Scaffold hybridization strategy towards potent hydroxamate-based inhibitors ofFlaviviridaeviruses andTrypanosomaspecies
نویسندگان
چکیده
منابع مشابه
A novel family of hydroxamate-based acylating inhibitors of cyclooxygenase.
Aspirin irreversibly inhibits cyclooxygenase (COX) by acetylating a serine residue in the active site. We synthesized a series of novel acylating agents based on our previously reported acetylating compound, O-acetylsalicylhydroxamic acid. One of these, triacetylsalicylhydroxamic acid (TriAcSHA) was more effective than aspirin and O-acetylsalicylhydroxamic acid in inactivating both COX-1 and CO...
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The antimalarial activity and pharmacology of a series of phenylthiazolyl-bearing hydroxamate-based histone deacetylase inhibitors (HDACIs) was evaluated. In in vitro growth inhibition assays approximately 50 analogs were evaluated against four drug resistant strains of Plasmodium falciparum. The range of 50% inhibitory concentrations (IC(50)s) was 0.0005 to >1 microM. Five analogs exhibited IC...
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Reversible acetylation of histones and other proteins has emerged over the last 10 years as an important mechanism for cell proliferation and has been identified as a valuable target for anticancer drug design. Acetylation is executed and maintained by the histone acetyltransferases and reversed by their counterparts, histone deacetylases (HDACs). The first HDAC inhibitors have already been app...
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Background and objectives: Tyrosinase is a copper containing oxidase which is crucial for controlling the production of melanin in creatures such as bacteria, fungi, plants and mammals. It is involved in the first two steps of melanin biosynthesis and leads to pigmentation and different types of cancer such as melanoma. Also, it is responsible for browning of fruits and vegetab...
متن کاملStructure-Guided Evolution of Potent and Selective CHK1 Inhibitors through Scaffold Morphing
Pyrazolopyridine inhibitors with low micromolar potency for CHK1 and good selectivity against CHK2 were previously identified by fragment-based screening. The optimization of the pyrazolopyridines to a series of potent and CHK1-selective isoquinolines demonstrates how fragment-growing and scaffold morphing strategies arising from a structure-based understanding of CHK1 inhibitor binding can be ...
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ژورنال
عنوان ژورنال: MedChemComm
سال: 2019
ISSN: 2040-2503,2040-2511
DOI: 10.1039/c9md00200f