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Synthesis and preliminary structure-activity relationship study of 3-methylquinazolinone derivatives as EGFR inhibitors with enhanced antiproliferative activities against tumour cells

期刊: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2021; 36 (1)

In this paper, a set of 3-methylquniazolinone derivatives were designed, synthesised, and studied the preliminary structure-activity relationship for ......

Piperazine skeleton in the structural modification of natural products: a review

期刊: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2021; 36 (1)

Piperazine moiety is a cyclic molecule containing two nitrogen atoms in positions 1 and 4, as well as four carbon atoms. Piperazine is one of the most......

Design, synthesis and biological evaluation of novel thiazole-naphthalene derivatives as potential anticancer agents and tubulin polymerisation inhibitors

期刊: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2021; 36 (1)

A novel series of thiazole-naphthalene derivatives as tubulin polymerisation inhibitors were designed, synthesised, and evaluated for the anti-prolife......

Synthesis and biological evaluation of 4-phenoxy-phenyl isoxazoles as novel acetyl-CoA carboxylase inhibitors

期刊: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2021; 36 (1)

Acetyl-CoA carboxylase (ACC) is a crucial enzyme in fatty acid metabolism, which plays a major role in the occurrence and development of certain tumou......

Tertiary sulphonamide derivatives as dual acting small molecules that inhibit LSD1 and suppress tubulin polymerisation against liver cancer

期刊: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2021; 36 (1)

A series of tertiary sulphonamide derivatives were synthesised and evaluated for their antiproliferative activity against liver cancer cell lines (SNU......

Identification of imidazo[4,5-c]pyridin-2-one derivatives as novel Src family kinase inhibitors against glioblastoma

期刊: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2021; 36 (1)

Glioblastoma multiforme (GBM) is the most common and malignant primary brain tumour in the central nervous system (CNS). As the ideal targets for GBM ......

Synthesis, biological evaluation and molecular docking investigation of new sulphonamide derivatives bearing naphthalene moiety as potent tubulin polymerisation inhibitors

期刊: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2021; 36 (1)

A new series of sulphonamide derivatives bearing naphthalene moiety were synthesised and evaluated for their antiproliferative and tubulin polymerisat......

Application of triazoles in the structural modification of natural products

期刊: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2021; 36 (1)

Nature products have been extensively used in the discovery and development of new drugs, as the most important source of drugs. The triazole ring is ......

Discovery of N-aryl sulphonamide-quinazoline derivatives as anti-gastric cancer agents in vitro and in vivo via activating the Hippo signalling pathway

期刊: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2021; 36 (1)

Hippo signalling pathway plays a crucial role in tumorigenesis and cancer progression. In this work, we identified an N-aryl sulphonamide-quinazoline ......

Dual inhibition of EGFR and IL-6-STAT3 signalling by miR-146b: a potential targeted therapy for epithelial ovarian cancer

期刊: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2021; 36 (1)

Epidermal growth factor receptor (EGFR) signalling and the interleukin-6 (IL-6)/signal transducer and activator of transcription 3 (STAT3) are aberran......

Structure-based virtual screening of highly potent inhibitors of the nematode chitinase CeCht1

期刊: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2021; 36 (1)

Nematode chitinases play vital roles in various physiological processes, including egg hatching, larva moulting, and reproduction. Small-molecule inhi......

Inhibition of catechol-O-methyltransferase by natural pentacyclic triterpenes: structure-activity relationships and kinetic mechanism

期刊: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2021; 36 (1)

Inhibitors of COMT are clinically used for the treatment of Parkinson's disease. Here, we report the first natural pentacyclic triterpenoid-type COMT ......

Identification of a novel SPT inhibitor WXP-003 by docking-based virtual screening and investigation of its anti-fungi effect

期刊: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2021; 36 (1)

Serine palmitoyltransferase (SPT) plays the key role on catalysing the formation of 3-ketodihydrosphingosine, which is the first step of the de novo b......

Structure-activity relationship, in vitro and in vivo evaluation of novel dienyl sulphonyl fluorides as selective BuChE inhibitors for the treatment of Alzheimer's disease

期刊: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2021; 36 (1)

To discover novel scaffolds as leads against dementia, a series of delta-aryl-1,3-dienesulfonyl fluorides with alpha-halo, alpha-aryl and alpha-alkyny......

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