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一些具有潜在抗癌作用的新型3-(2-(2-苯基噻唑-4-基)乙基)-喹唑啉-4(3H)酮衍生物的合成与细胞毒性评价

Synthesis and cytotoxic evaluation of some new 3-(2-(2-phenylthiazol-4-yl) ethyl)-quinazolin-4(3H) one derivatives with potential anticancer effects.

作者信息

Hosseinzadeh Leila, Aliabadi Alireza, Rahnama Mohsen, Sadeghi Hamid Mir Mohammad, Khajouei Marzieh Rahmani

机构信息

Pharmaceutical Sciences Research Center, School of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, I.R. Iran.

Department of Medicinal Chemistry, School of Pharmacy and Pharmaceutical Science, Kermanshah University of Medical Sciences, Kermanshah, I.R. Iran.

出版信息

Res Pharm Sci. 2017 Aug;12(4):290-298. doi: 10.4103/1735-5362.212046.

Abstract

Quinazolinones are a group of heterocyclic compounds that have important biological activities such as cytotoxicity, anti-bacterial, and anti-fungal effects. Thiazole-containing compounds have also many biological effects including antitumor, antibacterial, anti-inflammatory, and analgesic activities. Due to significant cytotoxic effects of both quinazoline and thiazole derivatives, in this work a group of quinazolinone-thiazol hybrids were prepared and their cytotoxic effects on three cell lines were evaluated using MTT assay. Compounds , , , and showed highest cytotoxic activities against PC3 cell line. Compounds , , and were most active against MCF-7 and , , and showed good cytotoxic effect on HT-29 cell line. According to the results, efficiently inhibited all cell growth tested in a dose dependent manner. The IC50 of A3 was 10 M, 10 μM, and 12 μM on PC3, MCF-7, and HT-29 cells, respectively.

摘要

喹唑啉酮是一类具有重要生物活性的杂环化合物,如细胞毒性、抗菌和抗真菌作用。含噻唑的化合物也有许多生物效应,包括抗肿瘤、抗菌、抗炎和镇痛活性。由于喹唑啉和噻唑衍生物都具有显著的细胞毒性作用,因此在本研究中制备了一组喹唑啉酮-噻唑杂化物,并使用MTT法评估了它们对三种细胞系的细胞毒性作用。化合物、、、对PC3细胞系表现出最高的细胞毒性活性。化合物、、对MCF-7最具活性,而、、对HT-29细胞系表现出良好的细胞毒性作用。根据结果,以剂量依赖性方式有效抑制了所有测试的细胞生长。A3对PC3、MCF-7和HT-29细胞的IC50分别为10 μM、10 μM和12 μM。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3771/5566003/3a5d7c3e4d96/RPS-12-290-g001.jpg

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