咪唑基 -（4 - 氧代喹唑啉 - 3(4H)-基）-乙酰胺对艾氏腹水癌的抗肿瘤作用
Antitumor actions of imidazolyl-(4-oxoquinazolin-3(4H)-yl)-acetamides against Ehrlich Ascites Carcinoma.
作者信息
Raghavendra Nulgumnalli Manjunathaiah, Gurubasavarajaswamy Purvarga Mattada, Nagaranavile Kanthappa Sathish, Parameshwaran Thampi
机构信息
Medicinal Chemistry Research Laboratory, Acharya and B.M. Reddy College of Pharmacy, Bangalore, Karnataka, India.
出版信息
Arch Pharm Res. 2009 Mar;32(3):431-6. doi: 10.1007/s12272-009-1317-8. Epub 2009 Apr 23.
Breast cancer is the second most common type of cancer after lung cancer and the fifth most common cause of cancer death. Several structural classes of compounds were discovered against tumor, but many of the existing antitumor agents exhibit severe side effects. Hence there is a need to identify a novel chemical entity having a broad range of therapeutic activity with fewer side effects. In this direction, several imidazolyl-(4-oxoquinazolin-3(4H)-yl)-acetamides 1-4(a-d) were screened for their antitumor activity against Ehrlich Ascites Carcinoma (EAC) using in-vitro and in-vivo models. Compounds 4b, 4d, and 3a showed highly significant antitumor activity against EAC in comparison with vincristine as standard.
乳腺癌是仅次于肺癌的第二大常见癌症类型，也是癌症死亡的第五大常见原因。已经发现了几类针对肿瘤的化合物结构，但许多现有的抗肿瘤药物都有严重的副作用。因此，需要鉴定一种具有广泛治疗活性且副作用较少的新型化学实体。在这个方向上，使用体外和体内模型筛选了几种咪唑基 -（4-氧代喹唑啉 - 3(4H)-基）-乙酰胺1 - 4(a - d)对艾氏腹水癌（EAC）的抗肿瘤活性。与作为标准的长春新碱相比，化合物4b、4d和3a对EAC显示出高度显著的抗肿瘤活性。
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