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The presence of nitrogen heterocycles in the architectural design of drugs has led to the discovery of new leading compounds.
Such analogues could be used as leading compounds for further rationale design and synthesis of efficient and specific therapeutic agents.
Although the leading compounds SU4984 and intedanib targets FGFR1, the kinase activity test revealed that these compounds only showed slight inhibitory activity on FGFR1 kinase.
This approach revealed two leading compounds, i.e. acetyl-[Ala15, Ala20]PACAP38-propylamide and acetyl-PACAP27-propylamide, which exhibited improved metabolic stability and potent biological activity.
Recently synthesized 12-mer peptide EBR28, which can strongly bind to IN, is one of the most potential small peptide leading compounds inhibiting IN binding with viral DNA.
The results of this study indicate that the new compounds are optimal anti-cancer leading compounds and merit further studies to optimize their structure, detect their biotargets and in vivo activity.
Similar(40)
DOX is the leading compound of a broad family of extractive or pharmaceutically engineered anticancer anthracyclines.
The leading compound 59 demonstrated subnanomolar inhibition of Wnt signaling in a paracrine cellular assay.
Furthermore compared with the leading compound hydrocortisone the safety of I6 was greatly improved.
In this study, the leading compound S8 was found based on virtual screening.
Compound 3a shows the most potent biological activity, which may be a promising antimicrobial leading compound for the further research.
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CEO of Professional Science Editing for Scientists @ prosciediting.com