Synthesis of indole based novel small molecules and their in vitro anti-proliferative effects on various cancer cell lines

被引：10

作者：

Dulla, Balakrishna ^{[1
]}

Sailaja, E. ^{[2
]}

Reddy, Upendar C. H. ^{[1
]}

Aeluri, Madhu ^{[1
]}

Kalle, Arunasree M. ^{[3
]}

Bhavani, S. ^{[4
]}

Rambabu, D. ^{[5
,6
]}

Rao, M. V. Basaveswara ^{[2
]}

Pal, Manojit ^{[1
]}

机构：

[1] Univ Hyderabad Campus, Dr Reddys Inst Life Sci, Hyderabad 500046, Andhra Pradesh, India

[2] Krishna Univ, Dept Chem, Machilipatnam 521001, Andhra Pradesh, India

[3] Univ Hyderabad, Sch Life Sci, Dept Anim Sci, Hyderabad 500046, Andhra Pradesh, India

[4] KL Univ, Dept Chem, Vaddeswaram Guntur 522502, Andhra Pradesh, India

[5] Ben Gurion Univ Negev, Dept Chem, IL-84105 Beer Sheva, Israel

[6] Ben Gurion Univ Negev, Natl Inst Biotechnol Negev, IL-84105 Beer Sheva, Israel

来源：

TETRAHEDRON LETTERS | 2014年 / 55卷 / 04期

关键词：

Indole; Alkyne; Coupling-cyclization; X-ray; Cancer; INDANONE; DERIVATIVES; INHIBITORS;

D O I：

10.1016/j.tetlet.2013.12.050

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Indole based novel small molecules were designed as potential anticancer agents. Multi step synthesis of these compounds was carried out by using Pd/C-Cu mediated coupling-cyclization strategy as a key step. The single crystal X-ray diffraction study was used to confirm the molecular structure of a representative compound unambiguously. Many of these compounds were evaluated for their anti-proliferative properties in vitro against six cancer cell lines as well as noncancerous cells. All these compounds showed selective growth inhibition of cancer cells and several of them were found to be promising with IC50 values in the range of 0.1-1.2 mu M, comparable to the known anticancer drug doxorubicin. (C) 2013 Elsevier Ltd. All rights reserved.

引用

页码：921 / 926

页数：6

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