Two novel macrocyclic organotin (IV) carboxylates based on bipyrazoledicarboxylic acid derivatives: syntheses, crystal structures and antifungal activities
Sign Up to like & getrecommendations! Published in 2021 at "Journal of Organometallic Chemistry"
DOI: 10.1016/j.jorganchem.2021.121913
Abstract: Abstract Two new organotin (IV) bipyrazole-dicarboxylate macrocyclic complexes, C1 (C58H100N8O10Sn4) and C2 (C58H100N8O12Sn4, 4 H2O), are synthesized by reaction of the bipyrazole-dicarboxylic acids L1 = 1,1′-(propane-1,3-diyl)bis(5-methyl-1H-pyrazole-3-carboxylic acid) and L2 = 1,1′-(2-hydroxypropane-1,3-diyl)bis(5-methyl-1H-pyrazole-3-carboxylic acid) with oxide di-(n-butyl)tin. The structure… read more here.
Keywords: two novel; carboxylates based; novel macrocyclic; organotin carboxylates ... See more keywords
Discovery of Novel Macrocyclic MERTK/AXL Dual Inhibitors.
Sign Up to like & getrecommendations! Published in 2024 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.4c00148
Abstract: MERTK and AXL are members of the TAM (TYRO3, AXL, MERTK) family of receptor tyrosine kinases that are aberrantly expressed and have been implicated as therapeutic targets in a wide variety of human tumors. Dual… read more here.
Keywords: mertk; novel macrocyclic; cell; discovery novel ... See more keywords
Discovery of a Novel Macrocyclic Noncovalent CDK7 Inhibitor for Cancer Therapy.
Sign Up to like & getrecommendations! Published in 2024 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.4c02098
Abstract: Cyclin-dependent kinase 7 (CDK7) is a key regulator of the cell cycle and transcription, making it a promising target for cancer therapy. Although current CDK7 inhibitors have improved in their selectivity and druglike properties, CDK7… read more here.
Keywords: cdk7; novel macrocyclic; macrocyclic noncovalent; cancer therapy ... See more keywords
Novel Macrocyclic Antagonists of the CGRP Receptor Part 2: Stereochemical Inversion Induces an Unprecedented Binding Mode.
Sign Up to like & getrecommendations! Published in 2022 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.2c00400
Abstract: The diastereomeric macrocyclic calcitonin gene-related peptide (CGRP) antagonists HTL0029881 (3) and HTL0029882 (4), in which the stereochemistry of a spiro center is reversed, surprisingly demonstrate comparable potency. X-ray crystallographic characterization demonstrates that 3 binds to… read more here.
Keywords: macrocyclic antagonists; receptor part; antagonists cgrp; novel macrocyclic ... See more keywords
Discovery and Optimization of a Novel Macrocyclic Amidinourea Series Active as Acidic Mammalian Chitinase Inhibitors.
Sign Up to like & getrecommendations! Published in 2023 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.2c00472
Abstract: Our research group has been involved for a long time in the development of macrocyclic amidinoureas (MCAs) as antifungal agents. The mechanistic investigation drove us to perform an in silico target fishing study, which allowed… read more here.
Keywords: optimization novel; chitinase; mammalian chitinase; discovery optimization ... See more keywords
Abstract A030: Discovery and preclinical characterization of novel macrocyclic KIF18A Inhibitors for treatment of chromosomally instable tumors
Sign Up to like & getrecommendations! Published in 2025 at "Molecular Cancer Therapeutics"
DOI: 10.1158/1535-7163.targ-25-a030
Abstract: Chromosome instability (CIN) and Genetic instability are hallmark features of malignant tumor cells, contributing to tumour progression, drug resistance and metastasis. KIF18A, a member of the kinesin superfamily of motor proteins, is essential for preserving… read more here.
Keywords: kif18a inhibitors; novel macrocyclic; macrocyclic kif18a; chromosomally instable ... See more keywords