3674-06-4Relevant articles and documents
Synthesis of pyrimidine nucleoside and amino acid conjugates
Koplūnait?, Martyna,Butkut?, Kamil?,Me?kys, Rolandas,Taurait?, Daiva
, (2020/11/13)
The synthesis of novel pyrimidine nucleoside bioconjugates with amino acids is presented. The N4-amino acid-acylated 2′-deoxycytidine analogues, modified with various amino acids, were synthesized using a three-step synthesis and obtained in moderate overall yields. Novel amino acid-alkylated 2′-deoxycytidine derivatives were obtained during the rearrangement of amino acid-acylated derivatives that occurred during Boc deprotection.
The Cooperative Effect of Both Molecular and Supramolecular Chirality on Cell Adhesion
Liu, Jinying,Yuan, Feng,Ma, Xiaoyu,Auphedeous, Dang-i Y.,Zhao, Changli,Liu, Chuntai,Shen, Changyu,Feng, Chuanliang
supporting information, p. 6475 - 6479 (2018/05/08)
Although helical nanofibrous structures have great influence on cell adhesion, the role played by chiral molecules in these structures on cells behavior has usually been ignored. The chirality of helical nanofibers is inverted by the odd–even effect of methylene units from homochiral l-phenylalanine derivative during assembly. An increase in cell adhesion on left-handed nanofibers and weak influence of cell behaviors on right-handed nanofibers are observed, even though both were derived from l-phenylalanine derivatives. Weak and negative influences on cell behavior was also observed for left- and right-handed nanofibers derived from d-phenylalanine, respectively. The effect on cell adhesion of single chiral molecules and helical nanofibers may be mutually offset.
New Class of Selective Estrogen Receptor Degraders (SERDs): Expanding the Toolbox of PROTAC Degrons
Wang, Lucia,Guillen, Valeria S.,Sharma, Naina,Flessa, Kevin,Min, Jian,Carlson, Kathryn E.,Toy, Weiyi,Braqi, Sara,Katzenellenbogen, Benita S.,Katzenellenbogen, John A.,Chandarlapaty, Sarat,Sharma, Abhishek
supporting information, p. 803 - 808 (2018/07/21)
An effective endocrine therapy for breast cancer is to selectively and effectively degrade the estrogen receptor (ER). Up until now, there have been largely only two molecular scaffolds capable of doing this. In this study, we have developed new classes of scaffolds that possess selective estrogen receptor degrader (SERD) and ER antagonistic properties. These novel SERDs potently inhibit MCF-7 breast cancer cell proliferation and the expression of ER target genes, and their efficacy is comparable to Fulvestrant. Unlike Fulvestrant, the modular protein-targeted chimera (PROTAC)-type design of these novel SERDs should allow easy diversification into a library of analogs to further fine-tune their pharmacokinetic properties including oral availability. This work also expands the pool of currently available PROTAC-type scaffolds that could be beneficial for targeted degradation of various other therapeutically important proteins.
