Novel spiro ‐thiazolidin‐4‐one and thioether derivatives of benzylidene flavanones: New leads in cancer and microbial chemotherapy

Abstract The synthesis of spiro‐thiazolidin‐4‐one and thioether derivatives of substituted E‐3‐benzylidene flavanones is reported for the first time. All new compounds were characterized by different spectroscopic techniques and elemental analyses. The in vitro anticancer activities were assessed against the full NCI 60 cell line panel representing nine types of human cancers, at 10‐fold dilutions at five different concentrations (0.01, 0.1, 1, 10, and 100 μM. Compound 2a gave noteworthy results in the case of colon (HT29), CNS (SNB‐75), melanoma (LOX‐IMVI), and renal (ACNH) cells, where the reduction in growth was found at 54, 54, 70, and 77%, respectively, at 10−4 M concentration. All new compounds were also evaluated for in vitro antimicrobial activity against bacterial and fungal strains, and the results showed that most of the compounds exhibited moderate to good antimicrobial activity compared to the reference drugs amoxicillin and fluconazole. These compounds could be useful leads in cancer and microbial chemotherapy which need to be further explored in order to discover and develop better and safer therapeutic agents against cancer and infectious diseases. New derivatives of E‐3‐benzylidene flavanones were synthesized and evaluated for anticancer and antimicrobial activities. Compound 2a showed noteworthy activity on colon, CNS, melanoma, and renal cancer cells. Most of the compounds also displayed higher antimicrobial activity than the ref...
Source: Archiv der Pharmazie - Category: Drugs & Pharmacology Authors: Tags: FULL PAPER Source Type: research