198210-37-6Relevant academic research and scientific papers
Sialyltransferase Inhibitors Suppress Breast Cancer Metastasis
Fu, Chih-Wei,Tsai, Han-En,Chen, Wei-Sheng,Chang, Tzu-Ting,Chen, Chia-Ling,Hsiao, Pei-Wen,Li, Wen-Shan
, p. 527 - 542 (2021)
We report the synthesis and evaluation of a series of cell-permeable and N- versus O-selective sialyltransferase inhibitors. Inhibitor design entailed the functionalization of lithocholic acid at C(3) and at the cyclopentane ring side chain. Among the series, FCW34 and FCW66 were shown to inhibit MDA-MB-231 cell migration as effectively as ST3GALIII-gene knockdown did. FCW34 was shown to inhibit tumor growth, reduce angiogenesis, and delay cancer cell metastasis in animal models. Furthermore, FCW34 inhibited vessel development and suppressed angiogenic activity in transgenic zebrafish models. Our results provide clear evidence that FCW34-induced sialyltransferase inhibition reduces cancer cell metastasis by decreasing N-glycan sialylation, thus altering the regulation of talin/integrin/FAK/paxillin and integrin/NFκB signaling pathways.
Amide-to-Ester Substitution as a Strategy for Optimizing PROTAC Permeability and Cellular Activity
Bond, Adam G.,Ciulli, Alessio,Craigon, Conner,Klein, Victoria G.,Lokey, R. Scott
supporting information, p. 18082 - 18101 (2021/12/17)
Criteria for predicting the druglike properties of “beyond Rule of 5” Proteolysis Targeting Chimeras (PROTAC) degraders are underdeveloped. PROTAC components are often combined via amide couplings due to their reliability. Amides, however, can give rise t
COMPOUNDS AND METHODS FOR THE TREATMENT OF OCULAR DISORDERS
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Paragraph 00202-00203, (2020/10/27)
Described herein are compositions and methods for the treatment of ocular surface disorders including meibomian gland dysfunction, blepharitis, dry eye disease and other inflammatory/ infections disease of the anterior surface of the eye. Said compositions and methods comprise keratolytic conjugate which demonstrate keratolytic activity, and anti-inflammatory or other desirable activities. Topical administration of said compositions to the eye, ocular surface or surrounding areas provides therapeutic benefit to patients suffering from ocular surface disorders.
PHENAZINE DERIVATIVES AS ANTIMICROBIAL AGENTS
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Paragraph 000385, (2018/09/12)
The present invention provides novel phenazine derivatives, such as compounds of Formula (I) (e.g., Formulae (II) - (XIX)), and pharmaceutically acceptable salts thereof. The compounds of the invention are expected to be antimicrobial agents and may act b
New deuterated oligo(ethylene glycol) building blocks and their use in the preparation of surface active lipids possessing labeled hydrophilic tethers
Faragher, Robert J.,Schwan, Adrian L.
, p. 1371 - 1378 (2008/04/12)
(Chemical Equation Presented) For the introduction of additional analysis protocols of tethered molecules, a method is presented to prepare functionalized, deuterated oligo(ethylene glycols) from ethylene glycol-d 4. Partial oligomerization of ethylene glycol-d4 and conversion to ditosylates is accompanied by coupling reactions to prepare doubly benzyl protected oligo(ethylene glycols) with two to five repeating units. The tetramer bearing 16 deuteria was elaborated at both ends to eventually prepare 2,3-di-O-phytanyl-sn-glycerol-1-tetraethylene glycol-D,L-α-lipoic acid ester (DPTL), which bears a fully deuterated tetra(ethylene glycol) spacer group. Through linking of functionalized components, an analogue of DPTL possessing an octa(ethylene glycol) spacer group was prepared, both in deuterated and unlabeled form.
Synthesis of a heterobifunctional PEG spacer terminated with aminooxy and bromide functionality
Dicus, Christopher W.,Nantz, Michael H.
, p. 2821 - 2823 (2008/02/11)
A simple and efficient synthesis of a novel heterobifunctional polyethylene glycol (PEG) spacer is described. The PEG spacer reagent is terminated with aminooxy and bromide functionality for ease of conjugation to a variety of electrophiles and/or nucleop
