Design, synthesis, anticancer evaluation and molecular docking studies of 1,2,3-triazole incorporated 1,3,4-oxadiazole-Triazine derivatives

Sujana Oggu; Parameswari Akshinthala; Naresh Kumar Katari; Laxmi Kumari Nagarapu; Srimannarayana Malempati; Rambabu Gundla; Sreekantha Babu Jonnalagadda

Heliyon (May 2023)

Design, synthesis, anticancer evaluation and molecular docking studies of 1,2,3-triazole incorporated 1,3,4-oxadiazole-Triazine derivatives

Sujana Oggu,
Parameswari Akshinthala,
Naresh Kumar Katari,
Laxmi Kumari Nagarapu,
Srimannarayana Malempati,
Rambabu Gundla,
Sreekantha Babu Jonnalagadda

Affiliations

Sujana Oggu: Department of Chemistry, GITAM School of Science, GITAM (Deemed to be University), Hyderabad, Telangana, 502 329, India; G. Narayanamma Institute of Technology & Science, Hyderabad, Telangana, 500 104, India
Parameswari Akshinthala: Department of Science and Humanities, MLR Institute of Technology, Dundigal, Medchal, Hyderabad, Rudraram, 500043, India
Naresh Kumar Katari: Department of Chemistry, GITAM School of Science, GITAM (Deemed to be University), Hyderabad, Telangana, 502 329, India; School of Chemistry & Physics, College of Agriculture, Engineering & Science, Westville Campus, University of KwaZulu-Natal, P Bag X 54001, Durban, 4000, South Africa
Laxmi Kumari Nagarapu: Department of Chemistry, GITAM School of Science, GITAM (Deemed to be University), Hyderabad, Telangana, 502 329, India
Srimannarayana Malempati: Department of Chemistry, GITAM School of Science, GITAM (Deemed to be University), Hyderabad, Telangana, 502 329, India; Corresponding author.
Rambabu Gundla: Department of Chemistry, GITAM School of Science, GITAM (Deemed to be University), Hyderabad, Telangana, 502 329, India; Corresponding author.
Sreekantha Babu Jonnalagadda: School of Chemistry & Physics, College of Agriculture, Engineering & Science, Westville Campus, University of KwaZulu-Natal, P Bag X 54001, Durban, 4000, South Africa; Corresponding author.

Journal volume & issue: Vol. 9, no. 5
p. e15935

Abstract

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A new library of 1,2,3-triazole-incorporated 1,3,4-oxadiazole-triazine derivatives (9a-j) was designed, synthesized, and tested in vitro for anticancer activity against PC3 and DU-145 (prostate cancer), A549 (lung cancer), and MCF-7 (breast cancer) cancer cell lines using the MTT assay with etoposide as the control drug. The compounds exhibited remarkable anticancer activity, with IC50 values ranging from 0.16 ± 0.083 μM to 11.8 ± 7.46 μM, whereas the positive control ranged from 1.97 0.45 μM to 3.08 0.135 μM. Compound 9 d with a 4-pyridyl moiety shown exceptional anticancer activity against PC3, A549, MCF-7, and DU-145 cell lines, with IC50 values of 0.17 ± 0.063 μM, 0.19 ± 0.075 μM, 0.51 ± 0.083 μM, and 0.16 ± 0.083 μM, respectively.

Published in Heliyon

ISSN: 2405-8440 (Online)
Publisher: Elsevier
Country of publisher: United Kingdom
LCC subjects: Science: Science (General); Social Sciences: Social sciences (General)
Website: https://www.cell.com/heliyon/home

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