Anticancer and Antimicrobial Activity of Some New 2,3-Dihydro-1,5-benzodiazepine Derivatives

IF 1.1 4区化学 Q3 CHEMISTRY, MULTIDISCIPLINARY Heteroatom Chemistry Pub Date : 2023-11-06 DOI:10.1155/2023/3390122

Felix Odame, Tatenda Madanhire, Clement Tettey, David Neglo, Francisca Adzaho, Daniel Sedohia, Eric C. Hosten

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Abstract

A series of 2,3-dihydro-1,5-benzodiazepine derivatives have been synthesized and characterized using IR, NMR, GC-MS, single crystal XRD, and microanalysis. The results of their antibacterial activity against methicillin-resistance Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Bacillus subtilis, Streptococcus mutans, Pseudomonas aeruginosa, Salmonella typhi, and Streptococcus pyrogens indicated that most of the compounds were bacteriostatic (0.125−4 mg/mL) and also exhibited good biofilm inhibition (0.21−72.69%). The compounds were found to be synergistic when used in combination with other antibiotics. The antiproliferative and cytotoxic effects were also investigated against PC-3 prostate cancer and RAW 264.7 macrophage cell lines, respectively, using the MTT assay. Apart from compounds 6 and 7, a good number of the compounds (1, 2, 3, 4, 5, and 8) were selectively toxic to the prostate cancer cells at 20 µM, whilst sparing the normal cells. Compound 3 demonstrated the highest antiprostate cancer effect by reducing the viability of PC-3 cells to (13.75%), which was followed by compounds 1 (47.72%), 2 (48.18%), 4 (62.61%), 5 (66.70%), and 8 (69.55%).

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一些新的2,3-二氢-1,5-苯二氮卓类衍生物的抗癌和抗菌活性

合成了一系列2,3-二氢-1,5-苯二氮卓衍生物，并采用IR、NMR、GC-MS、单晶XRD和微量分析对其进行了表征。对耐甲氧西林金黄色葡萄球菌、大肠埃希菌、肺炎克雷伯菌、枯草芽孢杆菌、变形链球菌、铜绿假单胞菌、伤寒沙门氏菌和热原链球菌的抑菌活性结果表明，大部分化合物具有抑菌作用(0.125 ~ 4 mg/mL)，并具有良好的生物膜抑制作用(0.21 ~ 72.69%)。当与其他抗生素联合使用时，发现这些化合物具有协同作用。采用MTT法分别研究了其对PC-3前列腺癌和RAW 264.7巨噬细胞的抗增殖和细胞毒作用。除化合物6和7外，许多化合物(1、2、3、4、5和8)在20µM下对前列腺癌细胞有选择性毒性，而对正常细胞没有毒性。化合物3的抗前列腺癌作用最强，可使PC-3细胞活力降低(13.75%)，其次是化合物1(47.72%)、2(48.18%)、4(62.61%)、5(66.70%)和8(69.55%)。

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来源期刊

Heteroatom Chemistry 化学-化学综合

CiteScore

1.20

自引率

0.00%

发文量

审稿时长

6 months

期刊介绍： Heteroatom Chemistry brings together a broad, interdisciplinary group of chemists who work with compounds containing main-group elements of groups 13 through 17 of the Periodic Table, and certain other related elements. The fundamental reactivity under investigation should, in all cases, be concentrated about the heteroatoms. It does not matter whether the compounds being studied are acyclic or cyclic; saturated or unsaturated; monomeric, polymeric or solid state in nature; inorganic, organic, or naturally occurring, so long as the heteroatom is playing an essential role. Computational, experimental, and combined studies are equally welcome. Subject areas include (but are by no means limited to): -Reactivity about heteroatoms for accessing new products or synthetic pathways -Unusual valency main-group element compounds and their properties -Highly strained (e.g. bridged) main-group element compounds and their properties -Photochemical or thermal cleavage of heteroatom bonds and the resulting reactivity -Uncommon and structurally interesting heteroatom-containing species (including those containing multiple bonds and catenation) -Stereochemistry of compounds due to the presence of heteroatoms -Neighboring group effects of heteroatoms on the properties of compounds -Main-group element compounds as analogues of transition metal compounds -Variations and new results from established and named reactions (including Wittig, Kabachnik–Fields, Pudovik, Arbuzov, Hirao, and Mitsunobu) -Catalysis and green syntheses enabled by heteroatoms and their chemistry -Applications of compounds where the heteroatom plays a critical role. In addition to original research articles on heteroatom chemistry, the journal welcomes focused review articles that examine the state of the art, identify emerging trends, and suggest future directions for developing fields.