Synthesis of new bioisosteric hemiasterlin analogues with extremely high cytotoxicity

[Display omitted] In this Letter, the synthesis and the evaluation of the cytotoxicity of new hemiasterlin analogues were reported. The indole moiety was replaced respectively by benzofurane, naphthalene and 4-bromobenzene groups. Most of these derivatives possess strong cytotoxic activity on two hu...

Full description

Saved in:
Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2014-11, Vol.24 (22), p.5216-5218
Main Authors: Anh Dang Thi, Tuyet, Pham The, Chinh, Ngo, Quoc Anh, Ha Vu Thi, Thu, Dung Nguyen, Tien, Tien Doan, Duy, Ba Thi, Cham, Jean, M., van de Weghe, P., Nguyen Van, Tuyen
Format: Article
Language:English
Subjects:
Cell Death - drug effects
Chemical Sciences
Cytotoxicity
Cytotoxins - chemistry
Cytotoxins - toxicity
Drug Screening Assays, Antitumor - methods
Hemiasterlin
Hep G2 Cells
Humans
Medicinal Chemistry
Oligopeptides - chemistry
Oligopeptides - toxicity
Stereoisomerism
Tripeptides
Unnatural hemiasterlin
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:[Display omitted] In this Letter, the synthesis and the evaluation of the cytotoxicity of new hemiasterlin analogues were reported. The indole moiety was replaced respectively by benzofurane, naphthalene and 4-bromobenzene groups. Most of these derivatives possess strong cytotoxic activity on two human tumour cell lines (KB and Hep-G2), and some analogues showed comparable cytotoxic activity to that observed for paclitaxel and ellipticine, against KB and Hep-G2 cancer cell lines.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2014.09.065