Please use this identifier to cite or link to this item: https://dspace.ctu.edu.vn/jspui/handle/123456789/5048
Title: Microwave assisted synthesis and cytotoxic activity evaluations of new benzimidazole derivatives
Authors: Bùi, Thị Bửu Huê
Hà, Thị Kim Quy
Mai, Văn Hiếu
Tran, Thi Loan
Tran, Phuong Thao
Pham, Canh Em
Tu, Thi Kim Cuc
Nguyen, Tram Yen Chau
Vo, Duc Duy
Oh, Won Keun
Keywords: 4-Oxo-4H-quinolizine
Naphthalene
Benzimidazole
Stobbe condensation
Microwave assisted organic synthesis
Human breast cancer cell line
Issue Date: 2016
Series/Report no.: Tetrahedron Letters;57 .- p.887–891
Abstract: Twelve new 2-quinolizinylbenzimidazole and 2-naphthalylbenzimidazole derivatives with various 5- and 6-positioned substituents (aza, H, CH₃, Cl, NO₂, NH₂, OCH₃), have been synthesized in moderate to excellent yields via the condensation of 4-oxo-4H-quinolizinecarbaldehyde or naphthalenecarbaldehyde with substituted o-phenylenediamines, o-nitroaniline, and 2,3-pyridinediamine using sodium metabisulfite or sodium hydrosulfite under microwave irradiation. The new benzimidazole derivatives were screened for their cytotoxic activity against the human breast cancer cell line (MCF-7). The results showed on one hand that 2-(substituted quinolizinyl)-1H-benzimidazoles (12b–f) were less active (3–6 fold) than the positive control Tamoxifen (CC₅₀ = 6.52 μM), and on the other hand, among the 2-(substituted naphthalyl)-1H-benzimidazoles series (13a–f), compounds 6,7,8-trimethoxy-3-(5-chloro-1H-benzo[d]imidazol-2-yl)naphthalen-1-ol (13c) (CC₅₀ = 7.48 μM) and 6,7,8-trimethoxy-3-(5-methoxy-1H-benzo [d] imidazol-2-yl)naphthalen-1-ol (13f) (CC₅₀ = 6.43 μM) were found to be as active as Tamoxifen.
URI: http://localhost:8080//jspui/handle/123456789/5048
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