Synthesis, Characterization and in vitro Cytotoxic Evaluation of Some Novel Heterocyclic Compounds Bearing Indole Ring

Abstract

Reaction 1H-indole-3-carboxaldhyde 1 with thiosemicarbazide derivatives to give thiosemicarbazone derivatives 2a,b. Cyclization of thiosemicarbazone 2a with HCl, Ac 2 O, phenacyl bromides and chloroacetic acid afforded the corresponding 1,2,4-triazole-3-thiol derivative 3, diacetyl derivative 4 and 1,3-thiazole derivative 5 and 1,3-thiazolidin-4-ones derivative 6 respectively. Compound 6 undergoes a series of heterocyclization reactions to give new heterocyclic compounds. The structure of the newly synthesized compounds had been confirmed by elemental analysis and spectra data. The some newly synthesized compounds were evaluated for in vitro cytotoxic activity against three human cancer cell lines, including human liver cancer (HepG2), human colon cancer (HT-29) and human breast cancer (MCF-7) using MTT assay.

New Antimicrobial Leads in Phenothiazine Scaffold: Synthesis, Biological Assay and Virtual Screening

“…Also compounds 6 recorded relatively close MIC (5.40 μg/mL) for Pseudomonas aeruginosa microbe compared to the standard drug (4.90 μg/mL). The minimum inhibitory concentration (MIC) was considered to be the lowest concentration of the tested compound which inhibits the growth of microorganisms . It was suggested that the activity of phenothiazine derivatives against micro‐organisms is as result of interaction of pharmacophoric substituents and multicyclic ring (pi‐pi interaction, intercalation in DNA) as well as the penetration of biological membrane as result of the lipophilic character of the molecule…”

“…The synthesis of new derivatives of phenothiazine has been a subject of interest in our research group . The quest for new antimicrobial agents as a result of increasing resistance of antimicrobial drugs to emerging pathogens motivated the screening of newly synthesized derivatives of phenothiazine ,…”

2-({6-[5-Methyl-1-(4-methylphenyl)-1H-1,2,3-triazol-4-yl]imidazo[2,1-b]thiazol-5-yl}methylidene)hydrazinecarbothioamide dimethylformamide 0.25-solvate

“…Heterocyclic compounds that contain the thiosemicarbazone residue show a number of biological applications (see, for example, Salman et al, 2016;Yusuf & Jain, 2014;Abdel-Wahab et al, 2017). As part of our studies in this area, we now describe the synthesis and structure of the title solvate.…”

Synthesis and characterization of substituted acetophenone-4, 4-dimethyl-3-thiosemicarbazone derivatives with an evaluation of antimicrobial and antioxidant activities

“…Chemically, Thiosemicarbazones are generally known as Schiff base compounds and contain azomethine (-C=N-) group (Mohan et al, 2018). In the presences, azomethein group thiosemicarbazones are intermediate and form heterocyclic compounds (Salman et al, 2017) with suitable agents and also forms, metal complexes (Suvarapu et al, 2012) with metal ions due to in the presence of N and S donor atoms. The derivatives of thiosemicarbazones in organic and metal bonding compounds are of high biological importance.…”