Novel 1,3,4-Thiadiazole Linked Amide Derivatives of Pteridone: Synthesis and Study of Anticancer Activities

被引:10
作者
Devi, Eeduri R. [1 ,2 ]
Sreenivasulu, Reddymasu [2 ]
Rao, Koya P. [1 ]
Nadh, Ratnakaram V. [3 ]
Sireesha, Malladi [1 ]
机构
[1] Deemed Univ, Vignans Fdn Sci Technol & Res, Dept Sci & Humanities, Div Chem, Guntur 522213, Andhra Pradesh, India
[2] Jawaharlal Nehru Technol Univ, Univ Coll Engn Autonomous, Dept Chem, Kakinada 533003, Andhra Pradesh, India
[3] Deemed Univ, Gandhi Inst Technol & Management, Dept Chem, Bangalore Campus, Bangalore 561203, Karnataka, India
关键词
Pteridone; pralatrexate; triamterene; thiamethoxam; anticancer activity; cancer; BIOLOGICAL EVALUATION; MOLECULAR DOCKING; ELLIPTICINE DERIVATIVES; INHIBITORS; ANALOGS; DESIGN; POTENT; SERIES;
D O I
10.2174/1570178616666190528095548
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Cancer is a second leading cause of death after heart attack, in developing as well as undeveloped countries. It is caused by unregulated growth and metastasis of the abnormal cancer cells. Cancer can be cured by radiation, immunotherapy and chemotherapy, among them; chemotherapy is a good treatment for cancer, in which chemotherapeutic drug is used. The anticancer activity of newly synthesized compounds (13a-j) was carried out on four different types of human cancer cell lines like MCF-7 (breast), A549 (lung), Colo-205 (colon) and A2780 (ovarian) by the MTT method, and compared to etoposide used as a positive control. Among them, compound 13g with electron-withdrawing (3,5-dinitro) group, exhibited more promising activity in all cell lines (MCF-7 = 0.10+0.076 mu M, A549 = 0.17+0.039 mu M, Colo-205= 0.13+0.022 mu M and A2780 - 0.87+0.027 mu M). This compound may act as lead drug in cancer chemotherapy. In future, this compound can be examined for clinical studies.
引用
收藏
页码:54 / 60
页数:7
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