Synthesis of various fused heterocyclic rings from thiazolopyridine and their pharmacological and antimicrobial evaluations

被引：18

作者：

Mahmoud, Naglaa F. H. ^{[1
]}

Balamon, Mina G. ^{[1
]}

机构：

[1] Ain Shams Univ, Fac Sci, Dept Chem, Cairo 11566, Egypt

来源：

JOURNAL OF HETEROCYCLIC CHEMISTRY | 2020年 / 57卷 / 08期

关键词：

RAPID COLORIMETRIC ASSAY; IN-VITRO; PART; DERIVATIVES; THIAZOLE; SURVIVAL; GROWTH;

D O I：

10.1002/jhet.4011

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Various fused-heterocyclic-derivatives containing thiazolopyridine moieties has been synthesized by allowing 5-aminothiazolo[3,2-a]pyridine derivative 1 to undergo annulations reactions with different reagents under different-reaction conditions. The biological assessment of compounds 2, 11, 14, 15, and 19 showed remarkable antimicrobial activities. In addition, selected derivatives of the products were screened for their anticancer activities against two tumor cell lines using MTT assay and the results showed that some of these compounds have potent cytotoxic effect, as concluded from their IC50 values. Meanwhile, compounds 3a, 7 have exhibited very strong potency as anticancer candidates. Thiazolopyridine structures have been confirmed as a useful lead compounds for the development of new anticancer agents. Molecular docking showed that,-some of the synthesized compounds more suitable inhibitor against-ALR2 with farther alteration in future.

引用

页码：3056 / 3070

页数：15

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