109180-95-2Relevant academic research and scientific papers
ISOINDOLINONE AND INDAZOLE COMPOUNDS FOR THE DEGRADATION OF EGFR
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, (2021/06/26)
The invention provides compounds that degrade the epidermal growth factor receptor (EGFR) including mutant forms via the ubiquitination of the EGFR protein and subsequent proteasomal degradation. The compounds are useful for the treatment of various cancers.
Design, Synthesis, and Characterization of Novel CXCR4 Antagonists Featuring Cyclic Amines
Fu, Chunyan,He, Sudan,Li, Zhanhui,Lin, Yu,Luo, Lusong,Ma, Haikuo,Song, Shiwei,Tian, Sheng,Wang, Xu,Wang, Yujie,Wu, Shuwei,Zhang, Xiaohu,Zhao, Li,Zheng, Jiyue,Zhu, Fang
, (2020/06/01)
Chemokine receptor CXCR4 and its natural ligand CXCL12 (also known as stromal cell-derived factor-1, or SDF-1) regulate a broad range of physiological functions. Dysregulation of the CXCL12/CXCR4 axis is involved in numerous pathological conditions such as HIV infection, inflammation and cancer. Herein, we report the design, synthesis, and characterization of novel CXCR4 antagonists based on cyclic amine scaffolds. Compound 24 was identified as a potent CXCR4 receptor antagonist (competitive inhibition of 12G5 binding, IC50=24 nM; functional inhibition of CXCL12-induced cytosolic calcium increase, IC50=0.1 nM). In addition, compound 24 potently inhibited cell migration in CXCR4/CXCL12-mediated chemotaxis in a matrigel invasion assay. The absolute configuration of compound 24 was elucidated by X-ray crystallography.
HETEROARYL COMPOUNDS AS CXCR4 INHIBITORS, COMPOSITION AND METHOD USING THE SAME
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Paragraph 00219-00221, (2019/04/16)
The present disclosure provides heteroaryl compounds of Formula (I), processes for their preparation, pharmaceutical compositions containing them, and their use in the treatment of diseases and disorders, arising from or related to the CXCR4 pathway.
Exploring β-hydroxy γ-amino acids (statines) in the design of hybrid peptide foldamers
Bandyopadhyay, Anupam,Malik, Ankita,Kumar, Mothukuri Ganesh,Gopi, Hosahudya N.
, p. 294 - 297 (2014/01/23)
The synthesis and characterization of syn and anti β-hydroxy γ-amino acid (statine) diastereoisomers, their utilization in the design of hybrid peptide foldamers, and their single crystal conformations are studied.
Enantiospecific first total synthesis of 7a(S)-p-hydroxyphenopyrrozin
Kothapalli, Yugandhar,Puthukanoori, Ravi Kumar,Alapati, Srinivasa Rao
, p. 1891 - 1893 (2012/05/07)
An enantiospecific first total synthesis of metabolite 7a(S)-p- hydroxyphenopyrrozin 2, isolated from the cultured fungi Chromocleista sp. has been achieved starting from readily and abundantly available l-proline. The strategy of synthesis utilizes base
A facile transformation of amino acids to functionalized coumarins
Bandyopadhyay, Anupam,Gopi, Hosahudya N.
, p. 8089 - 8095 (2012/01/04)
The synthesis of novel chiral coumarins functionalized with proteinogenic amino acid side chains via N-protected γ-amino-β-keto esters and their incorporation into the cell permeable HIV-1 TAT peptide through the modified solid phase peptide synthesis are
CONDENSED HETEROCYCLIC COMPOUNDS AS CALCITONIN AGONISTS
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Page/Page column 43, (2010/02/07)
The present invention relates to novel fused heterocyclic ring system compounds and methods for their use in the treatment and prevention of diseases or conditions which are related to irregular calcification.
STEREOSELECTIVE ADDITION OF LITHIOETHYLACETATE TO BOC-L-PROLINAL. A CONVENIENT CHIRAL SYNTHETIC BUILDING BLOCK FOR THE PYRROLIZIDINE ALKALOID RING SYSTEM
Hanson, Gunnar J.,Baran, John S.,Lindberg, Thomas
, p. 3577 - 3580 (2007/10/02)
Aldol condensation of lithioethyl acetate with Boc-L-prolinal proceeds stereoselectively to give R,S diastereomer 2.Acidolysis of the Boc group and lactamization gives crystalline 3 which possesses the pyrrolizidine alkaloid skeleton.Saponification and acidolysis of 2 yields 7, a novel GABA analogue.
