Synthesis of 1,2,3,4-Tetrahydroeudistomin U Derivatives and Preliminary In Vitro. Antitumor Evaluation

Jianbin Zheng School of Pharmacy, Fudan University, Shanghai, People's Republic of China; School of Pharmacy, East China University of Science and Technology, Shanghai, People's Republic of China

Zhiwen Zhang School of Pharmacy, Fudan University, Shanghai, People's Republic of China

Lingling Zhao School of Pharmacy, Fudan University, Shanghai, People's Republic of China

Xianyi Sha School of Pharmacy, Fudan University, Shanghai, People's Republic of China

Xiaochun Dong School of Pharmacy, Fudan University, Shanghai, People's Republic of China

Ren Wen School of Pharmacy, Fudan University, Shanghai, People's Republic of China; School of Pharmacy, East China University of Science and Technology, Shanghai, People's Republic of China

Figures & data

Figure 1 Structures of eudistomin U (1) and 1,2,3,4-tetrahydroeudistomin U derivatives (2a-– 2c).

Figure 2 The synthetic route of compounds 5–28. Reagents and conditions: (a) PhH, reflux (95%); (b) TFA, CHCl₃, rt (58%); (c) alkyl halides, K₂CO₃, KI, DMF or carbonyl halides, Et₃N, CH₂Cl₂.

Figure 2 The synthetic route of compounds 5–28. Reagents and conditions: (a) PhH, reflux (95%); (b) TFA, CHCl3, rt (58%); (c) alkyl halides, K2CO3, KI, DMF or carbonyl halides, Et3N, CH2Cl2.

Table 1 The yield, structure identification and bioassay data of 2-substituted 1,2,3,4-tetrahydroeudistomin U derivatives.

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Synthesis of 1,2,3,4-Tetrahydroeudistomin U Derivatives and Preliminary In Vitro. Antitumor Evaluation

Table 1 The yield, structure identification and bioassay data of 2-substituted 1,2,3,4-tetrahydroeudistomin U derivatives.

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Synthesis of 1,2,3,4-Tetrahydroeudistomin U Derivatives and Preliminary In Vitro. Antitumor Evaluation

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Table 1 The yield, structure identification and bioassay data of 2-substituted 1,2,3,4-tetrahydroeudistomin U derivatives.

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