17626-02-7Relevant articles and documents
COLLECTIONS OF PEPTIDES, PEPTIDE AGENTS, AND METHODS OF USE THEREOF
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Paragraph 0360-0361, (2020/03/15)
The present disclosure provides powerful technologies for the development, production, characterization, and/or use of stapled peptide compositions. Among other things, the present disclosure provides strategies for defining amino acid sequences particularly amenable or useful for stapling, as well as technologies, reagents, and systems for developing, producing, characterizing, and/or using stapled peptides having such amino acid sequences.
Total syntheses of the dipyrrolobenzoquinone (+)-terreusinone enabled by an evaluation of 4-methylpent-1-yn-3-ols in the Larock indole synthesis
Wang, Christy,Sperry, Jonathan
, p. 4563 - 4577 (2013/06/27)
The Larock indolization between 4-methylpent-1-yn-3-ols (alkynols) and ortho-bromo and ortho-iodoanilines has been studied. Although the unprotected alkynol was an unviable substrate for the annulation reaction, protected derivatives did proceed to the indole products. Interestingly, this reaction does not appear to occur by the widely accepted mechanism for the Larock indolization of internal alkynes, but by the initial formation of a cross-coupled arylalkyne followed by 5-endo-dig cyclization. Importantly, when a chiral alkynol is used, the stereochemical integrity is retained in the indole product. Although this methodology could not be successfully extended to a double Larock indolization approach to terreusinone, two separate total syntheses evolved from these studies: A bidirectional, double Sonogashira-hydroamination approach and a one-pot Larock indolization- Sonogashira coupling followed by hydroamination. This work has not only confirmed the gross structure and absolute configuration of the photoprotecting natural product terreusinone, but also uncovered several novel applications of known reaction conditions that should find broad applications in the field of heteroaromatic construction.
Design, synthesis, and cytotoxicity of indolizinoquinoxaline-5,12-dione derivatives, novel DNA topoisomerase IB inhibitors
Shen, De-Qing,Wu, Ning,Li, Yan-Ping,Wu, Zu-Ping,Zhang, Hong-Bin,Huang, Zhi-Shu,Gu, Lian-Quan,An, Lin-Kun
experimental part, p. 1116 - 1121 (2011/03/21)
A series of new indolizinoquinoxaline-5,12-dione derivatives were designed and synthesized via a heterocyclization reaction of 6,7-dichloroquinoxaline-5,8- dione with active methylene reagents and pyridine derivatives. The synthesized compounds exhibited significant activity to inhibit the growth of four human tumour cell lines, including lung adenocarcinoma cell, large-cell lung carcinoma cell, breast carcinoma cell, and ardriamycin-resistant breast carcinoma cell at micromolar range. These compounds were also investigated for their inhibition to DNA topoisomerase IB activity. The results indicated that the indolizinoquinoxaline-5,12-dione structure might be a potential pharmacophore in anti-cancer drug design.