Synthesis, Biological Evaluation, and Docking Studies of New 2-Furylbenzimidazoles as Anti- Angiogenic Agents: Part II

被引：19

作者：

Temirak, Ahmed ^{[1
]}

Shaker, Yasser M. ^{[1
]}

Ragab, Fatma A. F. ^{[2
]}

Ali, Mamdouh M. ^{[3
]}

Soliman, Salwa M. ^{[4
]}

Mortier, Jeremie ^{[4
,5
]}

Wolber, Gerhard ^{[4
]}

Ali, Hamed I. ^{[6
,7
]}

El Diwani, Hoda I. ^{[1
]}

机构：

[1] Natl Res Ctr, Div Pharmaceut & Drug Ind, Dept Chem Nat & Microbial Prod, Cairo 12622, Egypt

[2] Cairo Univ, Fac Pharm, Dept Pharmaceut Chem, Giza, Egypt

[3] Natl Res Ctr, Div Genet Engn & Biotechnol, Dept Biochem, Cairo 12622, Egypt

[4] Free Univ Berlin, Inst Pharm, Dept Pharmaceut Chem, Berlin, Germany

[5] Free Univ Berlin, Dept Organ Chem, Berlin, Germany

[6] Texas A&M Hlth Sci Ctr, Irma Lerma Rangel Coll Pharm, Dept Pharmaceut Sci, Round Rock, TX USA

[7] Helwan Univ, Fac Pharm, Dept Pharmaceut Chem, Cairo, Egypt

来源：

ARCHIV DER PHARMAZIE | 2014年 / 347卷 / 04期

关键词：

Angiogenesis; Cytotoxicity; 2-(2-Furyl)-1H-benzimidazoles; Molecular modeling; Vascular endothelial growth factor (VEGF); GROWTH-FACTOR RECEPTOR; TYROSINE KINASE INHIBITORS; TUMOR ANGIOGENESIS; VEGF; MECHANISMS; DERIVATIVES; LIGANDS; CANCER;

D O I：

10.1002/ardp.201300356

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The 2-(5-methyl-2-furyl)-1H-benzimidazole moiety has shown promising activity against vascular endothelial growth factor (VEGF)-induced angiogenesis. In part I of this study, we have synthesized new analogs and tested their anti-angiogenic potentials. Here, we continue our previous study with different new analogs. Some compounds show promising cytotoxic activity against the human breast cancer cell line MCF-7, with IC50 in the range of 7.80-13.90 mu g/mL, and exhibited remarkable in vitro inhibition against VEGF in the MCF-7 cancer cell line, with 95-98% of inhibition in comparison to tamoxifen as reference (IC50: 8.00 mu g/mL, % of inhibition=98%). Additionally, a molecular docking study was carried out to gain insight into plausible binding modes and to understand the structure-activity relationships of the synthesized compounds.

引用

页码：291 / 304

页数：14

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