Synthesis of New Simplified and Racemic Hemiasterlin Derivatives with Extremely High Cytotoxicity

Author:

Chinh Pham The1,Anh Đang Thi Tuyet23,Quynh Duong Huong3,Giang Le Nhat Thuy2,Thanh Nguyen Ha2,Thanh Hoang Thi1,Tam Khieu Thi1,Tham Pham Thi4,Anh Le Thị Tu2,Phuong Hoang Thi2,Van Tuyen Nguyen23,Van Kiem Phan35

Affiliation:

1. Thai Nguyen University of Sciences, Tan Thinh, Thai Nguyen, Vietnam

2. Insitute of Chemistry, Vietnam Academy of Science and Technology (VAST), 18 Hoang Quoc Viet, Cau Giay, Hanoi, Vietnam

3. Graduate Universty of Science and Technology, VAST, 18- Hoang Quoc Viet, Cau Giay, Hanoi, Vietnam

4. Hanoi University of Industry, Number 298, Cau Dien, Bac Tu Liem, Hanoi, Vietnam

5. Institute of Marine Biochemistry, VAST, 18 Hoang Quoc Viet, Cau Giay, Hanoi, Vietnam

Abstract

Hemiasterlin is a potent antimitotic agent acting through inhibition of microtubule depolymerization. For this reason, the synthesis of new hemiasterlin derivatives has attracted a lot of interest in the organic chemistry community recently. In this paper, the synthesis and evaluation of the cytotoxicity of new simplified and racemic hemiasterlin derivatives were reported. All of the synthesized analogues were evaluated in vitro for cytotoxic activity against four human cell lines (KB, Hep-G2, LU and MCF7). Most of these analogues possess a strong cytotoxic activity on two human cancer cell lines (KB and Hep-G2) and very weak activity on LU and MCF7 cell lines.

Publisher

SAGE Publications

Subject

Complementary and alternative medicine,Plant Science,Drug Discovery,Pharmacology,General Medicine

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