化学研究与应用
化學研究與應用
화학연구여응용
CHEMICAL RESEARCH AND APPLICATION
2015年
2期
145-150
,共6页
左建%王杰%李家明%钟国琛%张恩立
左建%王傑%李傢明%鐘國琛%張恩立
좌건%왕걸%리가명%종국침%장은립
1 ,2-苯并噻嗪类化合物%合成%酪氨酸激酶抑制剂%抗肿瘤
1 ,2-苯併噻嗪類化閤物%閤成%酪氨痠激酶抑製劑%抗腫瘤
1 ,2-분병새진류화합물%합성%락안산격매억제제%항종류
1,2-benzothiazine derivatives%synthesis%tyrosine kinase inhibitors%antitumor
根据拼合原理,设计合成了一系列全新的具有拉帕替尼和诺拉替尼分子片段的1,2-苯并噻嗪类化合物,其结构均经IR、1H NMR、13C NMR和MS确证。考察所合成化合物的体外抗肿瘤细胞(A549,MCF-7)活性,结果表明,所合成的化合物对肿瘤细胞增殖均有一定的抑制活性,并强于阳性对照药吉非替尼和美洛昔康。
根據拼閤原理,設計閤成瞭一繫列全新的具有拉帕替尼和諾拉替尼分子片段的1,2-苯併噻嗪類化閤物,其結構均經IR、1H NMR、13C NMR和MS確證。攷察所閤成化閤物的體外抗腫瘤細胞(A549,MCF-7)活性,結果錶明,所閤成的化閤物對腫瘤細胞增殖均有一定的抑製活性,併彊于暘性對照藥吉非替尼和美洛昔康。
근거병합원리,설계합성료일계렬전신적구유랍파체니화낙랍체니분자편단적1,2-분병새진류화합물,기결구균경IR、1H NMR、13C NMR화MS학증。고찰소합성화합물적체외항종류세포(A549,MCF-7)활성,결과표명,소합성적화합물대종류세포증식균유일정적억제활성,병강우양성대조약길비체니화미락석강。
According to combination principle,a series of 1,2-benzothiazine derivatives,which had fragments of Lapatinib and Nera-tinib were designed and synthesized. Their structures were identified with IR,1 H-NMR,13 C-NMR and MS. The target compounds were tested for cytotoxic activity against two cancer cell lines,including A549 and MCF-7 by MTT in vitro. All compounds demon-strated certain antitumor abilities,and were better than Gefitinib and Meloxicam.
