Synthesis and evaluation of thiazolidinone-pyrazole conjugates as anticancer and antimicrobial agents

被引：40

作者：

Bhat, Mahima ^{[1
]}

Poojary, Boja ^{[1
]}

Kalal, Bhuvanesh Sukhlal ^{[2
,3
]}

Matada, Purawarga

Swamy, Gurubasavaraja ^{[4
]}

Kabilan, Senthamaraikannan ^{[5
]}

Kumar, Vasantha ^{[6
]}

Shruthi, Nooji ^{[1
]}

Anand, Selvam Athavan Alias ^{[5
]}

Pai, Vinitha Ramanath ^{[2
]}

机构：

[1] Mangalore Univ, Dept Chem, Mangalagangothri 574199, Karnataka, India

[2] Yenepoya Univ, Dept Biochem, Yenepoya Med Coll, Mangaluru, Karnataka, India

[3] Yenepoya Univ, Yenepoya Res Ctr, Mangaluru, Karnataka, India

[4] Acharya & BM Reddy Coll Pharm, Med Chem Res Lab, Bangalore 560090, Karnataka, India

[5] Annamalai Univ, Dept Chem, Drug Discovery Lab, Annamalainagar 608002, Tamil Nadu, India

[6] SDM Coll Autonomous, Dept Chem, Ujire 574240, Karnataka, India

来源：

FUTURE MEDICINAL CHEMISTRY | 2018年 / 10卷 / 09期

关键词：

A375; ADME parameters; anticancer activity; cytotoxicity; HDF; MDA-MB-231; MDM2; molecular docking; molecular dynamics simulation; N-arylpyrazole; p53; thiazolidin-4-one; EHRLICH ASCITES-CARCINOMA; BIOLOGICAL EVALUATION; POTENTIAL ANTICANCER; MDM2-P53; INTERACTION; DRUG DISCOVERY; DERIVATIVES; INHIBITORS; ANTITUMOR; P53; 4-THIAZOLIDINONES;

D O I：

10.4155/fmc-2017-0191

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Aim: To synthesize a series of new thiazolidinone-pyrazole hybrids (5a-o) and assess their anticancer (in vitro and in vivo) and antimicrobial activities. Results: The compounds 5h (against Ehrlich ascites carcinoma cells), 5e and 5i (against the human breast cancer [MDA-MB231] cell line) exhibited potent anticancer activity. All the compounds except 5g and 5e found to be less toxic for the human dermal fibroblast cells. The effective interactions of the compounds in silico with MDM2 exemplified their inhibitory potency. The derivatives also showed moderate antimicrobial activity. Conclusion: The halogen atoms on various positions of the N-arylamino ring played an advantageous role in elevating the potency of the molecules. Thus, these conjugates could be used as a lead for further optimization to achieve promising therapeutics. [GRAPHICS] .

引用

页码：1017 / 1036

页数：20

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