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Recent News
11 April 2024
Press Release
Cambridge, UK and Kyiv, Ukraine, 11 April 2024: Metrion Biosciences Limited (“Metrion”), the specialist ion channel and cardiac safety screening contract research organisation (CRO) and drug discovery company, and Enamine Ltd (“Enamine”), the global leader in supplying small molecules and early drug discovery services, announced that Metrion has enhanced its High Throughput Screening (HTS) services with the addition of access to Enamine’s compound libraries.
27 March 2024
Press Release
March, 2024, Kyiv, Ukraine. Enamine Ltd, the global leader in supplying small molecules and early drug discovery services, announces the expansion of its library synthesis capabilities with a focus on Enamine REAL compounds to further support the growing demands of agricultural and pharmaceutical companies, research institutes, and drug discovery centers.
01 March 2024
News
We are excited to announce a strategic collaboration between Enamine, the world's leading provider of chemical building blocks, compound libraries, and biology services, and Genez International, a prominent enterprise with 15 years of experience in cross-border supply management, biopharmaceutical research and development, semiconductor equipment, and high-definition digital imaging systems.
J. Med. Chem.
2018, 61 (23), 10793-10813
DOI:
10.1021/acs.jmedchem.8b01428
Babii O.; Afonin S.; Ishchenko A.; Schober T.; Negelia A.; Tolstanova G.; Garmanchuk L.; Ostapchenko L.; Komarov I.; Ulrich A.
Five series (28 structures) of photoswitchable β-hairpin peptides were synthesized, based on the cyclic scaffold of the natural antibiotic gramicidin S. Cell-type selectivity was compared for all activated (diarylethene ring-open) and deactivated (closed) forms in terms of antibacterial activity (MIC against Escherichia coli and Bacillus subtilis), anticancer activity (IC50 against HeLa cell line), and hemolytic cytotoxicity (HC50 against human erythrocytes). Correlations between the conformational plasticity of the peptides, their hydrophobicity and their bioactivity were also analyzed. Considerable improvements in selectivity were achieved compared to the reference compound. We found a dissociation of the anticancer activity from hemolysis. Phototherapeutic indices (PTI) - HC50(closed)/MIC(open) and HC50(closed)/IC50(open) - were introduced for the peptides as safety criteria. The highest PTI for HeLa-selective toxicity were observed among analogues containing hydroxyleucine on the hydrophobic face. For one compound, high PTIs were demonstrated across a range of different cancer cell lines, including a doxorubicin-resistant one.