Design, synthesis and in vitro evaluation of coumarin-imidazo[1,2-a]pyridine derivatives against cancer induced osteoporosis

Sashidhara Koneni V.; Singh L. Ravithej; Choudhary Dharmendra; Arun Ashutosh; Gupta Sampa; Adhikary Sulekha; Palnati Gopala Reddy; Konwar Rituraj; Trivedi Ritu

首页> 外文期刊>RSC Advances >Design, synthesis and in vitro evaluation of coumarin-imidazo[1,2-a]pyridine derivatives against cancer induced osteoporosis

【24h】

Design, synthesis and in vitro evaluation of coumarin-imidazo[1,2-a]pyridine derivatives against cancer induced osteoporosis

机译：香豆素 - 咪唑的设计，合成和体外评价[1,2-A]吡啶衍生物对癌症诱导的骨质疏松症

获取原文

获取原文并翻译 | 示例

掌桥外文数据库（机构版） >>

开具论文收录证明 >>

文献代查 >>

页面导航

摘要
著录项
相似文献
相关主题

摘要

A series of biologically important 6-(imidazo[1,2-a]pyridin-2-yl)-2H-chromen-2-one derivatives were synthesized by employing the silver( I) catalysed Groebke-Blackburn-Bienayme multicomponent reaction. The synthesized compounds were tested in a primary calvarial osteoblast cells by alkaline phosphatase assay and an alizarin red-S staining assay for their possible osteoprotective properties. Further, the effects of active compounds 6h, 6l, and 6o on the expression of osteogenic genes BMP2, RUNX2, COL1, and OCN were measured by qPCR. Out of three promising compounds, 6l and 6o significantly induced apoptosis in MDA-MB-231 cancer cells via mitochondrial depolarisation without affecting normal cells. In an in vitro co-culture model of bone metastasis, we investigated the ability of coumarin-imidazo[1,2-a]pyridine hybrids to reverse the negative impact of MDA-MB-231 cancer cells on osteoblast differentiation. The results illustrate the potential of designed hybrids to re-establish the bone homeostasis. These findings demonstrate the significance of newly synthesized hybrids as lead molecules, possessing both anti-osteoporotic and anticancer properties that can be developed into new therapeutic agents to alleviate osteoporosis and bone metastasis.

机译：通过使用银（I）催化的Groebke-Blackburn-Bienayme多组分反应，合成了一系列生物学上重要的6-（咪唑吡啶-2-基）-2H-铬-2-一代衍生物。通过碱性磷酸酶测定和茜素红核染色测定在初级颅骨成骨细胞中测试合成的化合物，用于其可能的骨质保护性能。此外，通过QPCR测量活性化合物6H，6L和6O对骨质原基因BMP2，RUNX2，COL1和OCN的表达的影响。在三种承诺的化合物中，6L和6o通过线粒体去氧在MDA-MB-231癌细胞中显着诱导细胞凋亡，而不会影响正常细胞。在骨转移的体外共培养模型中，我们研究了香豆素-Imidazo [1,2-A]吡啶杂交体逆转MDA-MB-231癌细胞对成骨细胞分化的负面影响的能力。结果说明了设计杂种以重新建立骨稳态的潜力。这些发现表明，新合成的杂种作为铅分子的重要性，具有可开发到新的治疗剂中以缓解骨质疏松症和骨转移的抗骨质疏松性和抗癌性质。

著录项

来源
《RSC Advances》 |2016年第83期|共12页
作者
Sashidhara Koneni V.; Singh L. Ravithej; Choudhary Dharmendra; Arun Ashutosh; Gupta Sampa; Adhikary Sulekha; Palnati Gopala Reddy; Konwar Rituraj; Trivedi Ritu;
展开▼
作者单位

CSIR Cent Drug Res Inst Med &

Proc Chem Div BS-10-1 Sect 10 Sitapur Rd Lucknow 226031 Uttar Pradesh India;

CSIR Cent Drug Res Inst Med &

Proc Chem Div BS-10-1 Sect 10 Sitapur Rd Lucknow 226031 Uttar Pradesh India;

CSIR Cent Drug Res Inst Div Endocrinol BS-10-1 Sect 10 Sitapur Rd Lucknow 226031 Uttar Pradesh India;

