Synthesis of New Carbazole-Thiazole Analogues and Evaluating their Anticancer Activity

被引:1
|
作者
Elmorsy, Mohamed R. [1 ]
Eltoukhi, Mariam [1 ]
Fadda, Ahmed A. [1 ]
Abdel-Latif, Ehab [1 ]
Abdelmoaz, Miral A. [2 ]
机构
[1] Mansoura Univ, Fac Sci, Dept Chem, Mansoura 35516, Egypt
[2] Sinai Univ, Fac Pharm, Dept Pharmaceut Chem, Kantra, Egypt
关键词
Carbazole; thiazole; Knoevenagel reaction; anticancer activity; MTT assay; KNOEVENAGEL REACTION; CANCER; DERIVATIVES; INHIBITORS; ALKALOIDS;
D O I
10.1080/10406638.2022.2144909
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Medicinal research has focused on the discovery and progress of anticancer drugs. Carbazole and thiazole are organic heterocyclic compounds that are the building blocks for synthetic and natural pharmaceutical compounds. Thus, this research article involves the synthesis of nine carbazole linked thiazolidinone derivatives from the Knoevenagel reaction of 9-ethylcarbazole-3-carbaldehyde with several thiazolidine-5-one and thiazolin-4-one derivatives. The structures of these compounds were confirmed by spectroscopic tools such as IR, H-1 and C-13 NMR, and mass spectrometry. The MTT assay, using Cisplatin as a reference drug, was used to test the cytotoxicity of the synthesized carbazole-thiazole analogous against three different cell lines: breast cancer (MCF-7), hepatocellular carcinoma (HepG-2), and colon carcinoma (HCT-116). The 3b and 5c molecules were the most effective antitumor drugs against the three cell lines. Compound 3b has IC50 values of (0.0304 +/- 0.001, 0.058 +/- 0.002 and 0.047 +/- 0.002 mu M) for HepG-2, MCF-7, and HCT-116, respectively. When examined on HepG-2, MCF-7, and HCT-116 cell lines, the IC50 values revealed by component 5c were (0.048 +/- 0.002, 0.086 +/- 0.0025 and 0.06 +/- 0.007 mu M), respectively.
引用
收藏
页码:8048 / 8064
页数:17
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