Literature DB >> 31880237

Synthesis, Antimicrobial and Antitumor Evaluations of a New Class of Thiazoles Substituted on the Chromene Scaffold.

Dina H Elnaggar1, Naglaa A Abdel Hafez1, Huda R M Rashdan2, Nayera A M Abdelwahed2, Hanem M Awad3, Korany A Ali1,4.   

Abstract

BACKGROUND &
OBJECTIVE: A new series of thiazoles substituted on the chromene scaffold were prepared by facial approaches starting from (E)-1-(2,3-Dihydrochromen-4-ylidene)thiosemicarbazide derivatives (2a,b). The thiosemicarbazides (2a,b) were reacted with a series of α-halo carbonyl compounds to give the corresponding rhodanine analogues and reacted also with C-acetyl-or Cethoxy- N-hydrazonoyl chlorides to afford the corresponding tri- and tetra-substituted hybrid hydrazinyl thiazole substituted chromenes.
METHODS: The newly synthesized compounds were screened for their in vitro antimicrobial and antitumor activities by agar diffusion method and MTT assay, respectively.
RESULTS: The results of the antimicrobial activity revealed that some of the new compounds exhibited excellent activity against pathogenic microorganism; Candida albicans compared with Ciprofloxacin and nystatin, as the reference drugs. All of the tested compounds exhibited significant cytotoxic activities comparable to that of the reference drug; Doxorubicin® (on HCT116 (colorectal carcinoma human cell line). Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.

Entities:  

Keywords:  HCT116 (colorectal carcinoma); MTT assay; Thiosemicarbazide; antimicrobial activity; chromene scaffold; hydrazonoyl chlorides.

Mesh:

Substances:

Year:  2019        PMID: 31880237     DOI: 10.2174/1389557519666190722123422

Source DB:  PubMed          Journal:  Mini Rev Med Chem        ISSN: 1389-5575            Impact factor:   3.862


  5 in total

1.  Novel Thiadiazole-Based Molecules as Promising Inhibitors of Black Fungi and Pathogenic Bacteria: In Vitro Antimicrobial Evaluation and Molecular Docking Studies.

Authors:  Huda R M Rashdan; Mohamad T Abdelrahman; Ihsan A Shehadi; Sara S El-Tanany; Bahaa A Hemdan
Journal:  Molecules       Date:  2022-06-04       Impact factor: 4.927

2.  Simultaneous removal of Pb2+ and direct red 31 dye from contaminated water using N-(2-hydroxyethyl)-2-oxo-2H-chromene-3-carboxamide loaded chitosan nanoparticles.

Authors:  Mehrez E El-Naggar; Emad K Radwan; Huda R M Rashdan; Shaimaa T El-Wakeel; Asmaa A Koryam; Ahmed Sabt
Journal:  RSC Adv       Date:  2022-06-29       Impact factor: 4.036

3.  New Potent 5α- Reductase and Aromatase Inhibitors Derived from 1,2,3-Triazole Derivative.

Authors:  Mohamed El-Naggar; Amira S Abd El-All; Shweekar I A El-Naem; Mohamed M Abdalla; Huda R M Rashdan
Journal:  Molecules       Date:  2020-02-05       Impact factor: 4.411

4.  Synthesis, Anticancer Evaluation, Computer-Aided Docking Studies, and ADMET Prediction of 1,2,3-Triazolyl-Pyridine Hybrids as Human Aurora B Kinase Inhibitors.

Authors:  Huda R M Rashdan; Ihsan A Shehadi; Abobakr H Abdelmonsef
Journal:  ACS Omega       Date:  2021-01-05

5.  Solvent-Free Synthesis, In Vitro and In Silico Studies of Novel Potential 1,3,4-Thiadiazole-Based Molecules against Microbial Pathogens.

Authors:  Ihsan A Shehadi; Mohamad T Abdelrahman; Mohamed Abdelraof; Huda R M Rashdan
Journal:  Molecules       Date:  2022-01-06       Impact factor: 4.411

  5 in total

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