Design, synthesis of novel N prenylated indole-3-carbazones and evaluation of in vitro cytotoxicity and 5-LOX inhibition activities

被引：6
|
作者：
Choppara, Praveen [1 ]
Prasad, Y. V. [1 ]
Rao, C. V. [2 ]
Krishna, K. Hari [2 ]
Trimoorthulu, G. [2 ]
Rao, G. U. Maheswara [2 ]
Rao, J. Venkateswara [3 ]
Bethu, M. S. [3 ]
Murthy, Y. L. N. [1 ]
机构：
[1] Andhra Univ, Dept Organ Chem Foods Drugs & Water, Visakhapatnam 530003, Andhra Pradesh, India
[2] Laila Impex, Resaearch & Dev Ctr, Vijayawada 520007, India
[3] Indian Inst Chem Technol, Biol Div, Hyderabad 500007, AP, India
来源：
ARABIAN JOURNAL OF CHEMISTRY | 2019年 / 12卷 / 08期
关键词：
Brine shrimp lethality bioassay; Cytotoxicity; 5-Lipoxygenase inhibition; N prenylated indole-3-carbazones; SHRIMP LETHALITY ASSAY; BRINE SHRIMP; ANTIPROLIFERATIVE ACTIVITY; ANTIMYCOBACTERIAL ACTIVITY; RECEPTOR ANTAGONISTS; 5-LIPOXYGENASE; SEMICARBAZONES; DERIVATIVES; DISCOVERY; INDOLES;
D O I：
10.1016/j.arabjc.2015.02.006
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
A series of novel N-1 and C-3 substituted indole derivatives (5a-f) were designed, synthesized and evaluated for their cytotoxic properties, viz Brine Shrimp Lethality Bioassay (BSLB) besides 5-Lipoxygenase (5-LOX) inhibitory activities through in vitro assays. Structure Activity Relation (SAR) studies showed that compound 5d with an LC50 of 6.49 mu M and 5c with an IC50 of 33.69 mu M were found to be interesting for cytotoxicity and 5-LOX inhibitory activity respectively. (C) 2015 The Authors. Published by Elsevier B.V. on behalf of King Saud University.
引用
收藏
页码：2328 / 2335
页数：8
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