Anticarcinogenic and antioxidant activity of diindolylmethane derivatives
文献类型：期刊论文
| 作者 | Benabadji SH ; Wen R(闻韧) ; Zheng JB(郑剑斌) ; Dong XC(董晓春) ; Yuan SG(袁身刚) |
| 刊名 | Acta Pharmacol. Sin.
 |
| 出版日期 | 2004 |
| 卷号 | 25期号:5页码:666-671 |
| ISSN号 | 1671-4083 |
| 其他题名 | 二吲哚甲醛衍生物的抗癌和抗衰老活性研究 |
| 通讯作者 | 闻韧 |
| 英文摘要 | AIM: To investigate the synthesis methods and the bioactivity of diindolylmethane (DIM) derivatives. METHODS: 1) A 3D-Quantitative Structure-Active Relationships (QSAR) Comparative Molecular Field Analysis (CoMFA) study of 14 DIM derivatives was investigated to predict their anticarcinogenic activity. 2) Based on CoMFA model, a series of new derivatives of DIM were designed and synthesized. 3) Their free radical scavenging and antioxidant potentials were tested using in-vitro DPPH radical scavenging and P-carotene antioxidant models. 4) The anticarcinogenic activities of some compounds were tested by using microculture tetrazolium assay (MTT) and sulforhodamine B (SRB) proteochromosomic assays. RESULTS: 1) The CoMFA model derived from DIM analogues proved a good predictive ability with q(2) value of 0.827. 2) New designed compounds 3c and 4c exhibited 3-fold more potent radical scavenging activity than reference substance Vitamin E in DPPH model expressed by IC50 values. 3) The primary antitumor screening essay showed that some DIM derivatives designed exhibited the inhibitory activities to some tumor cell growth at relatively high concentration, and DIM was the most effective among them. CONCLUSION: DIM's 3D-QSAR model is reliable. According to it, eleven DIM derivatives were synthesized, and two derivatives of them possess potent radical scavenging activities and some showed the inhibitory activities in primary anticancer assay in vitro. |
| 学科主题 | 计算机化学与化学信息学 |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000221337100020 |
| 公开日期 | 2013-02-26 |
| 源URL | [http://202.127.28.38/handle/331003/20609]  |
| 专题 | 上海有机化学研究所_计算机化学与化学信息学研究室 |
| 推荐引用方式 GB/T 7714 | Benabadji SH,Wen R,Zheng JB,et al. Anticarcinogenic and antioxidant activity of diindolylmethane derivatives[J]. Acta Pharmacol. Sin.,2004,25(5):666-671. |
| APA | Benabadji SH,闻韧,郑剑斌,董晓春,&袁身刚.(2004).Anticarcinogenic and antioxidant activity of diindolylmethane derivatives.Acta Pharmacol. Sin.,25(5),666-671. |
| MLA | Benabadji SH,et al."Anticarcinogenic and antioxidant activity of diindolylmethane derivatives".Acta Pharmacol. Sin. 25.5(2004):666-671. |
入库方式： OAI收割
来源：上海有机化学研究所
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