Articles with "lead compound" as a keyword



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A herbicide structure-activity analysis of the antimalarial lead compound MMV007978 against Arabidopsis thaliana.

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Published in 2018 at "Pest management science"

DOI: 10.1002/ps.4872

Abstract: BACKGROUND To fight herbicide-resistant weeds, new herbicides are needed; particularly ones with new modes of action. Building on the revelation that many antimalarial drugs are herbicidal, here we focus on the Medicines for Malaria Venture… read more here.

Keywords: compound mmv007978; arabidopsis thaliana; herbicide; lead compound ... See more keywords
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Water-soluble derivatives of evodiamine: Discovery of evodiamine-10-phosphate as an orally active antitumor lead compound.

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Published in 2021 at "European journal of medicinal chemistry"

DOI: 10.1016/j.ejmech.2021.113544

Abstract: 10-Hydroxyevodiamine is a multitargeting antitumor lead compound with excellent in vitro activity. However, its in vivo antitumor potency is rather limited, which has hampered its further clinical development. To overcome this obstacle, a series of novel water-soluble… read more here.

Keywords: soluble derivatives; lead compound; water soluble; antitumor lead ... See more keywords
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Tubulin targeted antimitotic agents based on adamantane lead compound: synthesis, SAR and molecular modeling

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Published in 2020 at "Mendeleev Communications"

DOI: 10.1016/j.mencom.2020.07.005

Abstract: 5-Hydroxymethyl-2-methoxyphenyl adamantane-1-acetate inhibits cell proliferation and stimulates depolymerization of microtubules of cancer cells to free tubulin. Its analogues were synthesized via the Steglich or Mitsunobu reactions to determine the role of structural subunits of the… read more here.

Keywords: lead compound; targeted antimitotic; antimitotic agents; compound ... See more keywords
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Discovery of PMSA Derivative 11 as a Novel Lead Compound for Therapeutic Treatment of Osteoporosis In Vitro and In Vivo.

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Published in 2023 at "Journal of medicinal chemistry"

DOI: 10.1021/acs.jmedchem.3c00114

Abstract: To discover a potent candidate for suppressing mature osteoclasts formation in vitro using a TRAP staining assay. A series of PMSA derivatives were synthesized and evaluated for their bioactivity in our current study. Our results… read more here.

Keywords: vitro; lead compound; pmsa derivative; pmsa ... See more keywords
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Structural Modifications and Biological Evaluations of Rift Valley Fever Virus Inhibitors Identified from Chemical Library Screening

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Published in 2022 at "ACS Omega"

DOI: 10.1021/acsomega.1c06513

Abstract: The Rift Valley fever virus (RVFV) is an emerging high-priority pathogen endemic in Africa with pandemic potential. There is no specific treatment or approved antiviral drugs for the RVFV. We previously developed a cell-based high-throughput… read more here.

Keywords: compound; rift valley; valley fever; lead compound ... See more keywords
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Study on the properties of perovskite materials under light and different temperatures and electric fields based on DFT

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Published in 2020 at "RSC Advances"

DOI: 10.1039/d0ra02841j

Abstract: The photoelectric conversion efficiency of perovskite solar cells has improved rapidly, but their stability is poor, which is an important factor that restricts their commercial production. This paper studies the physical and chemical stability of… read more here.

Keywords: electric fields; lead compound; different temperatures; iodized lead ... See more keywords
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An Optimized Dihydrodibenzothiazepine Lead Compound (SBI-0797750) as a Potent and Selective Inhibitor of Plasmodium falciparum and P. vivax Glucose 6-Phosphate Dehydrogenase 6-Phosphogluconolactonase

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Published in 2022 at "Antimicrobial Agents and Chemotherapy"

DOI: 10.1128/aac.02109-21

Abstract: In Plasmodium, the first two and rate-limiting enzymes of the pentose phosphate pathway, glucose 6-phosphate dehydrogenase (G6PD) and the 6-phosphogluconolactonase, are bifunctionally fused to a unique enzyme named GluPho, differing structurally and mechanistically from the… read more here.

Keywords: plasmodium; glucose phosphate; lead compound; sbi 0797750 ... See more keywords
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Development of Antifungal Peptides against Cryptococcus neoformans; Leveraging Knowledge about the cdc50Δ Mutant Susceptibility for Lead Compound Development

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Published in 2022 at "Microbiology Spectrum"

DOI: 10.1128/spectrum.00439-22

Abstract: The authors have developed a lead compound peptide antifungal drug targeting a protein from the organism Cryptococcus neoformans. Binding of the drug to the target fungal protein causes charged lipid molecules to be retained on… read more here.

Keywords: development; lead compound; caspofungin; drug ... See more keywords
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Antitussive and Anti-inflammatory Dual-active Agents Developed from Natural Product Lead Compound 1-Methylhydantoin

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Published in 2019 at "Molecules"

DOI: 10.3390/molecules24132355

Abstract: Natural products play an important role in drug discovery. This work employed a natural product 1-methylhydantoin as the lead compound to develop novel dual-active drugs. 1-Methylhydantoin was isolated from Oviductus Ranae, which is a traditional… read more here.

Keywords: anti inflammatory; lead compound; dual active; compound ... See more keywords
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Pharmacological Characters and Toxicity Evaluation of Coumarin Derivative LP4C as Lead Compound against Biofilm Formation of Pseudomonas aeruginosa

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Published in 2023 at "Molecules"

DOI: 10.3390/molecules28073138

Abstract: Pseudomonas aeruginosa-induced biofilm infection is difficult to treat and poses a significant threat to public health. Our previous study found a new coumarin derivative LP4C which exerted potent in vitro and in vivo anti-biofilm activity… read more here.

Keywords: pseudomonas aeruginosa; lead compound; derivative lp4c; biofilm ... See more keywords