemical biology & …, 2018‏ - Wiley Online Library
Natural and synthetic coumarins have been described as prototypes of new drug candidates
against Chagas' disease. During a typical screening with new compounds, we observed the …

Randomized controlled studies on the efficacy of antiarthritic agents in inhibiting cartilage degeneration and pain associated with progression of osteoarthritis in the rat

EM TenBroek, L Yunker, MF Nies… - Arthritis research & …, 2016‏ - Springer
Background As an initial step in the development of a local therapeutic to treat osteoarthritis
(OA), a number of agents were tested for their ability to block activation of inflammation …