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Efficient Synthesis of New Thieno[2,3‐ d ]pyrimidin‐4(3 H )‐one Derivatives for Evaluation as Anticancer Agents
Author(s) -
Hu YangGen,
Zheng AiHua,
Li GaoJun,
Dong MengZhu,
Ye Fang,
Sun Feng,
Liu ZhengYun,
Li Wen
Publication year - 2014
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.1823
Subject(s) - chemistry , pyrimidinones , stereochemistry , cancer cell lines , combinatorial chemistry , cytotoxic t cell , elemental analysis , cancer cell , cancer , organic chemistry , biochemistry , in vitro , medicine
Thieno[2,3‐ d ]pyrimidinones were reported to act as potent anticancer agents; in this work, a series of new substituted thieno[2,3‐ d ]pyrimidinone ( 6 ) were synthesized via the aza‐Wittig reaction in satisfactory yields. The structures of these compounds were confirmed by elemental analysis, IR, 1 H‐NMR, and mass spectral data, and compound 6h was further analyzed by single crystal X‐ray diffraction. Cytotoxic effect of all the compounds was carried out on human breast and lung cancer cell lines (MCF‐7 and SPC‐A‐1, A459). Compound 6f exhibited the best inhibition activities against A459 with IC 50 4.1 μM.