N-(5-(TRIFLUOROMETHYL)-1,3,4-THIADIAZOL-2-YL)BENZAMIDE AND BENZOTHIOAMIDE DERIVATIVES INDUCE APOPTOSIS VIA CASPASE-DEPENDENT PATHWAY

被引：4

作者：

Aliabadi, Alireza ^{[1
,2
]}

Afnanzade, Nazanin-Sadat ^{[2
,3
]}

Hosseinzadeh, Leila ^{[1
,4
]}

Mohammadi-Farani, Ahmad ^{[1
,4
]}

Shafiee, Mohammad Hossein ^{[2
,3
]}

Nazari, Hanifeh ^{[3
,4
]}

Ahmadi, Farahnaz ^{[1
,4
]}

Foroumadi, Alireza ^{[5
,6
]}

机构：

[1] Kermanshah Univ Med Sci, Sch Pharm, Pharmaceut Sci Res Ctr, Kermanshah, Iran

[2] Kermanshah Univ Med Sci, Dept Med Chem, Fac Pharm, Kermanshah, Iran

[3] Kermanshah Univ Med Sci, Student Res Comm, Kermanshah, Iran

[4] Kermanshah Univ Med Sci, Dept Pharmacol & Toxicol, Fac Pharm, Kermanshah, Iran

[5] Univ Tehran Med Sci, Fac Pharm, Dept Med Chem, Tehran 14174, Iran

[6] Univ Tehran Med Sci, Pharmaceut Sci Res Ctr, Tehran 14174, Iran

来源：

PHARMACEUTICAL CHEMISTRY JOURNAL | 2019年 / 53卷 / 06期

关键词：

synthesis; bioisosteric change; 1,3,4-thiadiazole; MTT; caspase activity; TYROSINE KINASE INHIBITORS; BIOLOGICAL EVALUATION; 1,3,4-THIADIAZOLE DERIVATIVES; MOLECULAR DOCKING; ANTICANCER; CYTOTOXICITY; CANCER; DISCOVERY; SERIES; CELL;

D O I：

10.1007/s11094-019-02031-x

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

New 1,3,4-thiadiazole-based compounds were designed, synthesized, and their anticancer effects were assessed by MTT assay against PC3 (prostate cancer), HT-29 (colon cancer), and SKNMC (neuroblastoma) cell lines. The results were compared to that of doxorubicin. According to MTT assay, some of the synthesized compounds exhibit higher cytotoxic activity (IC50, mu M range) than doxorubicin against PC3 and SKNMC cells but not HT29 cells. According to the analysis of structure - activity relationship, compounds with methoxy group as an electron donating moiety rendered higher activity than nitro group as an electron withdrawing group. Compound 4d with ortho position of methoxy moiety activated caspases 3 and 9 in both PC3 and HT-29 cell lines.

引用

页码：521 / 526

页数：6

共 34 条

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