EFFICIENT SYNTHESIS OF NOVEL SPIRO[INDOLINE-3,5'-PYRANO- [2,3-d]PYRIMIDIN]-2-ONE DERIVATIVES AND ANTITUMOR ACTIVITY EVALUATION

An efficient method for synthesis of the spiro[indoline-3,5'-pyrano[2,3-d]pyrimidin]-2-one derivatives from 2'-amino-2-oxospiro[indoline-3,4'-pyran]-3'-carbonitriles using bis(trichloromethyl) carbonate (BTC) and triphenylphosphine oxide (TPPO) was developed. A series of target c...

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Bibliographic Details
Published inHeterocycles Vol. 104; no. 7; pp. 1212 - 1228
Main Authors Li, Zhenhua, Huang, Guoqing, Rong, Dayou, Cao, Yingyan, Hu, Ronghui
Format Journal Article
LanguageEnglish
Published OXFORD Elsevier 01.07.2022
Subjects
Chemistry
Chemistry, Organic
Physical Sciences
Science & Technology
POTENT
ANTICANCER
SPIROINDOLONES
BIS(TRICHLOROMETHYL) CARBONATE
INHIBITORS
FACILE
STRUCTURE-BASED DESIGN
CATALYTIC AMOUNT
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Summary:An efficient method for synthesis of the spiro[indoline-3,5'-pyrano[2,3-d]pyrimidin]-2-one derivatives from 2'-amino-2-oxospiro[indoline-3,4'-pyran]-3'-carbonitriles using bis(trichloromethyl) carbonate (BTC) and triphenylphosphine oxide (TPPO) was developed. A series of target compounds with broad substrate scope were synthesized in moderate to good yields. In addition, the antitumor activities against four cancer cell lines A549, HepG-2, MCF-7, and HeLa were evaluated using 5-FU and cisplatin as reference, all compounds showed good antitumor activity compared with the standard drugs.
ISSN:0385-5414
1881-0942
DOI:10.3987/COM-22-14658