Synthesis, X-ray Analysis, Biological Evaluation and Molecular Docking Study of New Thiazoline Derivatives

被引：14

作者：

Mabkhot, Yahia N. ^{[1
]}

Algarni, H. ^{[2
,3
]}

Alsayari, Abdulrhman ^{[4
]}

Bin Muhsinah, Abdullatif ^{[4
]}

Kheder, Nabila A. ^{[5
]}

Almarhoon, Zainab M. ^{[6
]}

Al-aizari, Faiz A. ^{[6
,7
]}

机构：

[1] King Khalid Univ, Coll Pharm, Dept Pharmaceut Chem, Abha 61441, Saudi Arabia

[2] King Khalid Univ, Dept Phys, Fac Sci, POB 9004, Abha 61441, Saudi Arabia

[3] King Khalid Univ, RCAMS, POB 9004, Abha 61441, Saudi Arabia

[4] King Khalid Univ, Coll Pharm, Dept Pharmacognosy, Abha 61441, Saudi Arabia

[5] Cairo Univ, Dept Chem, Fac Sci, Giza 12613, Egypt

[6] King Saud Univ, Coll Sci, Dept Chem, POB 2455, Riyadh 11451, Saudi Arabia

[7] AL Baydha Univ, Fac Sci, Dept Chem, Albaydah 38018, Yemen

来源：

MOLECULES | 2019年 / 24卷 / 09期

关键词：

thiazoline; X-ray crystallography; molecular docking; antimicrobial activity; cytotoxic activity; 2-MERCAPTOTHIAZOLINE; ANTICANCER; 4-THIAZOLINE-2-THIONES; 2-THIAZOLINE-2-THIOL; ADSORPTION; HISTORY; BINDING; POTENT; DRUGS;

D O I：

10.3390/molecules24091654

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of new thiazoline derivatives were synthesized. Structure analyses were accomplished employing H-1-NMR, C-13-NMR, X-ray and MS techniques. The in vitro antitumor activities were assessed against human hepatocellular carcinoma (HepG-2) and colorectal carcinoma (HCT-116) cell lines. The results revealed that the thiazolines 5b and 2c exhibited significant activity against the two cell lines. The in vitro antimicrobial screening showed that the thiazolines 2c, 5b and 5d showed promising inhibition activity against Salmonella sp. Additionally, the inhibition activity of thiazolines 2e and 5b against Escherichia coli was comparable to that of the reference compound gentamycin.

引用

页数：15

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