In-Vitro Anticancer and Antibacterial Activities of Brominated Indeno[1,2-b]qinoline Amines Supported with Molecular Docking and MCDM**

被引:15
作者
Aydin, Ali [1 ]
Okten, Salih [2 ]
Erkan, Sultan [3 ]
Bulut, Merve [4 ]
Ozcan, Evrencan [4 ]
Tutar, Ahmet [5 ]
Eren, Tamer [4 ]
机构
[1] Bozok Univ, Fac Med, Dept Basic Med Sci, Yozgat, Turkey
[2] Kirikkale Univ, Dept Maths & Sci Educ, Fac Educ, Yahsihan, Kirikkale, Turkey
[3] Sivas Cumhuriyet Univ, Dept Chem, Fac Sci, Sivas, Turkey
[4] Kirikkale Univ, Dept Ind Engn, Fac Engn & Architecture, Yahsihan, Kirikkale, Turkey
[5] Sakarya Univ, Fac Art & Sci, Dept Chem, Serdivan, Sakarya, Turkey
关键词
Antibacterial agents; Antitumor agents; Biological activity; Molecular docking; Multi criteria decision making; Indeno[1; 2-b]quinoline amine; CRYSTAL-STRUCTURE; DERIVATIVES;
D O I
10.1002/slct.202004753
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
The present study describes mono substituted indeno[1,2-b]quinolines (3 a-c and 5) have much more antiproliferative potentials than positive controls against A549, HeLa, MCF7 and Hep3B cell lines (IC50 values 1.1-29.6 mu g/mL) and show similar cytotoxicity (14.3 % to 19.8 %) to cells such as controls. Moreover, the mono substituted indeno[1,2-b]quinoline amines (3 a-c and 5) exhibit significant antimicrobial activity with MIC values between 15.62 mu g/mL and 250 mu g/mL. The compounds can also bind to DNA in the groove binding mode with a binding constant range of 1.1x10(3)-1.1x10(5) M-1. The anticancer and antibacterial properties of compounds were confirmed with the molecular docking simulation for their pharmacokinetic. As a result, the preliminary experimental data and a multi-criteria decision-making methodology (MCDM) indicated that the mono substituted indeno[1,2-b]quinoline amine derivatives, especially 3 a and 5, exhibit effective pharmacological properties. parameters and their interaction with related cells at the molecular level.
引用
收藏
页码:3286 / 3295
页数:10
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