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KD5170, a novel mercaptoketone-based histone deacetylase inhibitor that exhibits broad spectrum antitumor activity in vitro and in vivo
TLDR
The biological and pharmaceutical profile of KD5170 supports its continued preclinical and clinical development as a broad spectrum anticancer agent and shows significant antiproliferative activity against a variety of human tumor cell lines, including the NCI-60 panel.
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Discovery of inducible nitric oxide synthase (iNOS) inhibitor development candidate KD7332, part 1: Identification of a novel, potent, and selective series of quinolinone iNOS dimerization inhibitors…
TLDR
Compounds 12 and 42--potent inhibitors of the human and mouse iNOS enzyme that were highly selective over endothelial NOS (eNOS) were identified from an ultra high-throughput screen of a novel series of quinolinone small molecule, nonarginine iNos dimerization inhibitors.
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Identification of KD5170: a novel mercaptoketone-based histone deacetylase inhibitor.
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Discovery of dual inducible/neuronal nitric oxide synthase (iNOS/nNOS) inhibitor development candidate 4-((2-cyclobutyl-1H-imidazo[4,5-b]pyrazin-1-yl)methyl)-7,8-difluoroquinolin-2(1H)-one (KD7332)…
TLDR
4,7-imidazopyrazine 42 was confirmed as an iNOS dimerization inhibitor and was efficacious in the mouse formalin model of nociception and Chung model of neuropathic pain, without showing tolerance after repeat dosing, demonstrating a wide therapeutic margin.
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KLYP956 Is a Non-Imidazole-Based Orally Active Inhibitor of Nitric-Oxide Synthase Dimerization
TLDR
KLYP956 represents the first nonimidazole-based inhibitor of iNOS and nNOS dimerization and provides a novel pharmaceutical alternative to previously described substrate competitive inhibitors.
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DCAF11 Supports Targeted Protein Degradation by Electrophilic Proteolysis-Targeting Chimeras.
TLDR
A functional screening strategy performed with a focused library of candidate electrophilic PROTACs is described to discover bifunctional compounds that degrade proteins in human cells by covalently engaging E3 ligases.
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Pharmacological Characterization of KLYP961, a Dual Inhibitor of Inducible and Neuronal Nitric-Oxide Synthases
TLDR
KLYP961 represents an ideal tool with which to probe the physiological role of NO derived from iNOS and nNOS in human pain and inflammatory states and has ideal drug like-properties, including excellent rodent and primate pharmacokinetics coupled with a minimal off-target activity profile.
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Alpha-mercaptoketone based histone deacetylase inhibitors.
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Identification and SAR of selective inducible nitric oxide synthase (iNOS) dimerization inhibitors.
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KD 5170 , a novel mercaptoketone-based histone deacetylase inhibitor that exhibits broad spectrum antitumor activity in vitro and in vivo
TLDR
The biological and pharmaceutical profile of KD5170 supports its continued preclinical and clinical development as a broad spectrum anticancer agent and shows significant antiproliferative activity against a variety of human tumor cell lines, including the NCI-60 panel.
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