One-Pot Synthesis of Novel 2-Imino-5-Arylidine-Thiazolidine Analogues and Evaluation of Their Anti-Proliferative Activity against MCF7 Breast Cancer Cell Line

被引：4

作者：

Aziz, Marian N. ^{[1
,2
]}

Patel, Arzoo ^{[1
]}

Iskander, Amany ^{[1
]}

Chini, Avisankar ^{[1
]}

Gout, Delphine ^{[1
]}

Mandal, Subhrangsu S. ^{[1
]}

Lovely, Carl J. ^{[1
]}

机构：

[1] Univ Texas Arlington, Dept Chem & Biochem, Arlington, TX 76019 USA

[2] Natl Res Ctr, Dept Pesticide Chem, Giza 12622, Egypt

来源：

MOLECULES | 2022年 / 27卷 / 03期

关键词：

hydrothiolation; propargyl amine; surface-mediated cyclization; cytotoxicity; X-ray; PROPARGYL AMINES; IONIC LIQUID; THIAZOLIDINE; ANTICANCER; EFFICIENT; CATALYST; 1,3-THIAZOLIDIN-4-ONES; ANTICONVULSANT; FUNCTIONALITY; DERIVATIVES;

D O I：

10.3390/molecules27030841

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：

An efficient surface-mediated synthetic method to facilitate access to a novel class of thiazolidines is described. The rationale behind the design of the targeted thiazolidines was to prepare stable thiazolidine analogues and evaluate their anti-proliferative activity against a breast cancer cell line (MCF7). Most of the synthesized analogues exhibited increased potency ranging from 2-15-fold higher compared to the standard reference, cisplatin. The most active thiazolidines contain a halogenated or electron withdrawing group attached to the N-phenyl ring of exocyclic 2-imino group. However, combination of the two substituents did not enhance the activity. The anti-proliferative activity was measured in terms of IC50 values using an MTT assay.

引用

页数：15

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