Eco-Friendly Synthesis, Characterization and Biological Evaluation of Some Novel Pyrazolines Containing Thiazole Moiety as Potential Anticancer and Antimicrobial Agents

被引：58

作者：

Edrees, Mastoura M. ^{[1
,2
]}

Abu-Melha, Sraa ^{[1
]}

Saad, Amirah M. ^{[3
]}

Kheder, Nabila A. ^{[3
,4
]}

Gomha, Sobhi M. ^{[4
]}

Muhammad, Zeinab A. ^{[2
]}

机构：

[1] King Khalid Univ, Dept Chem, Fac Sci, Abha 61413, Saudi Arabia

[2] Natl Org Drug Control & Res NODAR, Dept Organ Chem, Giza 12311, Egypt

[3] King Khalid Univ, Dept Pharmaceut Chem, Fac Pharm, Abha 61441, Saudi Arabia

[4] Cairo Univ, Dept Chem, Fac Sci, Giza 12613, Egypt

来源：

MOLECULES | 2018年 / 23卷 / 11期

关键词：

pyrazolines; thiazoles; hydrazonoyl halides; antimicrobial activity; anticancer activity; ONE-POT SYNTHESIS; EFFICIENT SYNTHESIS; IN-VITRO; DERIVATIVES; GROWTH; INHIBITION; ACTIVATORS; SOLVENT;

D O I：

10.3390/molecules23112970

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The one-pot synthesis of a series of pyrazoline derivatives containing the bioactive thiazole ring has been performed through a 1,3-dipolar cycloaddition reaction of N-thiocarbamoylpyrazoline and different hydrazonoyl halides or alpha-haloketonesin the presence of DABCO (1,4-diazabicyclo[2.2.2] octane) as an eco-friendly catalyst using the solvent-drop grinding method. The structure of the synthesized compounds was elucidated using elemental and spectroscopic analyses (IR, NMR, and Mass). The activity of these compounds against human hepatocellular carcinoma cell line (HepG2) was tested and the results showed that the pyrazoline 11f, which has a fluorine substituent, is the most active. The antimicrobial activities of the newly synthesized compounds were determined against two fungi and four bacterial strains, and the results indicated that some of the newly synthesized pyrazolines are more potent than the standard drugs against test organisms.

引用

页数：13

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