N-芳基-5-取代-1,3,4-恶二唑-2-胺类似物的合成及其抗癌活性
Synthesis and anticancer activity of N-aryl-5-substituted-1,3,4-oxadiazol-2-amine analogues.
作者信息
Ahsan Mohamed Jawed, Sharma Jyotika, Singh Monika, Jadav Surender Singh, Yasmin Sabina
机构信息
Department of Pharmaceutical Chemistry, Maharishi Arvind College of Pharmacy, Jaipur, Rajasthan 302 023, India.
Department of Pharmaceutical Chemistry, Birla Institute of Technology, Mesra, Ranchi, Jharkhand 835 215, India.
出版信息
Biomed Res Int. 2014;2014:814984. doi: 10.1155/2014/814984. Epub 2014 May 26.
In continuance of our search for anticancer agents, we report herein the synthesis and anticancer activity of some novel oxadiazole analogues. The compounds were screened for anticancer activity as per National Cancer Institute (NCI US) protocol on leukemia, melanoma, lung, colon, CNS, ovarian, renal, prostate, and breast cancers cell lines. N-(2,4-Dimethylphenyl)-5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-amine (4s) showed maximum activity with mean growth percent (GP) of 62.61 and was found to be the most sensitive on MDA-MB-435 (melanoma), K-562 (leukemia), T-47D (breast cancer), and HCT-15 (colon cancer) cell lines with GP of 15.43, 18.22, 34.27, and 39.77, respectively. Maximum GP was observed on MDA-MB-435 (melanoma) cell line (GP = 6.82) by compound N-(2,4-dimethylphenyl)-5-(4-hydroxyphenyl)-1,3,4-oxadiazol-2-amine (4u).
在持续寻找抗癌药物的过程中，我们在此报告一些新型恶二唑类似物的合成及抗癌活性。按照美国国立癌症研究所（NCI US）的方案，对这些化合物在白血病、黑色素瘤、肺癌、结肠癌、中枢神经系统癌、卵巢癌、肾癌、前列腺癌和乳腺癌细胞系上进行了抗癌活性筛选。N-(2,4-二甲基苯基)-5-(4-甲氧基苯基)-1,3,4-恶二唑-2-胺（4s）显示出最大活性，平均生长百分比（GP）为62.61，并且发现在MDA-MB-435（黑色素瘤）、K-562（白血病）、T-47D（乳腺癌）和HCT-15（结肠癌）细胞系上最为敏感，其GP分别为15.43、18.22、34.27和39.77。化合物N-(2,4-二甲基苯基)-5-(4-羟基苯基)-1,3,4-恶二唑-2-胺（4u）在MDA-MB-435（黑色素瘤）细胞系上观察到最大GP（GP = 6.82）。
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