- Straightforward synthesis, characterization, and cytotoxicity evaluation of hybrids of natural alkaloid evodiamine/rutaecarpine and thieno[2,3-d]pyrimidinones
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Dozens of hybrids of natural alkaloid evodiamine/rutaecarpine and thieno[2,3-d]pyrimidinones were synthesized in a straightforward method by condensation of substituted 2H-thieno[2,3-d][1, 3]oxazine-2,4(1H)-diones or N-methyl-2H-thieno[2,3-d][1, 3]oxazine-2,4(1H)-dione with 3,4-dihydro-β-carbolines. In vitro cytotoxic assay discovered that compounds 9a, 10e, 11a, 11d, 11f, and 12a could induce antiproliferation against four different types of human cancer cells while compounds 10f and 12e were inactive. Notably, compound 11a displayed potent cell cytotoxicity for human non-small cell lung cancer cells A549, PC-9, human prostate cancer cells PC-3, and human breast cancer cell line MCF-7. Furthermore, compound 11a exhibited strong colony formation inhibition to A549 cells. These results unfold potential anticancer therapeutic applications of hybrids of thieno[2,3-d]pyrimidinones and quinazolinones.
- Aisa, Haji Akber,Cao, Jian-Guo,Huang, Guo-Zheng,Liu, Fei-Ze,Nie, Li-Fei,Wang, Si-Si,Xiamuxi, Hainimu
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- Thienopyridine-carboxylic acid derivatives
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Novel thienopyridine-carboxylic acid derivatives, which are shown by the general formula SPC1 Wherein R1 represents hydrogen or a lower alkyl; R2 represents hydrogen, a lower alkyl or a halogen; or R1 and R2, taken together, may represent an alkylene to form a 5- or 6-membered ring with or without alkyl substituents; each of R4 and R5 represents hydrogen or a lower alkyl; and their pharmaceutically acceptable salts obtainable when R4 is hydrogen, which are useful medicines such as chemotherapeutic agents of bacterial infections.
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