Synthesis of novel fluorinated 1,5-benzothiazepine derivatives and their biological evaluation as anticancer and antibacterial agent

IF 1 4区化学 Q4 CHEMISTRY, MULTIDISCIPLINARY

Journal of The Serbian Chemical Society Pub Date : 2022-01-01 DOI:10.2298/jsc210428041b

Sonal Bhabal, S. Shaikh, Ishita Yellapurkar, G. Pavale, M. Ramana

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引用次数: 0

Abstract

A series of novel fluorinated 1,5-benzothiazepine derivatives were synthesized, characterized and evaluated for in vitro anticancer and antibacterial activity. The in vitro anticancer activity of the synthesized compounds 4(a-h) was evaluated against four human cancer cell lines namely lung (A549), breast (MCF-7), liver (HEPG2) and prostate (PC-3) cancer. Compounds 4c, 4d, 4g and 4h exhibited good activity with GI50 <10 ?g ml-1 against all four human cancer cell lines which was comparable to standard drug Adriamycin. Additionally, antibacterial activity of synthesized compounds was estimated using resazurin microtiter assay (REMA) and compared with standard drug Ampicillin. Among the synthesized compounds, 4c, 4d, 4g and 4h showed in good antibacterial activity and all the synthesized compounds were found to be more active towards gram negative than gram positive. These promising results obtained from in vitro anticancer and antibacterial activity, inferred that the synthesized compounds are capable of being anticancer as well as antibacterial agent.

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新型氟化1,5-苯并噻唑类衍生物的合成及其抗癌、抗菌生物学评价

合成了一系列新型氟化1,5-苯并噻唑类衍生物，并对其体外抗癌和抗菌活性进行了表征和评价。合成的化合物4(a-h)对肺癌(A549)、乳腺癌(MCF-7)、肝癌(HEPG2)和前列腺癌(PC-3)四种人癌细胞的体外抗癌活性进行了评价。化合物4c、4d、4g和4h对四种人类癌细胞具有良好的活性，其GI50 <10 μ g ml-1，与标准药物阿霉素相当。此外，采用瑞唑脲微效价测定法(REMA)评估合成化合物的抗菌活性，并与标准药物氨苄西林进行比较。在所合成的化合物中，4c、4d、4g和4h均表现出较好的抗菌活性，且所有化合物对革兰氏阴性菌的活性均高于革兰氏阳性菌。从体外抗癌和抗菌活性的研究结果来看，所合成的化合物具有抗癌和抗菌的双重作用。

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来源期刊

Journal of The Serbian Chemical Society 化学-化学综合

CiteScore

1.80

自引率

0.00%

发文量

审稿时长

1 months

期刊介绍： The Journal of the Serbian Chemical Society -JSCS (formerly Glasnik Hemijskog društva Beograd) publishes articles original papers that have not been published previously, from the fields of fundamental and applied chemistry: Theoretical Chemistry, Organic Chemistry, Biochemistry and Biotechnology, Food Chemistry, Technology and Engineering, Inorganic Chemistry, Polymers, Analytical Chemistry, Physical Chemistry, Spectroscopy, Electrochemistry, Thermodynamics, Chemical Engineering, Textile Engineering, Materials, Ceramics, Metallurgy, Geochemistry, Environmental Chemistry, History of and Education in Chemistry.