Synthesis and cytotoxicity studies of novel 2-Hydrazonylpyrido[2,3-b]pyrazin-3(4H)-ones

Guogang Zhang; Yajing Liu; Shuobing Wang; Chuan Zhou; Qingchang Huang; Ping Gong

doi:10.1002/ardp.201100103

Synthesis and cytotoxicity studies of novel 2-Hydrazonylpyrido[2,3-b]pyrazin-3(4H)-ones

Arch Pharm (Weinheim). 2012 Jan;345(1):49-56. doi: 10.1002/ardp.201100103. Epub 2011 Sep 23.

Authors

Guogang Zhang¹, Yajing Liu, Shuobing Wang, Chuan Zhou, Qingchang Huang, Ping Gong

Affiliation

¹ Key Laboratory of Original New Drugs Design and Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang, P. R. China.

PMID: 21953529
DOI: 10.1002/ardp.201100103

Abstract

In an attempt to develop potent antitumor agents, a series of novel 2-hydrazonylpyrido[2,3-b]pyrazin-3(4H)-one derivatives were designed and synthesized. All the prepared compounds were screened for their cytotoxic activities against A549, MDA-MB-231 and HT-29 cell lines in vitro. Pharmacological data indicated that five of the target compounds showed cytotoxicity against A549 cell line below a concentration of 1 µM. Compound 15g was the most potent one with IC(50) values of 0.19, 2.11 and 2.15 µM against A549, MDA-MB-231 and HT29 cell lines, respectively.

Publication types

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

MeSH terms

Antineoplastic Agents / chemical synthesis*
Antineoplastic Agents / chemistry
Antineoplastic Agents / pharmacology
Cell Survival / drug effects
Chemistry Techniques, Synthetic
Dose-Response Relationship, Drug
Drug Design*
HT29 Cells
Humans
Inhibitory Concentration 50
Molecular Structure
Pyrazines / chemical synthesis*
Pyrazines / chemistry
Pyrazines / pharmacology
Structure-Activity Relationship

Substances

Antineoplastic Agents
Pyrazines