Design, synthesis, and biological evaluation of 4-H pyran derivatives as antimicrobial and anticancer agents

被引：0

作者：

Reddy, Thatikonda Narendar ^{[1
,4
]}

Ravinder, Mettu ^{[1
]}

Bikshapathi, Raktani ^{[1
]}

Sujitha, Pombala ^{[2
]}

Kumar, C. Ganesh ^{[2
]}

Rao, Vaidya Jayathirtha ^{[1
,3
]}

机构：

[1] CSIR Indian Inst Chem Technol, Crop Protect Chem Div, Uppal Rd, Hyderabad 500007, Andhra Pradesh, India

[2] CSIR Indian Inst Chem Technol, Med Chem & Pharmacol Div, Uppal Rd, Hyderabad 500007, Andhra Pradesh, India

[3] CSIR Indian Inst Chem Technol, Acad Sci & Innovat Res, Uppal Rd, Hyderabad 500007, Andhra Pradesh, India

[4] Acad Sinica, Genom Res Ctr, 128 Acad Rd,Sect 2, Taipei 115, Taiwan

来源：

MEDICINAL CHEMISTRY RESEARCH | 2017年 / 26卷 / 11期

关键词：

4-H pyran; Baylis-Hillman reaction; Antibacterial activity; Antifungal activity; Cytotoxicity; BAYLIS-HILLMAN REACTION; THROUGHPUT SCREENING ASSAY; ENANTIOSELECTIVE SYNTHESIS; INHIBITORS; DISCOVERY; ADDUCTS; SERIES; 4-ARYL-4H-CHROMENES; 2-AMINO-4H-PYRANS; ZANAMIVIR;

D O I：

10.1007/s00044-017-1982-y

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of pyran derivatives (5-27) were synthesized in good yields by utilizing Baylis-Hillman chemistry and were further investigated for their in vitro anticancer, antibacterial, and antifungal activities. Most of the tested compounds exhibited promising antibacterial activity as compared to the standard towards Gram-positive bacterial strains. The compounds 5-7, 11-13, and 17-19 displayed two-fold higher activity whereas compound 21 showed four-fold higher antibacterial activity against Staphylococcus aureus MTCC 96 as compared to the standard Neomycin. Some of these compounds exhibited moderate antifungal activity against all the tested fungal strains. Two compounds 16 and 23 showed promising anticancer activity against selected four human cancer cell lines such as A549, DU145, HeLa, and MCF7.

引用

页码：2832 / 2844

页数：13

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