Format

Send to

Choose Destination
See comment in PubMed Commons below
Eur J Med Chem. 2013 Sep;67:293-301. doi: 10.1016/j.ejmech.2013.06.055. Epub 2013 Jul 4.

Design and synthesis of novel quinazoline nitrogen mustard derivatives as potential therapeutic agents for cancer.

Author information

1
Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, PR China.

Abstract

Thirteen novel quinazoline nitrogen mustard derivatives were designed, synthesized and evaluated for their anticancer activities in vitro and in vivo. Cytotoxicity assays were carried out in five cancer cell lines (HepG2, SH-SY5Y, DU145, MCF-7 and A549) and one normal human cell line (GES-1), in which compound 22b showed very low IC50 to HepG2 (the IC50 value is 3.06 μM), which was lower than Sorafenib. Compound 22b could inhibit cell cycle at S and G2/M phase and induce cell apoptosis. In the HepG2 xenograft model, 22b exhibited significant cancer growth inhibition with low host toxicity in vivo.

KEYWORDS:

(3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide; 4-dimethylaminopyridine; A549; Anticancer; Apoptosis; Cell cycle; DMAP; DU145; FBS; HCC; HepG2; MCF-7; MTT; Nitrogen mustard; PBS; PI; Quinazoline; RNase A; SH-SY5Y; Xenograft model; fetal bovine serum; hepatic carcinoma; human alveolar adenocarcinoma cell line; human breast cancer cell line; human liver carcinoma cell line; human neuroblastoma cell line; human prostate cancer cell lines; phosphate buffer solution; propidium iodide; ribonuclease A

PMID:
23871909
DOI:
10.1016/j.ejmech.2013.06.055
[Indexed for MEDLINE]
PubMed Commons home

PubMed Commons

0 comments
How to join PubMed Commons

    Supplemental Content

    Full text links

    Icon for Elsevier Science
    Loading ...
    Support Center