Design, synthesis, anticancer evaluation, and molecular docking studies of 1,3,4-thiadiazole bearing 1,3,5-triazine-thiazoles

被引:0
作者
Nalla, Somaiah [1 ]
Pavani, Y. [2 ]
Kumar, Gollapudi Ravi [3 ]
Sumalatha, Poodari [3 ]
Syed, Tasqeeruddin [4 ]
Subbarao, Mannam [1 ,5 ]
机构
[1] Acharya Nagarjuna Univ, Dept Chem, Guntur, India
[2] PVP Siddhartha Inst Technol, Dept Freshman Engn, Vijayawada, India
[3] Govt Degree Coll Autonomous, Siddipet, India
[4] King Khalid Univ, Coll Pharm, Dept Pharmaceut Chem, Abha, Saudi Arabia
[5] Acharya Nagarjuna Univ, Dept Chem, Guntur, Andhra Prades, India
关键词
MBX-2982; thiazole; 1,3,4-thiadiazole and anticancer activity; IN-VITRO; DERIVATIVES; ANTITUMOR; ANTICONVULSANT; THIADIAZOLES; CYTOTOXICITY; THIAZOLE; SERIES;
D O I
10.1080/00397911.2023.2286473
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A new library of 1,3,4-thiadiazole bearing 1,3,5-triazine-thiazole (9a-j) compounds have been designed, synthesized, and assessed for their in vitro anticancer applications against a panel of human cancer cell lines, including prostate cancer (PC3&DU-145), lung cancer (A549), and breast cancer (MCF-7) by using the MTT method. The results were expressed as IC50 mu M. Most of the tested compounds displayed good to moderate activity and were compared with the standard compound etoposide. The IC50 values ranged for synthesized compounds from 0.11 +/- 0.078 to 10.6 +/- 5.47 mu M and etoposide showed values ranging from 1.97 +/- 0.45 to 3.08 +/- 0.135 mu M. Among the evaluated compounds, five (9a, 9b, 9c, 9d, and 9e) were found to show more potent activity. Specifically, compound 9a displayed good activity.
引用
收藏
页码:268 / 281
页数:14
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