Synthesis, characterization and cytotoxic investigations of novel bis(indole) analogues besides antimicrobial study

被引:22
作者
Choppara, Praveen [1 ,2 ]
Bethu, M. S. [3 ]
Prasad, Y. Vara [1 ]
Rao, J. Venkateswara [3 ]
Ranjan, T. J. Uday [4 ]
Prasad, G. V. Siva [1 ,2 ]
Doradla, Rajitha [1 ]
Murthy, Y. L. N. [1 ]
机构
[1] Andhra Univ, Dept Organ Chem Foods Drugs & Water, Visakhapatnam 530003, Andhra Pradesh, India
[2] Raghu Engn Coll, Dept Sci & Humanities, Visakhapatnam 531162, Andhra Pradesh, India
[3] Indian Inst Chem Technol, Biol Div, Hyderabad 500007, Andhra Pradesh, India
[4] Andhra Univ, Dept Marine Living Resources, Visakhapatnam 530003, Andhra Pradesh, India
关键词
Indole-3-acylhydrazides; Indole-3-carboxaldehyde; N-prenylated indole-3-carboxaldehyde; Bis(indole) analogues; Antimicrobial activity; Anticancer activity; MARINE ALKALOID NORTOPSENTIN; ANTIPROLIFERATIVE ACTIVITY; INDOLE-DERIVATIVES; BIOLOGICAL-ACTIVITIES; ANTICANCER EVALUATION; ANALGESIC ACTIVITY; ANTITUMOR-ACTIVITY; IRON CHELATORS; SPONGE; ACYLARYLHYDRAZONES;
D O I
10.1016/j.arabjc.2015.05.015
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Two series of novel bis(indole) analogues viz., N'-((5-substituted-1H-indol-3-yl)methylene)-n-(1H-indol-3-yl)alkanehydrazides (7af) and N'-((5-substituted-1-(3-methylbut-2-enyl)-1H-indol-3-yl)methylene)-n-(1H-indol-3-yl)acetohydrazide (8af) were synthesized and characterized by spectral analysis. The target molecules were screened for their antimicrobial, anticancer activities and structure and activity relationship (SAR) was investigated. Compounds 7a, 7c and 8a were found to be active in antimicrobial screening. Anticancer screening reveals that Compound 7c was active against HeLa cell line with an IC50 of 43.1 mu M and compound 7d was found to be interesting candidate with an IC50 of 26.0 and 30.2 mu M against Colo-205 and Hep G2 cell lines respectively. (C) 2015 The Authors. Published by Elsevier B.V. on behalf of King Saud University. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).
引用
收藏
页码:2721 / 2731
页数:11
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