Literature DB >> 33479622

New imidazo[2,1-b]thiazole-based aryl hydrazones: unravelling their synthesis and antiproliferative and apoptosis-inducing potential.

Mohd Adil Shareef1,2, Ganthala Parimala Devi1,2, Sunitha Rani Routhu3, C Ganesh Kumar3, Ahmed Kamal2,4, Bathini Nagendra Babu1,2.   

Abstract

Herein, we have designed and synthesized new imidazo[2,1-b]thiazole-based aryl hydrazones (9a-w) and evaluated their anti-proliferative potential against a panel of human cancer cell lines. Among the synthesized compounds, 9i and 9m elicited promising cytotoxicity against the breast cancer cell line MDA-MB-231 with IC50 values of 1.65 and 1.12 μM, respectively. Cell cycle analysis revealed that 9i and 9m significantly arrest MDA-MB-231 cells in the G0/G1 phase. In addition, detailed biological studies such as annexin V-FITC/propidium iodide, DCFH-DA, JC-1 and DAPI staining assays revealed that 9i and 9m triggered apoptosis in MDA-MB-213 cells. Overall, the current work demonstrated the cytotoxicity and apoptosis-inducing potential of 9i and 9m in breast cancer cells and suggested that they could be explored as promising antiproliferative leads in the future. This journal is © The Royal Society of Chemistry 2020.

Entities:  

Year:  2020        PMID: 33479622      PMCID: PMC7651857          DOI: 10.1039/d0md00188k

Source DB:  PubMed          Journal:  RSC Med Chem        ISSN: 2632-8682


  35 in total

1.  Mitochondria-targeted triphenylphosphonium conjugated glycyrrhetinic acid derivatives as potent anticancer drugs.

Authors:  Le Jin; Lumei Dai; Min Ji; Hengshan Wang
Journal:  Bioorg Chem       Date:  2019-01-03       Impact factor: 5.275

2.  Synthesis and apoptosis inducing studies of triazole linked 3-benzylidene isatin derivatives.

Authors:  Atulya Nagarsenkar; Lalita Guntuku; Sravanthi Devi Guggilapu; Danthi Bai K; Srinivasulu Gannoju; V G M Naidu; Nagendra Babu Bathini
Journal:  Eur J Med Chem       Date:  2016-09-04       Impact factor: 6.514

3.  Synthesis and biological evaluation of new bisindole-imidazopyridine hybrids as apoptosis inducers.

Authors:  Satish Sunkari; Srinivasa Reddy Bonam; A V Subba Rao; Sd Riyaz; V Lakshma Nayak; Halmuthur Mahabalarao Sampath Kumar; Ahmed Kamal; Bathini Nagendra Babu
Journal:  Bioorg Chem       Date:  2019-03-22       Impact factor: 5.275

Review 4.  Aldoxorubicin for the treatment of soft tissue sarcoma.

Authors:  Esha Sachdev; Divesh Sachdev; Monica Mita
Journal:  Expert Opin Investig Drugs       Date:  2017-08-28       Impact factor: 6.206

5.  Design, synthesis and antiproliferative activity of novel heterobivalent hybrids based on imidazo[2,1-b][1,3,4]thiadiazole and imidazo[2,1-b][1,3]thiazole scaffolds.

Authors:  Romeo Romagnoli; Pier Giovanni Baraldi; Filippo Prencipe; Jan Balzarini; Sandra Liekens; Francisco Estévez
Journal:  Eur J Med Chem       Date:  2015-06-25       Impact factor: 6.514

Review 6.  Activation of apoptosis signalling pathways by reactive oxygen species.

Authors:  Maureen Redza-Dutordoir; Diana A Averill-Bates
Journal:  Biochim Biophys Acta       Date:  2016-09-17

7.  Synthesis and anticancer evaluation of 3-aryl-6-phenylimidazo [2,1-b]thiazoles.

Authors:  Satish Koppireddi; Deepika Raj Kumari Chilaka; Sreenivas Avula; Jayaram Reddy Komsani; Srigiridhar Kotamraju; Rambabu Yadla
Journal:  Bioorg Med Chem Lett       Date:  2014-12-01       Impact factor: 2.823

8.  Combretastatin linked 1,3,4-oxadiazole conjugates as a Potent Tubulin Polymerization inhibitors.

Authors:  Ahmed Kamal; P S Srikanth; M V P S Vishnuvardhan; G Bharath Kumar; Korrapati Suresh Babu; S M Ali Hussaini; Jeevak Sopanrao Kapure; Abdullah Alarifi
Journal:  Bioorg Chem       Date:  2016-02-26       Impact factor: 5.275

Review 9.  N-Acylhydrazones as drugs.

Authors:  Sreekanth Thota; Daniel A Rodrigues; Pedro de Sena Murteira Pinheiro; Lídia M Lima; Carlos A M Fraga; Eliezer J Barreiro
Journal:  Bioorg Med Chem Lett       Date:  2018-07-09       Impact factor: 2.823

10.  Design, synthesis, molecular docking and biological activity evaluation of some novel indole derivatives as potent anticancer active agents and apoptosis inducers.

Authors:  Ahmed M Sh El-Sharief; Yousry A Ammar; Amany Belal; Marwa A M Sh El-Sharief; Yehia A Mohamed; Ahmed B M Mehany; Gameel A M Elhag Ali; Ahmed Ragab
Journal:  Bioorg Chem       Date:  2019-01-08       Impact factor: 5.275

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  1 in total

1.  Evaluation of antioxidant and cytotoxic properties of phenolic N-acylhydrazones: structure-activity relationship.

Authors:  Jovica Branković; Nevena Milivojević; Vesna Milovanović; Dušica Simijonović; Zorica D Petrović; Zoran Marković; Dragana S Šeklić; Marko N Živanović; Milena D Vukić; Vladimir P Petrović
Journal:  R Soc Open Sci       Date:  2022-06-08       Impact factor: 3.653

  1 in total

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