Design and synthesis of a bis(cycloisodityrosine) analogue of RA-VII, an antitumor bicyclic hexapeptide.

Lee JE; Hitotsuyanagi Y; Nakagawa Y; Kato S; Fukaya H; Takeya K

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Design and synthesis of a bis(cycloisodityrosine) analogue of RA-VII, an antitumor bicyclic hexapeptide.

机译：设计和合成RA-VII（一种抗肿瘤双环六肽）的双（环异酪氨酸）类似物。

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An analogue of an antitumor bicyclic hexapeptide RA-VII was prepared, in which the Ala-2 and Tyr-3 residues of RA-VII were replaced by a cycloisodityrosine unit. In the crystalline state, the peptide backbone structures and the side-chain conformations at Tyr-3, Tyr-5, and Tyr-6 of this analogue and of RA-II were very similar. This analogue, however, showed much weaker cytotoxicity against P-388 leukemia cells than parent RA-VII.

机译：制备了抗肿瘤双环六肽RA-VII的类似物，其中RA-VII的Ala-2和Tyr-3残基被环异酪氨酸单元取代。在结晶状态下，该类似物和RA-II的肽骨架结构和Tyr-3，Tyr-5和Tyr-6的侧链构象非常相似。然而，该类似物对P-388白血病细胞的毒性比亲本RA-VII弱得多。

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来源
《Bioorganic and Medicinal Chemistry Letters》 |2008年第24期|共4页
作者
Lee JE; Hitotsuyanagi Y; Nakagawa Y; Kato S; Fukaya H; Takeya K;
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正文语种 eng
中图分类药学;生物化学;
关键词
RA VII; Tyrosine; Cytotoxicity; Vertebral column; 酪氨酸;

机译：RA VII;Tyrosine;Cytotoxicity;Vertebral column;酪氨酸;

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专利

1. Design and synthesis of a bis(cycloisodityrosine) analogue of RA-VII, an antitumor bicyclic hexapeptide. [J] . Lee JE, Hitotsuyanagi Y, Nakagawa Y, Bioorganic and Medicinal Chemistry Letters . 2008,第24期

机译：设计和合成RA-VII（一种抗肿瘤双环六肽）的双（环异酪氨酸）类似物。
2. Aza-cycloisodityrosine analogue of RA-VII, an antitumor bicyclic hexapeptide [J] . HitotsuyanagiY., MiyazawaA., HinosawaT.-A., Bioorganic and Medicinal Chemistry Letters . 2013,第24期

机译：RA-VII（抗肿瘤双环六肽）的氮杂-环异酪氨酸类似物
3. Aza-cycloisodityrosine analogue of RA-VII, an antitumor bicyclic hexapeptide [J] . HitotsuyanagiY., MiyazawaA., HinosawaT.-A., Bioorganic and Medicinal Chemistry Letters . 2013,第24期

机译：RA-VII（抗肿瘤双环六肽）的氮杂-环异酪氨酸类似物
4. Design, Synthesis and Evaluation of Antitumor Activity against Human Cancer Cell Lines,Sansalvamide Analogues [C] . Xiaoli Zhen, Yihua Yang, Junzhang Li, Chinese international peptide symposium . 2011

机译：抗肿瘤性抗肿瘤性抗肿瘤活性的设计，合成与评价，桑拉酰胺类似物
5. Part I. Asymmetric synthesis of bicyclic analogues of risedronate as molecular probes of the mechanism of action of bisphosphonate antiosteoporotic drugs and potentially more efficacious antiosteoporotic agents. Part II. Facile preparation and functionalization of chiral stabilized ylides from common chiral auxiliaries using the Bestmann ylide and their use in Wittig reactions. Part III. Asymmetric organocatalysis: 1. An investigation of alpha-hydroxylation of aldehydes; 2. Synthesis of a novel camphor-based alpha-aminotetrazole organocatalyst. [D] . Song, Xinyi. 2007

机译：第一部分：利塞膦酸盐双环类似物的不对称合成，作为双膦酸盐类抗骨质疏松药和潜在更有效的抗骨质疏松药作用机理的分子探针。第二部分使用Bestmann内酯从常见手性助剂轻松制备和官能化手性稳定化的叶基及其在Wittig反应中的用途。第三部分不对称有机催化：1.醛的α-羟基化研究； 2.合成新的基于樟脑的α-氨基四唑有机催化剂。
6. Design synthesis and biological activity of bicyclic radester analogues as Hsp90 inhibitors [O] . Vinod D. Jadhav, Adam S. Duerfeldt, Brian S. J. Blagg -1

机译：双环射兰类似物作为HSP90抑制剂的设计合成和生物活性
7. Synthesis of Gly-1RA-VII, Gly-2RA-VII and Gly-4RA-VII. Glycine-containing Analogues of RA-VII, an Antitumor Bicyclic Hexapeptide from Rubia Plants [O] . -1

机译：GLY-1 RA-VII，GLY-2 RA-VII和GLY-4 RA-VII的合成。 Rabia植物的含甘氨酸类似Ra-VII的类似物的抗肿瘤双环肽

Design and synthesis of a bis(cycloisodityrosine) analogue of RA-VII, an antitumor bicyclic hexapeptide.

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