Design, Synthesis and Anticancer Evaluation of Acetamides Comprising 1,2,3-triazole, 1,3,4-thiadiazole and Isothiazolo[4,3-b]pyridine Rings
Shaik Shahinshavali, Poojith Nuthalapati, Venkat Rao Guttikonda, Reddymasu Sreenivasulu, Mandava Venkata Basaveswara Rao
Abstract
We have synthesized a library of new 1,2,3-triazole incorporated 1,3,4-thiadiazoleisothiazolo[ 4,3-b]pyridine derivatives 12a-j and have screened these products for their anticancer activities against four human cancer cell lines such as MCF-7 (breast cancer), A549 (lung cancer), DU-145 (prostate cancer), and MDA MB-231 (breast cancer) using MTT assay with etoposide as a positive control. Among them, compound 12e has shown excellent activities against MCF-7, A549, DU-145, and MDA-MB-231 with IC50 values of 0.53±0.055 μM, 0.18±0.077 μM, 0.10±0.082 μM, and 0.92±0.041 μM, respectively.
Topics & Concepts
ChemistryPyridineEtoposideIC50TriazoleMTT assayCancerLung cancerBreast cancerStereochemistryCombinatorial chemistryIn vitroMedicinal chemistryOncologyBiochemistryInternal medicineOrganic chemistryChemotherapyMedicineSynthesis and biological activitySynthesis and Characterization of Heterocyclic CompoundsSynthesis and Biological Evaluation