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Dentine biomodification by sulphonamides pre-treatment: bond strength, proteolytic inhibition, and antimicrobial activity

期刊: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2023; 38 (1)

We evaluated the effects of dentine biomodification after pre-treatment with two sulphonamide carbonic anhydrase inhibitors (CAIs) of the N-[4-sulpham......

1,2,3-Benzoxathiazine-2,2-dioxides - effective inhibitors of human carbonic anhydrases

期刊: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2023; 38 (1)

A series of 1,2,3-benzoxathiazine-2,2-dioxides possessing various substituents in the 5, 7, or 8 position was obtained from corresponding 2-hydroxyben......

Click chemistry approaches for developing carbonic anhydrase inhibitors and their applications

期刊: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2023; 38 (1)

Click chemistry reactions constitute an important and relatively new approach in the medicinal chemistry toolbox and offer substantial advantages to m......

Adiponectin - stratification biomarker in diastolic cardiac dysfunction

期刊: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2023; 38 (1)

This study does not propose to elucidate how adiponectin secretion is regulated, but how its adiponectin concentration is an indicator of heart diseas......

Unveiling the mechanism of action of acylated temporin L analogues against multidrug-resistant Candida albicans

期刊: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2023; 38 (1)

The increasing resistance of fungi to conventional antifungal drugs has prompted worldwide the search for new compounds. In this work, we investigated......

Flavone-based dual PARP-Tubulin inhibitor manifesting efficacy against endometrial cancer

期刊: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2023; 38 (1)

Structural tailoring of the flavone framework (position 7) via organopalladium-catalyzed C-C bond formation was attempted in this study. The impact of......

Investigation of novel alkyl/benzyl (4-sulphamoylphenyl)carbamimidothioates as carbonic anhydrase inhibitors

期刊: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2023; 38 (1)

A library of novel alkyl/benzyl (4-sulphamoylphenyl)carbamimidothioates was synthesised by selective S-alkylation of the easily accessible 4-thioureid......

Simultaneous administration of EZH2 and BET inhibitors inhibits proliferation and clonogenic ability of metastatic prostate cancer cells

期刊: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2023; 38 (1)

Androgen deprivation therapy (ADT) is a common treatment for recurrent prostate cancer (PC). However, after a certain period of responsiveness, ADT re......

Investigating the potential anticancer activities of antibiotics as topoisomerase II inhibitors and DNA intercalators: in vitro, molecular docking, molecular dynamics, and SAR studies

期刊: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2023; 38 (1)

Topoisomerase II (TOP-2) is a promising molecular target for cancer therapy. Numerous antibiotics could interact with biologically relevant macromolec......

Discovery of new 6-ureido/amidocoumarins as highly potent and selective inhibitors for the tumour-relevant carbonic anhydrases IX and XII

期刊: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2023; 38 (1)

A series of 6-ureido/amidocoumarins (5a-p and 7a-c) has been designed and synthesised to develop potent and isoform- selective carbonic anhydrase hCA ......

Design, synthesis and cytotoxic evaluation of novel bis-thiazole derivatives as preferential Pim1 kinase inhibitors with in vivo and in silico study

期刊: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2023; 38 (1)

Bis-thiazole derivatives were synthesised conforming to the Pim1 pharmacophore model following Hantzsch condensation. Pim1 has a major role in regulat......

Rational repurposing, synthesis, in vitro and in silico studies of chromone-peptidyl hybrids as potential agents against Leishmania donovani

期刊: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2023; 38 (1)

A chromone-peptidyl hybrids series was synthesised and rationally repurposed towards identification of potential antileishmanial hits against visceral......

Discovery of new pyridine-quinoline hybrids as competitive and non-competitive PIM-1 kinase inhibitors with apoptosis induction and caspase 3/7 activation capabilities

期刊: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2023; 38 (1)

New quinoline-pyridine hybrids were designed and synthesised as PIM-1/2 kinase inhibitors. Compounds 5b, 5c, 6e, 13a, 13c, and 14a showed in-vitro low......

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