Literature DB >> 25765907

Synthesis, in vitro anticancer and antimycobacterial evaluation of new 5-(2,5-dimethoxyphenyl)-1,3,4-thiadiazole-2-amino derivatives.

Naveen Polkam1, Parsharamulu Rayam1, Jaya Shree Anireddy2, Satyanarayana Yennam3, Hasitha Shilpa Anantaraju4, Sriram Dharmarajan4, Yogeeswari Perumal4, Sudha Sravanti Kotapalli5, Ramesh Ummanni5, Sridhar Balasubramanian6.   

Abstract

A series of 2,5-disubstituted-1,3,4-thiadiazole derivatives 5a-5l, 7a-7e and 9 have been synthesised and screened for in vitro antimycobacterial activity against Mycobacterium smegmatis MC-155. In addition these compounds have also been screened for cytotoxic activity against cancer cell lines HT-29, MDA-MB-231 by MTT colorimetric assay. The compounds are well characterized by spectral analysis viz. (1)H NMR, (13)C NMR, FT-IR, mass and HRMS. Screening results indicate that compounds 5g, 7a possess good antitubercular activity with MIC value 65.74 and 40.86, respectively, compounds 5g, 7a, 7b, 7d, 7e and 9 displayed promising cytotoxic activity against the cell lines tested. 5g and 7a stand out to be potent antimycobacterial and anticancer agents among the tested series. Further the title compounds were also tested on human normal cells HEK293T and are found to be safer with lesser cytotoxicity. It is interesting to observe that compound 5g has come out to be safer, potent anticancer and antimycobacterial agent.
Copyright © 2015 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  2,5-Disubstitued-1,3,4-thiadiazole; Anti-mycobacterial activity; Cytotoxic activity; In vitro studies; MTT colorimetric assay

Mesh:

Substances:

Year:  2015        PMID: 25765907     DOI: 10.1016/j.bmcl.2015.02.052

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


  7 in total

1.  An integrated approach towards the development of novel antifungal agents containing thiadiazole: synthesis and a combined similarity search, homology modelling, molecular dynamics and molecular docking study.

Authors:  Mustafa Er; Abdulati Miftah Abounakhla; Hakan Tahtaci; Ali Hasin Bawah; Süleyman Selim Çınaroğlu; Abdurrahman Onaran; Abdulilah Ece
Journal:  Chem Cent J       Date:  2018-11-23       Impact factor: 4.215

2.  Spectroscopic Studies of Dual Fluorescence in 2-(4-Fluorophenylamino)-5-(2,4-dihydroxybenzeno)-1,3,4-thiadiazole: Effect of Molecular Aggregation in a Micellar System.

Authors:  Grzegorz Czernel; Arkadiusz Matwijczuk; Dariusz Karcz; Andrzej Górecki; Agnieszka Niemczynowicz; Aleksandra Szcześ; Grzegorz Gładyszewski; Alicja Matwijczuk; Bożena Gładyszewska; Andrzej Niewiadomy
Journal:  Molecules       Date:  2018-11-02       Impact factor: 4.411

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.  A comparison between observed and DFT calculations on structure of 5-(4-chlorophenyl)-2-amino-1,3,4-thiadiazole.

Authors:  Nagaraju Kerru; Lalitha Gummidi; Sandeep V H S Bhaskaruni; Surya Narayana Maddila; Parvesh Singh; Sreekantha B Jonnalagadda
Journal:  Sci Rep       Date:  2019-12-17       Impact factor: 4.379

5.  Synthesis of novel cytotoxic tetracyclic acridone derivatives and study of their molecular docking, ADMET, QSAR, bioactivity and protein binding properties.

Authors:  Rajkumar Veligeti; Rajesh Bagepalli Madhu; Jayashree Anireddy; Visweswara Rao Pasupuleti; Vijaya Kumar Reddy Avula; Krishna S Ethiraj; Srinivas Uppalanchi; Sivaprasad Kasturi; Yogeeswari Perumal; Hasitha Shilpa Anantaraju; Naveen Polkam; Mallilkarjuna Reddy Guda; Swetha Vallela; Grigory Vasilievich Zyryanov
Journal:  Sci Rep       Date:  2020-11-26       Impact factor: 4.379

Review 6.  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

7.  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

  7 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.