CSIR Cent Drug Res Inst Div Endocrinol BS-10-1 Sect 10 Sitapur Rd Lucknow 226031 Uttar Pradesh India;

CSIR Cent Drug Res Inst Med &

Proc Chem Div BS-10-1 Sect 10 Sitapur Rd Lucknow 226031 Uttar Pradesh India;

CSIR Cent Drug Res Inst Div Endocrinol BS-10-1 Sect 10 Sitapur Rd Lucknow 226031 Uttar Pradesh India;

CSIR Cent Drug Res Inst Med &

Proc Chem Div BS-10-1 Sect 10 Sitapur Rd Lucknow 226031 Uttar Pradesh India;

CSIR Cent Drug Res Inst Div Endocrinol BS-10-1 Sect 10 Sitapur Rd Lucknow 226031 Uttar Pradesh India;

CSIR Cent Drug Res Inst Div Endocrinol BS-10-1 Sect 10 Sitapur Rd Lucknow 226031 Uttar Pradesh India;

展开▼
收录信息
原文格式 PDF
正文语种 eng
中图分类化学;
关键词

相似文献

外文文献
中文文献
专利

1. Design, synthesis and in vitro evaluation of coumarin-imidazo[1,2-a]pyridine derivatives against cancer induced osteoporosis [J] . Sashidhara Koneni V., Singh L. Ravithej, Choudhary Dharmendra, RSC Advances . 2016,第83期

机译：香豆素 - 咪唑的设计，合成和体外评价[1,2-A]吡啶衍生物对癌症诱导的骨质疏松症
2. Design, Synthesis, In Vitro Cytotoxic Activity Evaluation, and Study of Apoptosis Inducing Effect of New Styrylimidazo[1,2-a] Pyridines as Potent Anti-Breast Cancer Agents [J] . Khalili Faeze, Akrami Sara, Safavi Malihe, Nature reviews Cancer . 2019,第2期

机译：设计，合成，体外细胞毒性活性评价，以及新的STYRYLIMIDAZO [1,2-A]吡啶作为有效抗乳腺癌药物的凋亡诱导诱导诱导
3. Design, Synthesis, In Vitro Cytotoxic Activity Evaluation, and Study of Apoptosis Inducing Effect of New Styrylimidazo[1,2-a] Pyridines as Potent Anti-Breast Cancer Agents [J] . Khalili Faeze, Akrami Sara, Safavi Malihe, Anti-cancer agents in medicinal chemistry . 2019,第2期

机译：设计，合成，体外细胞毒性活性评价，以及新的STYRYLIMIDAZO [1,2-A]吡啶作为有效的抗乳腺癌药物的凋亡诱导诱导诱导效应
4. Benzofuran-3(2H)-Ones Derivatives: Synthesis, Docking and Evaluation of Their in Vitro Anticancer Studies [C] . Nishant Verma, Shaily, Kalpana Chauhan, International Conference on Trends in Computational and Cognitive Engineering . 2020

机译：Benzofuran-3（2H） - 衍生物：其体外抗癌研究的合成，对接和评估
5. Design, synthesis and evaluation of quercetin analogues and derivatives intended towards the treatment of prostate cancer. [D] . Al-Jabban, Sami M.R. 2015

机译：槲皮素类似物和衍生物的设计，合成和评估，旨在治疗前列腺癌。
6. Design synthesis and biological evaluation of novel pyridine derivatives as anticancer agents and phosphodiesterase 3 inhibitors [O] . Ashraf H. Abadi, Tamer M. Ibrahim, Khaled M. Abouzid, -1

机译：新型吡啶衍生物作为抗癌剂和磷酸二酯酶3抑制剂的设计合成和生物学评价
7. Synthesis of Novel 2-Butyl-1H-Benzo 4, 5 Imidazo 1, 2-A Imidazo 4, 5-E Pyridine-5-Carbonitrile Derivatives and Evaluation of Their Anticancer Activity [O] . Achanta Venkata Hanumantha Rao, Rayam Parsharamulu, Malthum Shankaraiah, 2016

机译：新型2-丁基-1H-苯并4,5咪唑1,2-A咪唑4,5-e吡啶-5-腈衍生物及其抗癌活性的评价

Design, synthesis and in vitro evaluation of coumarin-imidazo[1,2-a]pyridine derivatives against cancer induced osteoporosis

摘要

著录项

相似文献

相关主题

期刊订阅