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#1Hiroyuki Watanabe (Kyoto University)H-Index: 18
#2Naoki Matsushita (Kyoto University)
Last. Masahiro Ono (Kyoto University)H-Index: 31
view all 7 authors...
Orexin 2 receptor (OX2R) is thought to play an important role in the arousal-promoting function, but its distribution and function in the pathophysiology of orexin-mediated disorders remains to be fully elucidated. In the present study, we synthesized and characterized a novel 18F-labeled 2,5-diarylnicotinamide (DAN) derivative as a potential positron emission tomography (PET) probe for in vivo imaging of OX2R. In in vitro binding experiments, [18F]DAN-1 selectively bound to OX2R. In a biodistri...
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#1Weicong LiuH-Index: 7
#2Ying PanH-Index: 2
Last. Jian-Qiang LiuH-Index: 19
view all 8 authors...
The high storage capacities and excellent biocompatibilities of zinc(II) metal–organic frameworks (Zn-MOFs) have made them outstanding candidates as drug delivery carriers. Recent studies on the pH-responsive processes based on carrier–drug interactions have proven them to be the most efficient and effective way to control the release profiles of drugs. To satisfy the ever-growing demand in cancer therapy, great efforts are being devoted to the development of methods to precisely control drug re...
1 CitationsSource
#1Charlotta Wallinder (Uppsala University)H-Index: 11
#2Christian Sköld (Uppsala University)H-Index: 15
Last. Mathias Alterman (Uppsala University)H-Index: 20
view all 9 authors...
Rigidification of the isobutyl side chain of drug-like AT2 receptor agonists and antagonists that are structurally related to the first reported selective AT2 receptor agonist 1 (C21) delivered bioactive indane derivatives. Four enantiomer pairs were synthesized and the enantiomers were isolated in an optical purity >99%. The enantiomers 7a, 7b, 8a, 8b, 9a, 9b, 10a and 10b bind to the AT2 receptor with moderate (Ki = 54–223 nM) to high affinity (Ki = 2.2–7.0 nM). The enantiomer with positive opt...
1 CitationsSource
#1Kusum VatsH-Index: 3
#2Kanhaiyalal Agrawal (AIIMS: All India Institute of Medical Sciences)
Last. Ashutosh Dash (HBNI: Homi Bhabha National Institute)H-Index: 3
view all 6 authors...
This study explores the feasibility of radiolabeling the HBED-CC-PSMA (PSMA-11) ligand with Tc-99m for SPECT imaging of prostate cancer patients. 68Ga-HBED-CC-PSMA (PSMA-11) is used clinically for PET/CT imaging of prostate cancer (PCa) patients. However, a PET/CT facility may not be affordable and/or accessible to remotely located health centers. Thus, economic considerations require development of a SPECT-based tracer to provide low cost effective health care to the entire global population. H...
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#1Clinton G. MikekH-Index: 3
#2Modi WangH-Index: 1
Last. Herman O. SintimH-Index: 33
view all 4 authors...
The cyclic dinucleotide-cGAS-STING axis plays important roles in host immunity. Activation of this signaling pathway, via cytosolic sensing of bacterial-derived c-di-GMP/c-di-AMP or host-derived cGAMP, leads to the production of inflammatory interferons and cytokines that help resolve infection. Small molecule activators of the cGAS-STING axis have the potential to augment immune response against various pathogens or cancer. The aberrant activation of this pathway, due to gain-of-function mutati...
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#1João Paulo Bizarro Lopes (UFRGS: Universidade Federal do Rio Grande do Sul)H-Index: 3
#2Luana Silva (UFRGS: Universidade Federal do Rio Grande do Sul)H-Index: 1
Last. Laurent E. DardenneH-Index: 12
view all 14 authors...
In this study, we synthesized nine novel hybrids derived from D-xylose, D-ribose, and D-galactose sugars connected by a methylene chain with lophine. The compounds were synthesized by a four-component reaction to afford the substituted imidazole moiety, followed by the displacement reaction between sugar derivatives with an appropriate N-alkylamino-lophine. All the compounds were found to be the potent and selective inhibitors of BuChE activity in mouse serum, with compound 9a (a D-galactose der...
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#1Hang Gao (BNU: Beijing Normal University)H-Index: 1
#2Shuxia Wang (BNU: Beijing Normal University)H-Index: 1
Last. Huabei Zhang (BNU: Beijing Normal University)H-Index: 10
view all 5 authors...
A series of 9H-fluoren-9-one substituents were synthesized and evaluated for imaging cerebral α7-nAChRs. Meta-iodine substituted 9-fluorenone 5 with high binding affinity (Ki = 9.3 nM) and selectivity was radiolabeled with 125I. Fully in vitro and in vivo studies of [125I]5 have been performed. [125I]5 exhibited well brain uptake with a peak concentration of 7.5 ± 0.9% ID/g in mice brains. Moreover, ex vivo autoradiography studies and micro single-photon emission computed tomography (micro-SPECT...
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#1Yue-Yang Ji (ECNU: East China Normal University)H-Index: 2
#2Zhi-Long Wang (CAS: Chinese Academy of Sciences)H-Index: 4
Last. Li-Fang Yu (ECNU: East China Normal University)H-Index: 13
view all 10 authors...
Previously we identified a series of amidoalkylindoles as potent and selective CB2 partial agonists. In the present study, we report our continuous effort to improve the aqueous solubility by introducing N atoms to the amidoalkylindole framework. Synthesis, characterization, and pharmacology evaluations were described. Bioisosteric replacements of the indole nucleus with an indazole, azaindole and benzimidazole were explored. Benzimidazole 43 (EC50,CB1 = NA, EC50,CB2 = 0.067 μM) and azaindole 24...
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#1K. Y. Yeong (Monash University Malaysia Campus)
#2M. I. H. Nor Azizi (Monash University Malaysia Campus)
Last. Keykavous Parang (URI: University of Rhode Island)H-Index: 29
view all 7 authors...
New benzimidazoles were synthesized based on the previously identified sirtuin inhibitor BZD9L1. The compounds were screened for their sirtuin (SIRT1, SIRT2 and SIRT3) inhibitory activities. Compound BZD9Q1 was determined to be a pan-SIRT1–3 inhibitor. Furthermore, the proliferation of various cancer cells was inhibited by BZD9Q1. It was shown that BZD9Q1 elicits a cytostatic effect by inducing cell cycle arrest at the G2/M phase while also showing a prominent induction of apoptosis against oral...
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#1Andrew M. Beekman (UEA: University of East Anglia)H-Index: 7
#2Marco M. D. Cominetti (UEA: University of East Anglia)H-Index: 3
Last. Mark Searcey (UEA: University of East Anglia)H-Index: 20
view all 5 authors...
In a proof-of-concept study, solid phase synthesis allowed the rapid generation of a small molecule drug conjugate in which the glutamate carboxypeptidase II (GCPII) targeting small molecule DUPA was conjugated to the alkylating subunit of the potent cytotoxin duocarmycin SA. The targeted SMDC contained a cathepsin B cleavable linker, which was shown to be active and selective against cathepsin B over-expressing and GCPII-expressing tumour cell lines.
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