Synthesis and Anticancer Activity of Novel Urea and Thiourea Bearing Thiophene-2-carboxalate Derivatives

被引：1
|
作者：
Gulipalli, K. Ch. [1 ]
Ravula, P. [2 ]
Bodige, S. [1 ]
Endoori, S. [1 ]
Cherukumalli, P. Koteswara Rao [1 ]
Chandra, J. N. Narendra Sharath [3 ]
Seelam, N. [1 ]
机构：
[1] Koneru Lakshmaiah Educ Fdn, Dept Chem, Guntur 522502, Andhra Pradesh, India
[2] Gurunanak Inst Tech Campus, Dept Pharmaceut Chem, Sch Pharm, Hyderabad 501506, Telangana, India
[3] Gurukrupa Inst Pharm, Dept Pharmaceut Chem, Majalgaon 431129, Maharashtra, India
来源：
RUSSIAN JOURNAL OF GENERAL CHEMISTRY | 2020年 / 90卷 / 07期
关键词：
synthesis; thiophene-2-carboxalate; urea; thiourea; anticancer activity; molecular docking; protein tyrosine phosphatase inhibitor; TYROSINE-PHOSPHATASE; 1B; BIOLOGICAL EVALUATION; THIOPHENE DERIVATIVES; PYRAZOLE DERIVATIVES; IN-SILICO; DESIGN; IDENTIFICATION; DOCKING;
D O I：
10.1134/S1070363220070221
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
A new series of urea and thiourea bearing thiophene-2-carboxalate derivatives has been designed against protein tyrosine phosphatase 1B (PTP1B) active site, synthesized and charecterized by(1)H and(13)C NMR, and mass spectra. The compounds have been evaluated for in vitro anticancer activity against different cancer cell lines using the MTT colorimetric assay and doxorubicin as a standard drug. Among the tested compounds, methyl 3-methoxy-4-{4-[3-(4-methoxyphenyl)thioureido]phenyl}thiophene-2-carboxylate demonstrates the highest inhibitory activity against MCF-7, K562, HepG2, MDA-MB-231, and HeLa cell lines. The new molecular structures and their interactions with PNP1B have been evaluated by docking studies.
引用
收藏
页码：1336 / 1344
页数：9
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