Synthesis, Evaluation and Docking Studies of Disubstituted N‐Heterocyclic Derivatives as Anticancer Agents

Cancer is a chronic disease reported with alarming rates of mortalities every year. Herein, we reported the synthesis of nitrogen based novel heterocyclic disubstituted derivatives and evaluated them against L929 and A549 cell lines using MTT assay. Among all, 6a2 and 6c1 were significantly active against L929 with IC<sub>50</sub> value of 2.61±9.58 and 2.64±8.97 μg/mL respectively. Compounds 6a2 and 6c1 were also active against A549 with IC<sub>50</sub> value of 2.36±9.20 and 2.43±6.28 μg/mL respectively and were found to be more potent than the standard drug Doxorubicin. A molecular docking study of the active compounds was also done against EGFR, conferring good binding affinity and binding interactions. Further biological investigations may provide valuable insights towards exploring the therapeutic potential of the active compounds in future.

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Journal
Chemistry & Biodiversity
Published
2024-08-23
DOI
https://doi.org/10.1002/cbdv.202401010
Primary Topic
Synthesis and biological activity
Type
article
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article

Synthesis, Evaluation and Docking Studies of Disubstituted N‐Heterocyclic Derivatives as Anticancer Agents

Vivek Panwar, Manish Jain, Ankan Kumar Sarkar, Deepak Kumar et al.
Chemistry & Biodiversity
Synthesis and biological activity
article

Synthesis, Evaluation and Docking Studies of Disubstituted N‐Heterocyclic Derivatives as Anticancer Agents

Vivek Panwar, Manish Jain, Ankan Kumar Sarkar, Deepak Kumar, Kothapalli Bannoth Tejaswini, Sreenivasulu Reddy Gopireddy, Kothapalli Bannoth Chandrasekhar
article en

Abstract

Cancer is a chronic disease reported with alarming rates of mortalities every year. Herein, we reported the synthesis of nitrogen based novel heterocyclic disubstituted derivatives and evaluated them against L929 and A549 cell lines using MTT assay. Among all, 6a2 and 6c1 were significantly active against L929 with IC<sub>50</sub> value of 2.61±9.58 and 2.64±8.97 μg/mL respectively. Compounds 6a2 and 6c1 were also active against A549 with IC<sub>50</sub> value of 2.36±9.20 and 2.43±6.28 μg/mL respectively and were found to be more potent than the standard drug Doxorubicin. A molecular docking study of the active compounds was also done against EGFR, conferring good binding affinity and binding interactions. Further biological investigations may provide valuable insights towards exploring the therapeutic potential of the active compounds in future.

Chemistry & BiodiversityVol. 21(12)
Shoolini University (IN), Indian Institute of Science Education and Research, Tirupati (IN), Panjab University (IN), Jawaharlal Nehru Technological University Anantapur (IN)
Good health and well-being
Openalex Percentile: Top 90%
Synthesis and biological activity
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Synthesis, Evaluation and Docking Studies of Disubstituted N‐Heterocyclic Derivatives as Anticancer Agents — Vivek Panwar, Manish Jain, et al. · Chemistry & Biodiversity (2024) | TGRS Research Map | TGRS