Synthesis of new simplified hemiasterlin derivatives with α,β-unsaturated carbonyl moiety

TheC.P.; ThiT.A.D.; HoangT.P.; NgoQ.A.; DoanD.T.; ThiT.H.N.; ThiT.P.; ThiT.H.V.; JeanM.; VanDeWegheP.; VanT.N.

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Synthesis of new simplified hemiasterlin derivatives with α,β-unsaturated carbonyl moiety

机译：用α，β-不饱和羰基部分合成新的简化半岛衍生物

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In this Letter, we report a convenient and efficient method for the synthesis of new simplified derivatives of hemiasterlin in which the α,α-dimethylbenzylic moiety A is replaced by α,β- unsaturated aryl groups as Michael acceptor. Most of these derivatives have a strong cytotoxic activity on three human tumor cell lines (KB, Hep-G2 and MCF7). Analogs 17b and 17f showed a high cytotoxicity against KB and Hep-G2 cancer cell lines comparable to paclitaxel and ellipticine.

机译：在这封信中，我们报告了一种方便，高效的方法，用于合成半岛林的新型简化衍生物，其中α，α-二甲基苄基部分A被α，β-不饱和芳基作为迈克尔受体所取代。大多数这些衍生物对三种人肿瘤细胞系（KB，HEP-G2和MCF7）具有强烈的细胞毒性活性。类似物17b和17f显示出对Kb和Hep-g2癌细胞系的高细胞毒性，与紫杉醇和椭圆形相当。

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来源
《Bioorganic and Medicinal Chemistry Letters》 |2014年第10期|共3页
作者
TheC.P.; ThiT.A.D.; HoangT.P.; NgoQ.A.; DoanD.T.; ThiT.H.N.; ThiT.P.; ThiT.H.V.; JeanM.; VanDeWegheP.; VanT.N.;
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作者单位

Institute of Chemistry-Vietnam Academy of Science and Technology 18 Hoang Quoc Viet Cau Giay;

Institute of Chemistry-Vietnam Academy of Science and Technology 18 Hoang Quoc Viet Cau Giay;

Institute of Chemistry-Vietnam Academy of Science and Technology 18 Hoang Quoc Viet Cau Giay;

Institute of Chemistry-Vietnam Academy of Science and Technology 18 Hoang Quoc Viet Cau Giay;

Institute of Chemistry-Vietnam Academy of Science and Technology 18 Hoang Quoc Viet Cau Giay;

Institute of Chemistry-Vietnam Academy of Science and Technology 18 Hoang Quoc Viet Cau Giay;

Institute of Chemistry-Vietnam Academy of Science and Technology 18 Hoang Quoc Viet Cau Giay;

Institute of Chemistry-Vietnam Academy of Science and Technology 18 Hoang Quoc Viet Cau Giay;

Equipe Produits Naturels Synthèses et Chimie Médicinale (PNSCM) Université de Rennes 1 2 Avenue;

Equipe Produits Naturels Synthèses et Chimie Médicinale (PNSCM) Université de Rennes 1 2 Avenue;

Institute of Chemistry-Vietnam Academy of Science and Technology 18 Hoang Quoc Viet Cau Giay;

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正文语种 eng
中图分类药学;
关键词
Cytotoxicity; Hemiasterlin; Tripeptides;

机译：细胞毒性;Hemiaysterlin;三肽;

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专利

1. Synthesis of new simplified hemiasterlin derivatives with α,β-unsaturated carbonyl moiety [J] . TheC.P., ThiT.A.D., HoangT.P., Bioorganic and Medicinal Chemistry Letters . 2014,第10期

机译：用α，β-不饱和羰基部分合成新的简化半岛衍生物
2. Synthesis of new simplified hemiasterlin derivatives with α,β-unsaturated carbonyl moiety [J] . TheC.P., ThiT.A.D., HoangT.P., Bioorganic and Medicinal Chemistry Letters . 2014,第10期

机译：具有α，β-不饱和羰基部分的新型简化半胱氨酸衍生物的合成
3. Synthesis and cytotoxic effect of pregnenolone derivatives with one or two alpha,beta-unsaturated carbonyls and an ester moiety at C-21 or C-3 [J] . Chavez-Riveros Alejandra, Cruz Noriega Abigail, Ramirez Apan Maria Teresa, Steroids: An International Journal . 2018,第期

机译：妊娠蛋白衍生物用一个或两个α，β-不饱和羰基和C-21或C-3酯部分的合成和细胞毒性作用
4. SYNTHESIS OF NITROGEN-CONTAINING CARBOHYDRATE DERIVATIVES BEARING AN α,β-UNSATURATED CARBONYL SYSTEM [C] . Xavier N. M., Rauter A. P. International Carbohydrate Symposium . 2013

机译：含氮碳水化合物衍生物的合成α，β-不饱和羰基体系
5. Development of palladium catalyzed methodology to synthesize alpha-substituted alpha,beta-unsaturated carbonyl derivatives. [D] . Liao, Baiqiao. 1999

机译：钯催化方法的发展，以合成α-取代的α，β-不饱和羰基衍生物。
6. Gold-Catalyzed Highly Regioselective Oxidation of C-C Triple Bonds Without Acid Additives: Propargyl Moieties as Masked αβ-Unsaturated Carbonyls [O] . Biao Lu, Chaoqun Li, Liming Zhang -1

机译：金催化的C-C叁键的高度选择性氧化没有酸添加剂：炔部分作为屏蔽αβ不饱和羰基
7. Synthesis of new simplified hemiasterlin derivatives with α,β-unsaturated carbonyl moiety. [O] . The, Chinh Pham, Thi, Tuyet Anh Dang, Hoang, Thi Phuong, 2014

机译：合成具有α，β-不饱和羰基部分的新的简化的半甾醇衍生物。

Synthesis of new simplified hemiasterlin derivatives with α,β-unsaturated carbonyl moiety

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