Syntheses of novel β-carboline derivatives and the activities against five tumor-cell lines

Bing Bai; Xing-Yao Li; Li Liu; Yan Li; Hua-Jie Zhu

doi:10.1016/j.bmcl.2013.11.076

Syntheses of novel β-carboline derivatives and the activities against five tumor-cell lines

Bioorg Med Chem Lett. 2014 Jan 1;24(1):96-8. doi: 10.1016/j.bmcl.2013.11.076. Epub 2013 Dec 4.

Authors

Bing Bai¹, Xing-Yao Li², Li Liu³, Yan Li², Hua-Jie Zhu⁴

Affiliations

¹ Chinese Center for Chirality, The Key Laboratory of Medicinal Chemistry and Molecular Diagnostics, Department of Chemistry and Chemical Engineering, Hebei University, Baoding 071002, China; School of Food and Biological Engineering, Zhengzhou University of Light Industry, Zhengzhou 450002, China.
² The State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, CAS, Kunming 650204, China.
³ Chinese Center for Chirality, The Key Laboratory of Medicinal Chemistry and Molecular Diagnostics, Department of Chemistry and Chemical Engineering, Hebei University, Baoding 071002, China.
⁴ Chinese Center for Chirality, The Key Laboratory of Medicinal Chemistry and Molecular Diagnostics, Department of Chemistry and Chemical Engineering, Hebei University, Baoding 071002, China; The State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, CAS, Kunming 650204, China. Electronic address: hjzhu@mail.kib.ac.cn.

PMID: 24345445
DOI: 10.1016/j.bmcl.2013.11.076

Abstract

A series of β-carbolines possessing the aryl group at C-1 position has been synthesized from tryptophan. The newly synthesized compounds were screened for their in vitro anticancer activity against various human cancer cell lines by MTT assay. Some of them exhibited anticancer activity with IC50 values lower than 10μM outdistanced the cisplatin level. Structure-activity relationship reveals that the alcohol substituents at C-3 position played an important role in inhibition activity.

Keywords: Cytotoxic activity; MTT; Structure–activity relationship; β-Carbolines.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Antineoplastic Agents / chemical synthesis
Antineoplastic Agents / chemistry
Antineoplastic Agents / pharmacology*
Carbolines / chemical synthesis
Carbolines / chemistry
Carbolines / pharmacology*
Cell Line, Tumor
Cell Proliferation / drug effects
Cell Survival / drug effects
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
HL-60 Cells
Humans
Inhibitory Concentration 50
MCF-7 Cells
Molecular Structure
Neoplasms / pathology*
Structure-Activity Relationship

Substances

Antineoplastic Agents
Carbolines