Molbank, 2021 2-Aryl-2-(3-indolyl)acetohydroxamic acids demonstrate promising antitumor activity, but quickly metabolize in vivo via glucuronidation of hydroxamic acid residue. In an attempt to improve their pharmacokinetics, methyl esters were synthesized via a newly
Dmitrii A. Aksenov +5 more
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Probing the Binding Requirements of Modified Nucleosides with the DNA Nuclease SNM1A
Molecules, 2021 SNM1A is a nuclease that is implicated in DNA interstrand crosslink repair and, as such, its inhibition is of interest for overcoming resistance to chemotherapeutic crosslinking agents.
Eva-Maria Dürr, Joanna F. McGouran
doaj +1 more source
Anti-tumor effect in human lung cancer by a combination treatment of novel histone deacetylase inhibitors: SL142 or SL325 and retinoic acids. [PDF]
PLoS ONE, 2010 Histone deacetylase (HDAC) inhibitors arrest cancer cell growth and cause apoptosis with low toxicity thereby constituting a promising treatment for cancer.
Shaoteng Han +7 more
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A minimalist chemical model of matrix metalloproteinases- Can small peptides mimic the more rigid metal binding sites of proteins? [PDF]
, 2013 In order to develop a minimalist chemical model of matrix metalloproteinases (MMPs), we synthesized a pentadecapeptide (Ac-KAHEFGHSLGLDHSK-NH2) corresponding to the catalytic zinc(II) binding site of human MMP-13.
Aguilar +48 more
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Iron‐Photocatalyzed C(sp3)–H Phosphonylation of Alkanes
Angewandte Chemie, EarlyView.Alkyl phosphonates are valuable motifs that can be prepared by phosphonylations of various common functional groups. However, direct phosphonylations of C(sp3)–H bonds are limited to activated positions. Herein, we report an iron‐photocatalyzed phosphonylation of unactivated C(sp3)–H bonds using a novel phosphite radical trap, which is equipped with an
Ya Dong +6 more
wiley +2 more sources
Journal of Enzyme Inhibition and Medicinal Chemistry, 2020 Oxazolidinone hydroxamic acid derivatives were synthesised and evaluated for inhibitory activity against leukotriene (LT) biosynthesis in three in vitro cell-based test systems and on direct inhibition of recombinant human 5-lipoxygenase (5-LO). Thirteen
Oludotun A. Phillips +2 more
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Phase I dose-escalation study of the mTOR inhibitor sirolimus and the HDAC inhibitor vorinostat in patients with advanced malignancy. [PDF]
, 2016 Preclinical models suggest that histone deacetylase (HDAC) and mammalian target of rapamycin (mTOR) inhibitors have synergistic anticancer activity. We designed a phase I study to determine the safety, maximum tolerated dose (MTD), recommended phase II ...
Falchook, Gerald S. +17 more
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Interactions of Bacillus Mojavensis and Fusarium Verticillioides With a Benzoxazolinone (Boa) and Its Transformation Product, Apo [PDF]
, 2007 En:Journal of Chemical Ecology (2007, vol. 33, n. 10, p. 1885-1897)The benzoxazolinones, specifically benzoxazolin-2(3H)-one (BOA), are important transformation products of the benzoxazinones that can serve as allelochemicals providing resistance to ...
A. Baumeler +55 more
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Rescue of cell cycle progression in BRAF inhibitor–resistant human melanoma by a chromatin modifier
Tumor Biology, 2017 The BRAF V600E -specific inhibitor vemurafenib blocks mitogen-activated protein kinase pathway and induces cell cycle arrest at G0/G1 phase leading to apoptosis of melanomas.
Antoni X Torres-Collado +2 more
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PREPARATION OF NEW COMPLEXES DERIVED FROM DIETHYLGLUTART AND STUDYING THEIR SPECTRUM PROPERTIES AND BIOLOGICAL ACTIVITY [PDF]
مجلة جامعة الانبار للعلوم الصرفة, 2012 This research designed to be on four steps: The first step includes preparation of a group legends derived from glutaric acid, the second step which the research includes is converting the acid derivatives that being prepared into hydroxamic acids.
SHAKIR F TULEAB
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