Thiazole‐Based IL‐17 Inhibitors Discovered by Scaffold Morphing
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DOI: 10.1002/cmdc.202400851
Abstract: The pro‐inflammatory cytokine interleukin‐17A (IL‐17) plays an important role in the body's defense against bacterial and fungal infections. However, overexpression of IL‐17 has been associated with several diseases, including rheumatoid arthritis, asthma, psoriasis, and even… read more here.
Keywords: based inhibitors; scaffold morphing; discovered scaffold; thiazole based ... See more keywords
Discovery of novel piperidine-substituted indolylarylsulfones as potent HIV NNRTIs via structure-guided scaffold morphing and fragment rearrangement.
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DOI: 10.1016/j.ejmech.2016.10.009
Abstract: To further explore the chemical space around the entrance channel of HIV-1 reverse transcriptase (RT), a series of novel indolylarylsulfones (IASs) bearing N-substituted piperidine at indole-2-carboxamide were identified as potent HIV NNRTIs by structure-guided scaffold… read more here.
Keywords: scaffold morphing; structure guided; guided scaffold; hiv nnrtis ... See more keywords
Serendipitous Identification of Azine Anticancer Agents Using a Privileged Scaffold Morphing Strategy
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DOI: 10.3390/molecules29071452
Abstract: The use of privileged scaffolds as a starting point for the construction of libraries of bioactive compounds is a widely used strategy in drug discovery and development. Scaffold decoration, morphing and hopping are additional techniques… read more here.
Keywords: identification azine; scaffold morphing; azine anticancer; serendipitous identification ... See more keywords