One-Pot Synthesis of Novel 2-Imino-5-Arylidine-Thiazolidine Analogues and Evaluation of Their Anti-Proliferative Activity against MCF7 Breast Cancer Cell Line |
| |
| Authors: | Marian N. Aziz Arzoo Patel Amany Iskander Avisankar Chini Delphine Gout Subhrangsu S. Mandal Carl J. Lovely |
| |
| Affiliation: | 1.Department of Chemistry and Biochemistry, University of Texas-Arlington, Arlington, TX 76019-0065, USA; (M.N.A.); (A.P.); (A.I.); (A.C.); (D.G.); (S.S.M.);2.Department of Pesticide Chemistry, National Research Centre, Dokki, Giza 12622, Egypt |
| |
| Abstract: | 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. |
| |
| Keywords: | hydrothiolation propargyl amine surface-mediated cyclization cytotoxicity X-ray |
|
|
