Literature DB >> 25827522

Synthesis and evaluation of benzosuberone embedded with 1,3,4-oxadiazole, 1,3,4-thiadiazole and 1,2,4-triazole moieties as new potential anti proliferative agents.

Bandi Yadagiri1, Srikanth Gurrala1, Rajashaker Bantu1, Lingaiah Nagarapu2, Sowjanya Polepalli3, Garimella Srujana3, Nishant Jain3.   

Abstract

As an aspect of our ongoing research in search of new anti proliferative agents, a series of novel analogs of benzosuberone embedded with 1,3,4-oxadiazole, 1,3,4-thiadiazole and 1,2,4-triazole moieties were synthesized in excellent yields (82-93%). All the newly synthesized compounds were characterized by (1)H NMR, (13)C NMR, ESI/LC-MS, HRMS and evaluated for their in vitro anti proliferative activity against four human cancer cell lines (cervical, breast, pancreatic and alveolar). Among the synthesized compounds, 4b, 6a, 7d and 7l showed potent anti proliferative activity with GI50 values range of 0.079-0.957μM against four human cancer cell lines. However, it was revealed that the compound 7d have shown very close GI50 value 0.079μM as compared with positive control of colchicine against cervical cancer cell line.
Copyright © 2015 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  1,2,4-Triazole; 1,3,4-Oxadiazole; 1,3,4-Thiadiazole; Anti-proliferative; Benzosuberone; Cell lines

Mesh:

Substances:

Year:  2015        PMID: 25827522     DOI: 10.1016/j.bmcl.2015.03.032

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  14 in total

1.  Design, Synthesis, and Biological Evaluation of Novel 1,3,4-Thiadiazole Derivatives as Potential Antitumor Agents against Chronic Myelogenous Leukemia: Striking Effect of Nitrothiazole Moiety.

Authors:  Mehlika Dilek Altıntop; Halil Ibrahim Ciftci; Mohamed O Radwan; Belgin Sever; Zafer Asım Kaplancıklı; Taha F S Ali; Ryoko Koga; Mikako Fujita; Masami Otsuka; Ahmet Özdemir
Journal:  Molecules       Date:  2017-12-27       Impact factor: 4.411

2.  Design, Synthesis and Molecular Docking Study of Novel 3-Phenyl-β-Alanine-Based Oxadiazole Analogues as Potent Carbonic Anhydrase II Inhibitors.

Authors:  Kashif Rafiq; Najeeb Ur Rehman; Sobia Ahsan Halim; Majid Khan; Ajmal Khan; Ahmed Al-Harrasi
Journal:  Molecules       Date:  2022-01-26       Impact factor: 4.411

3.  Novel heterocyclic 1,3,4-oxadiazole derivatives of fluoroquinolones as a potent antibacterial agent: Synthesis and computational molecular modeling.

Authors:  Tejeswara Rao Allaka; Bhaskar Kummari; Naveen Polkam; Naveen Kuntala; Kalyani Chepuri; Jaya Shree Anireddy
Journal:  Mol Divers       Date:  2021-08-02       Impact factor: 2.943

Review 4.  Antimicrobial Activity of 1,3,4-Oxadiazole Derivatives.

Authors:  Teresa Glomb; Piotr Świątek
Journal:  Int J Mol Sci       Date:  2021-06-29       Impact factor: 5.923

5.  Synthesis, Structural Studies and Biological Evaluation of Connections of Thiosemicarbazide, 1,2,4-Triazole and 1,3,4-Thiadiazole with Palmitic Acid.

Authors:  Michał Jóźwiak; Karolina Stępień; Małgorzata Wrzosek; Wioletta Olejarz; Grażyna Kubiak-Tomaszewska; Anna Filipowska; Wojciech Filipowski; Marta Struga
Journal:  Molecules       Date:  2018-04-03       Impact factor: 4.411

6.  Synthesis, Molecular Docking and Anticancer Activity of Diflunisal Derivatives as Cyclooxygenase Enzyme Inhibitors.

Authors:  Göknil Pelin Coşkun; Teodora Djikic; Taha Bartu Hayal; Nezaket Türkel; Kemal Yelekçi; Fikrettin Şahin; Ş Güniz Küçükgüzel
Journal:  Molecules       Date:  2018-08-06       Impact factor: 4.411

7.  Synthesis and Cytotoxic Activity of New 1,3,4-Thiadiazole Thioglycosides and 1,2,3-Triazolyl-1,3,4-Thiadiazole N-glycosides.

Authors:  Fahad M Alminderej; Hussein H Elganzory; Mohamed N El-Bayaa; Hanem M Awad; Wael A El-Sayed
Journal:  Molecules       Date:  2019-10-16       Impact factor: 4.411

Review 8.  Cytotoxic Properties of 1,3,4-Thiadiazole Derivatives-A Review.

Authors:  Sara Janowska; Agata Paneth; Monika Wujec
Journal:  Molecules       Date:  2020-09-20       Impact factor: 4.411

Review 9.  Groundbreaking Anticancer Activity of Highly Diversified Oxadiazole Scaffolds.

Authors:  Alessandra Benassi; Filippo Doria; Valentina Pirota
Journal:  Int J Mol Sci       Date:  2020-11-18       Impact factor: 5.923

10.  New 1,3,4-Thiadiazole Derivatives with Anticancer Activity.

Authors:  Sara Janowska; Dmytro Khylyuk; Anna Bielawska; Anna Szymanowska; Agnieszka Gornowicz; Krzysztof Bielawski; Jarosław Noworól; Sławomir Mandziuk; Monika Wujec
Journal:  Molecules       Date:  2022-03-10       Impact factor: 4.411

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