Synthesis and evaluation of new 4(3H)-Quinazolinone derivatives as potential anticancer agents

被引：22

作者：

Gatadi, Srikanth ^{[1
]}

Pulivendala, Gauthami ^{[2
]}

Gour, Jitendra ^{[1
]}

Malasala, Satyaveni ^{[1
]}

Bujji, Sushmitha ^{[1
]}

Parupalli, Ramulu ^{[1
]}

Shaikh, Mujahid ^{[1
]}

Godugu, Chandraiah ^{[2
]}

Nanduri, Srinivas ^{[1
]}

机构：

[1] NIPER, Dept Med Chem, Hyderabad 500037, India

[2] NIPER, Dept Pharmacol & Toxicol, Hyderabad 500037, India

来源：

JOURNAL OF MOLECULAR STRUCTURE | 2020年 / 1200卷

关键词：

4(3H)-quinazolinone; Cytotoxicity; MDA-MB-231; Cell migration; Colony formation; IN-VITRO; BIOLOGICAL EVALUATION; ANTIBACTERIAL AGENTS; APOPTOSIS PATHWAYS; MOLECULAR DOCKING; RECEPTOR-ACTIVITY; INHIBITORS; ANTITUMOR; TUMOR; PROTEIN;

D O I：

10.1016/j.molstruc.2019.127097

中图分类号：

O64 [物理化学（理论化学）、化学物理学];

学科分类号：

070304 ; 081704 ;

摘要：

A series of new 4(3H)-quinazolinones were synthesized and evaluated for their cytotoxic activity against a set of human cancer cell lines MDA-MB-231 and MCF-7 (breast), HCT-116 and HT-29 (colon) and A549 (lung). Among the tested compounds, 22a exhibited promising cytotoxic activity against MDA-MB-231 (IC50: 3.21 mu M) and HT-29 (IC50: 7.23 mu M) cell lines. The mechanism of action and the apoptosis inducing effect of the compound 22a were studied using the breast cancer cell line MDA-MB-231. Treatment of MDA-MB-231 cell line with compound 22a showed typical apoptotic morphology like cell shrinkage, chromatin condensation and horseshoe shaped nuclei formation. Flow cytometric analysis indicated that the compound induces G0/G1 phase of cell cycle arrest in a dose dependent manner. The binding modes of the potent compounds with EGFR target protein were investigated by docking studies. (C) 2019 Elsevier B.V. All rights reserved.

引用

页数：13

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