Synthesis and evaluation of antitumor activity of dibenzodiazepine derivatives

被引：4

作者：

Cao, Ke ^{[1
]}

Yan, Jianwei ^{[1
]}

Yan, Fulin ^{[1
,2
]}

Yin, Tiantian ^{[2
]}

机构：

[1] Xinxiang Med Univ, Pharm Coll, Xinxiang 453003, Henan, Peoples R China

[2] Xinxiang Med Univ, Sanquan Coll, Xinxiang 453003, Henan, Peoples R China

来源：

MOLECULAR DIVERSITY | 2021年 / 25卷 / 02期

关键词：

Dibenzodiazepine; Halogenation; Suzuki reaction; N-methylpiperazine; Antitumor activity; CLOZAPINE; OPTIMIZATION; POTENT;

D O I：

10.1007/s11030-020-10051-z

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of dibenzodiazepine 2-position derivatives, bearing N-methylpiperazine at the C-11 position, were prepared by using a concise approach. Their inhibitory activities of tumor cell proliferation in vitro were tested in five cell lines, including breast cancer cell BCAP37, gastric cancer cell SGC7901, liver cancer cell HepG2, cervical cancer cell HeLa and acute promyelocytic leukemia cell HL-60. Several compounds showed efficient tumor activity with IC50 values down to 0.30 mu M. These compounds are expected to be a new class of potential anticancer lead compounds. [GRAPHICS] .

引用

页码：1111 / 1122

页数：12

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