Anticancer and immunomodulatory activities of novel 1,8-naphthyridine derivatives

被引：11

作者：

Kumar, Vivek ^{[1
,2
]}

Madaan, Alka ^{[1
]}

Sanna, Vinod K. ^{[1
]}

Vishnoi, Manupriya ^{[1
]}

Joshi, Narendra ^{[1
]}

Singh, Anu T. ^{[1
]}

Jaggi, Manu ^{[1
]}

Sharma, Pramod K. ^{[2
]}

Irchhaiya, Raghuveer ^{[2
]}

Burman, Anand C. ^{[1
]}

机构：

[1] Dabur Res Fdn, Ghaziabad 201010, UP, India

[2] Bundelkhand Univ, Inst Pharm, Jhansi, Uttar Pradesh, India

来源：

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY | 2009年 / 24卷 / 05期

关键词：

Anticancer; anti-inflammatory; naphthyridine; 7-SUBSTITUTED 1,4-DIHYDRO-4-OXO-1-(2-THIAZOLYL)-1,8-NAPHTHYRIDINE-3-CARBOXYLIC ACIDS; ANTITUMOR AGENTS;

D O I：

10.1080/14756360802696802

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A number of 1,8-naphthyridine derivatives (22-62) have been synthesized and screened for their in vitro cytotoxicity against eight tumors and two non-tumor cell lines. Halogen substituted 1,8-naphthyridine-3-caboxamide derivatives showed potent activity with compound 47 having IC(50) of 0.41 and 0.77 mu M on MIAPaCa and K-562 cancer cell lines, respectively while, compound 36 had IC(50) of 1.19 mu M on PA-1 cancer cell line. However, one of the unsubstituted 1,8-naphthyridine-C-3'-heteroaryl derivative 29 showed potent cytotoxicity with IC(50) of 0.41 and 1.4 mu M on PA-1 and SW620 cancer cell lines, respectively. These compounds were also evaluated for anti-inflammatory activity as suggested by downregulation of proinflammaotory cytokines.

引用

页码：1169 / 1178

页数：10

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