新型1,4-苯并恶嗪-[1,2,3]三唑杂化物的合理设计、合成及抗增殖活性评价
Rational design, synthesis and anti-proliferative evaluation of novel 1,4-benzoxazine-[1,2,3]triazole hybrids.
作者信息
Bollu Rajitha, Palem Jyothsna Devi, Bantu Rajashaker, Guguloth Vijayacharan, Nagarapu Lingaiah, Polepalli Sowjanya, Jain Nishant
机构信息
Organic Chemistry Division II (CPC), CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India.
Organic Chemistry Division II (CPC), CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India.
出版信息
Eur J Med Chem. 2015 Jan 7;89:138-46. doi: 10.1016/j.ejmech.2014.10.051. Epub 2014 Oct 18.
A series of novel 1,2,3-triazole-1,4-benzoxazine hybrids 5a-n were efficiently synthesized employing click chemistry approach and evaluated for anti-proliferative activity against four cancer cell lines such as HeLa (cervical), MIAPACA (pancreatic), MDA-MB-231 (breast) and IMR32 (neuroblastoma). Compounds 5n and 5g exhibited promising anti-proliferative activity with GI50 values ranging from 1.2 to 2.5 μM and 0.1-1.1 μM respectively against all cell lines, like HeLa, MDA-MB-231, MIAPACA and IMR32, while compound 5l showed significant activity against MDA-MB-231 and IMR32 with GI50 values ranging from 1.1 and 1.4 μM. This is the first report on the synthesis and in vitro anti-proliferative evaluation of 1,2,3-triazole-1,4-benzoxazine hybrids.
采用点击化学方法高效合成了一系列新型的1,2,3-三唑-1,4-苯并恶嗪杂化物5a-n，并对其针对四种癌细胞系（如HeLa（宫颈癌）、MIAPACA（胰腺癌）、MDA-MB-231（乳腺癌）和IMR32（神经母细胞瘤））的抗增殖活性进行了评估。化合物5n和5g表现出有前景的抗增殖活性，针对所有细胞系（如HeLa、MDA-MB-231、MIAPACA和IMR32）的GI50值分别为1.2至2.5 μM和0.1 - 1.1 μM，而化合物5l对MDA-MB-231和IMR32表现出显著活性，GI50值为1.1至1.4 μM。这是关于1,2,3-三唑-1,4-苯并恶嗪杂化物的合成及体外抗增殖评估的首次报道。
Zotero 插件