Design, Synthesis, Anticancer Evaluation, and Molecular Docking Studies of Oxazole‐Incorporated Naphthyridine Derivatives

Author:

Rangaswamy Singamsetty1,Sreenivasulu Reddymasu2,Babu Vankayala Ramesh1,Syed Tasqeeruddin3,Kapavarapu Ravi Kumar4,Jayaprakash Hulikunte Veeranna5,Abbaraju Venkata Durga Nagendra Kumar1ORCID

Affiliation:

1. Department of Chemistry GITAM School of Science Gandhi Institute of Technology and Management (Deemed to be University) Visakhapatnam Andhra Pradesh 530045 India

2. Department of Chemistry University College of Engineering (Autonomous) Jawaharlal Nehru Technological University Kakinada Andhra Pradesh 533003 India

3. Department of Pharmaceutical Chemistry College of Pharmacy King Khalid University Abha Saudi Arabia

4. Department of Pharmaceutical Chemistry and Phytochemistry Nirmala College of Pharmacy Atmakur, Mangalagiri Andhra Pradesh 522503 India

5. Department of Chemistry Sri Siddartha Institute of Technology Sri Siddartha Academy of Higher Education (Deemed to be University) Tumkur Karnataka 572107 India

Abstract

AbstractA novel series of oxazole incorporated naphthyridine (21 aj) derivatives were designed and, synthesized followed by screening of their anticancer activity profiles against human breast cancer (MCF‐7), human lung cancer (A549) and human prostate (PC3 & DU‐145) cancer cell lines by employing MTT [3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyl‐2H‐tetrazolium bromide] assay using etoposide as the positive control. Of these compounds, N‐(6‐chloro‐3‐(4‐(3,4,5‐trimethoxyphenyl)oxazol‐2‐yl)‐1,5‐naphthyridin‐4‐yl)oxazol‐2‐amine with 3,4,5‐trimethoxy substituent on the aryl moiety attached to oxazole ring showed potent anticancer activity against PC3, A549, MCF‐7, and DU‐145 cell lines with IC50 values of 0.13±0.095 μM; 0.10±0.084 μM; 0.18±0.087 μM and 0.15±0.076 μM respectively. Apart from this, compounds N‐(6‐chloro‐3‐(4‐(3,5‐dimethoxyphenyl)oxazol‐2‐yl)‐1,5‐naphthyridin‐4‐yl)oxazol‐2‐amine, N‐(6‐chloro‐3‐(4‐(4‐methoxyphenyl)oxazol‐2‐yl)‐1,5‐naphthyridin‐4‐yl)oxazol‐2‐amine, and N‐(6‐chloro‐3‐(4‐(3,5‐dimethylphenyl)oxazol‐2‐yl)‐1,5‐naphthyridin‐4‐yl)oxazol‐2‐amine also showed better anticancer activities against four cancer cell lines screened for. These activities were also validated through the molecular docking simulations, which further indicated demonstration of better interaction energy and profile by these compounds.

Funder

King Khalid University

Publisher

Wiley

Subject

Molecular Biology,Molecular Medicine,General Chemistry,Biochemistry,General Medicine,Bioengineering

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