Synthesis of Substituted Aryl Incorporated Oxazolo[4,5-b]Pyridine-Triazole Derivatives: Anticancer Evaluation and Molecular Docking Studies

被引：16

作者：

Sireesha, Reddymasu ^{[1
]}

Tej, Mandava Bhuvan ^{[2
]}

Poojith, Nuthalapati ^{[3
]}

Sreenivasulu, Reddymasu ^{[4
]}

Musuluri, Murali ^{[5
]}

Subbarao, Mannam ^{[1
]}

机构：

[1] Acharya Nagarjuna Univ, Dept Chem, Guntur 522510, Andhra Pradesh, India

[2] Sri Ramachandra Inst Higher Educ & Res, Dept Pharm, Chennai, Tamil Nadu, India

[3] PJ Biousys LLC, Irving, TX USA

[4] Jawaharlal Nehru Technol Univ, Univ Coll Engn Autonomous, Dept Chem, Kakinada, Andhra Pradesh, India

[5] RVR & JC Coll Engn, Dept Chem, Guntur, Andhra Pradesh, India

来源：

POLYCYCLIC AROMATIC COMPOUNDS | 2023年 / 43卷 / 01期

关键词：

1; 2; 3-Triazoles; Anticancer activity; hDHODH; Molecular docking; Oxazolo[4; 5-b]pyridine; BIOLOGICAL EVALUATION; ANTIMICROBIAL EVALUATION; ELLIPTICINE DERIVATIVES; INHIBITORY-ACTIVITY; AMIDE DERIVATIVES; DESIGN; ANALOGS; POTENT; DISCOVERY; BINDING;

D O I：

10.1080/10406638.2021.2021256

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A new series of structurally modified oxazolo[4,5-b]pyridine based triazoles (18a-j) derivatives were synthesized, and designed and screened for their anticancer activities against human cancer cell lines like PC3 (prostate), A549 (lung), MCF-7 (breast), and DU-145 (prostate) by using MTT assay method. Most of the tested compounds exhibited good to moderate anticancer potential in comparison with etoposide. Among all, compounds 18a, 18b, 18c, 18d, 18e, and 18i displayed promising anticancer activities on four cell lines. Furthermore, molecular docking studies were carried out on human dihydroorotate dehydrogenase (hDHODH), a potential target for anticancer drugs, that is linked to proliferation, invasion, and migration of cancerous cell in acute myeloid leukemia, colorectal cancer melanoma, and pancreatic cancer cells. The investigated oxazolo[4,5-b]pyridine-based triazoles (18a-j) showed efficient inhibition of hDHODH in molecular docking studies.

引用

页码：915 / 932

页数：18

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