N'-(取代亚苄基)-2-(苯并[d]恶唑-3(2H)-基)乙酰肼衍生物的合成、抗菌及抗癌活性评价

Synthesis, antimicrobial and anticancer evaluation of N'-(substituted benzylidene)-2-(benzo[d]oxazol-3(2H)-yl)acetohydrazide derivatives.

作者信息

Rohilla P, Deep A, Kamra M, Narasimhan B, Ramasamy K, Mani V, Mishra R K, Lim S M

机构信息

Department of Pharmaceutical Chemistry, Hindu College of Pharmacy, Sonepat, India.

Faculty of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, India.

出版信息

Drug Res (Stuttg). 2014 Oct;64(10):505-9. doi: 10.1055/s-0034-1368720. Epub 2014 Jul 3.

DOI:10.1055/s-0034-1368720

PMID:24992500

Abstract

A series of N'-(substituted benzylidene)-2-(benzo[d]oxazol-3(2H)-yl)acetohydrazide derivatives was synthesized and evaluated for its in vitro antimicrobial and anticancer activities. Antimicrobial activity results revealed that compound 12 was found to be the most potent antimicrobial agent. Results of anticancer study indicated that the synthesized compounds exhibited average anticancer potential. Compound 7 (IC 50 =3.12 µM) and compound 16 (IC 50 =2.88 µM) were found to be most potent against breast cancer (MCF7) cell lines. In conclusion, compound 12 and 16 have the potential to be selected as lead compound for the developing of novel antimicrobial and anticancer agents respectively.

摘要

合成了一系列N'-(取代亚苄基)-2-(苯并[d]恶唑-3(2H)-基)乙酰肼衍生物，并对其体外抗菌和抗癌活性进行了评估。抗菌活性结果表明，化合物12是最有效的抗菌剂。抗癌研究结果表明，合成的化合物具有平均抗癌潜力。发现化合物7(IC50 = 3.12 μM)和化合物16(IC50 = 2.88 μM)对乳腺癌(MCF7)细胞系最有效。总之，化合物12和16分别有潜力被选为开发新型抗菌剂和抗癌剂的先导化合物。