Synthesis and Biological Evaluation of Some Novel Thiazole-Based Heterocycles as Potential Anticancer and Antimicrobial Agents

被引:61
|
作者
Abu-Melha, Sraa [1 ]
Edrees, Mastoura M. [1 ,2 ]
Salem, Heba H. [3 ,4 ]
Kheder, Nabila A. [5 ,6 ]
Gomha, Sobhi M. [5 ,7 ]
Abdelaziz, Mohamad R. [8 ]
机构
[1] King Khalid Univ, Dept Chem, Fac Sci, Abha 61413, Saudi Arabia
[2] NODCAR, Dept Organ Chem, Giza 12311, Egypt
[3] King Khalid Univ, Fac Pharm, Abha 61441, Saudi Arabia
[4] Cairo Univ, Dept Biochem, Fac Pharm, Cairo 11562, Egypt
[5] Cairo Univ, Dept Chem, Fac Sci, Giza 12613, Egypt
[6] King Khalid Univ, Dept Pharmaceut Chem, Fac Pharm, Abha 61441, Saudi Arabia
[7] Islamic Univ Almadinah Almonawara, Dept Chem, Fac Sci, Almadinah Almonawara 42351, Saudi Arabia
[8] MIU Univ, Dept Pharmaceut Chem, Fac Pharm, Cairo 19648, Egypt
关键词
thiazoles; hydrazonoyl halides; hepatoprotective activity; anticancer activity; antimicrobial activity; IN-VITRO; DERIVATIVES; CHALCONES; SOLVENT;
D O I
10.3390/molecules24030539
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
A novel series of thiazole-based heterocycles was synthesized using 1,3-dipolar cycloaddition reactions in the presence of chitosan-grafted-poly(vinylpyridine) as an eco-friendly biopolymeric basic catalyst. The molecular structure of the synthesized compounds was illustrated by spectroscopic and elemental analysis. Various in vitro biological assays were performed to explore the potential antitumor, antimicrobial and hepatoprotective activities of the newly synthesized compounds. The cytotoxic activities were assessed against human hepatocellular carcinoma (HepG-2), colorectal carcinoma (HCT-116) and breast cancer (MCF-7) cell lines and results revealed that all compounds displayed antitumor activities with the chlorine-containing derivatives, 11c and 6g, being the most potent. The majority of the tested thiazole derivatives exhibited satisfactory antibacterial activity towards the used gram positive and gram-negative bacterial species. Moreover, many derivatives showed weak hepatoprotective activity against CCl4-induced hepatotoxicity.
引用
收藏
页数:15
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