异硫氰酸盐
依托泊苷
医学
A549电池
癌症研究
异硫氰酸苄酯
结构-活动关系
细胞培养
部分
细胞生长
生物化学
肿瘤科
化学
细胞
立体化学
内科学
药理学
肺癌
体外
化疗
生物
遗传学
作者
Jaruwan Chatwichien,Buntarika Prachavna,Rinrada Suntivich,Sarawut Kumphune
出处
期刊:Letters in Organic Chemistry
[Bentham Science]
日期:2019-05-30
卷期号:16 (7): 569-574
标识
DOI:10.2174/1570178615666181011145219
摘要
Isothiocyanate functional group (-N=C=S) is widely accepted as an important moiety for anti- cancer effects of naturally occurring isothiocyanate compounds (ITCs). Herein, a series of diisothiocyanate (diITCs) derivatives were synthesized and evaluated in antiproliferative assays on A549 human non-small cell lung cancer and IMR90 human foetal lung cell lines for structure-activity relationship (SAR) and cancer cell selectivity studies. Results showed that aliphatic and benzylic diITCs were more cytotoxic to A549 cells than natural ITCs; benzyl isothiocyanate (BITC) and phenyl isothiocyanate (PITC), and a currently available anticancer drug; etoposide. Aromatic diITCs were not as active. Notably, most of the diITCs reported in this work were significantly more selective than etoposide to inhibit proliferation of the cancer cells (A549) over the normal cells (IMR90). This study demonstrated a guideline to modify chemical structures of diITCs for anti-NSCLC agents.
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