flexx version 3.1.2 (BioSolveIT GmbH)
90
Structured Review
BioSolveIT GmbH
flexx version 3.1.2
Flexx Version 3.1.2, supplied by BioSolveIT GmbH, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
https://www.bioz.com/product/flexx+3%2E1%2E2/flexx+3+1/10__2174_slash_1570180818666211207125903-43-15-18
Average 90 stars, based on 1 article reviews
Flexx Version 3.1.2, supplied by BioSolveIT GmbH, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
https://www.bioz.com/product/flexx+3%2E1%2E2/flexx+3+1/10__2174_slash_1570180818666211207125903-43-15-18
Average 90 stars, based on 1 article reviews
flexx version 3.1.2 - by Bioz Stars,
2026-09
90/100 stars
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other:Article Title: N⁴-(3-Bromophenyl)-7-(substituted benzyl) pyrrolo[2,3-d]pyrimidines as potent multiple receptor tyrosine kinase inhibitors: design, synthesis, and in vivo evaluation. Article Snippet: Article Title: Discovery of highly potent, nonsteroidal 17β-hydroxysteroid dehydrogenase type 1 inhibitors by virtual high-throughput screening. Article Snippet: 17 -Hydroxysteroid dehydrogenase type 1 (17 -HSD1) catalyzes the formation of the potent proliferation-stimulating hormone estradiol, and it is thus involved in the development of hormonedependent breast cancer.. Due to its high substrate specificity and the known relationships between its overexpression and disease incidence, 17 -HSD1 is considered an attractive target for drug develop- Article Title: Design and synthesis of substrate mimetics based on an indole scaffold: potential inhibitors of 17β-HSD type 1 Article Snippet: Background: Human 17b-hydroxysteroid dehydrogenase type 1 (17b-HSD1) acts at a pre-receptor level.. It catalyzes NADPH-dependent reduction of the weak estrogen estrone into the most potent estrogen estradiol, which exerts its proliferative effects via estrogen receptors.. Overexpression of 17b-HSD1 in estrogen-responsive tissues is related to the development of hormone-dependent diseases, such as breast cancer and endometriosis. Article Title: Phosphorylated hydroxyethylamines as novel inhibitors of the bacterial cell wall biosynthesis enzymes MurC to MurF. Article Snippet: 0045-2068/$ see front matter 2009 Elsevier Inc. A doi:10.1016/j.bioorg.2009.09.001 * Corresponding author.. Fax: +386 1 4258031.. E-mail address: gobecs@ffa.uni-lj.si (S. Gobec). Article Title: Design, synthesis and evaluation of 2-amino-4-m-bromoanilino-6-arylmethyl-7H-pyrrolo[2,3-d]pyrimidines as tyrosine kinase inhibitors and antiangiogenic agents1 Article Snippet: Flexx 3.1.2 BioSolveIT GmbH, An der Ziegelei 79, Article Title: The Synthesis of Novel 2,4,6-Trisubstituted 1,3,5-Triazines: A Search for Potential MurF Enzyme Inhibitors Article Snippet: A series of new 2,4,6-trisubstituted 1,3,5-triazines, possessing a variety of substituents (–OH, –SH, –OMe, –Cl, –HNR, –SR and amino acid moieties), were synthesized and evaluated for the inhibition of the bacterial peptidoglycan biosynthesis enzyme MurF.. Ethoxycarbonyl isothiocyanate successfully reacted with a variety of amidines, enabling an approach to 6-substituted-4-thioxo-1,3,5-triazin-2-ones.. Also, a representative set of 2-thio-, 2-amino-, and 2-oxo-substituted 1,3,5-triazines was synthesized by the SNAr reaction, employing 2,4,6-trichloro-1,3,5-triazine and 2-chloro-4,6-dimethoxy1,3,5-triazine as the starting materials. Article Title: Synthesis and biological evaluation of (6- and 7-phenyl) coumarin derivatives as selective nonsteroidal inhibitors of 17β-hydroxysteroid dehydrogenase type 1. Article Snippet: 17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1) is an enzyme that catalyzes NADPH-dependent reduction of the weak estrogen, estrone, into the most potent estrogen, estradiol, which exerts proliferative effects via the estrogen receptors.. Overexpression of 17β-HSD1 in estrogen-responsive tissues is related to the development of hormone-dependent diseases, such as breast cancer and endometriosis; thus, 17β-HSD1 represents an attractive target for the development of new therapies.We have discovered that simple coumarines 1 and 2 significantly inhibit 17β-HSD1 in a recombinant enzyme assay, with high selectivity against 17β-HSD2.Wepostulated that the introduction of various p-substituted phenyl moieties to position 6 or 7 of the coumarin core using the Suzuki-Miyaura cross-coupling reaction wouldprovidemimetics of steroidal structureswith improved inhibitionof 17β-HSD1.Thebest inhibitor in the series proved to be 6a, with an IC50 of 270 nM, and with exceptional selectivity for 17β-HSD1 over 17β-HSD2 and against the R and β estrogen receptors. |