Synthesis of Novel Diaziridinyl Quinone Isoxazole Hybrids and Evaluation of Their Anti-Cancer Activity as Potential Tubulin-Targeting Agents (vol 69, pg 406, 2019)

被引：0

作者：

Kumar, P. Ravi

Yennam, Satyanarayana

Raghavulu, K.

Velatooru, Loka Reddy

Kotla, Siva Reddy

Penugurti, Vasudevarao

Hota, Prasanta K.

Behera, Manoranjan

Shree, A. Jaya

机构：

[1] Department of Medicinal Chemistry, GVK Biosciences Pvt. Ltd., Plot No's 125(part) & 126 IDA Mallapur, Hyderabad Telangana

[2] Centre for Chemical Sciences and Technology, Institute of Science and Technology, JNT University, Telangana

[3] Biochemistry Department, School of Life Sciences, University of Hyderabad, Telangana

[4] Department of Chemistry, School of Sciences, HNBG University, Uttarakhand

来源：

DRUG RESEARCH | 2019年 / 69卷 / 07期

关键词：

aziridine; cytotoxicity; diaziridinyl quinone isoxazole; isoxazole; molecular docking; quinone;

D O I：

10.1055/a-0852-0469

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Two series of diaziridinyl quinone isoxazole derivatives were prepared and evaluated for their cytotoxic activity against MCF7, HeLa, BT549, A549 and HEK293 cell lines and interaction with tubulin. Compounds (6a-m) showed promising activity against all the 5 human cancer cell lines. Compounds 6a, 6e and 6 m were potent [IC 50 ranging between 2.21 μg to 2.87 μg] on ER-positive MCF7 cell line similar to the commercially available drug molecule Doxorubicin. The results from docking models are in consistent with the experimental values which demonstrated the favourable binding modes of compounds 6a-m to the interface of α- and β-tubulin dimer. © 2019 Georg Thieme Verlag KG Stuttgart New York.

引用

页码：406 / 414

页数：1