Regioselective synthesis and in vitro anticancer activity of 4-aza-podophyllotoxin derivatives catalyzed by L-proline.
A series of 4-aza-podophyllotoxin derivatives have been synthesized regioselectively via the three-component reaction of aldehydes, aromatic amines, and tetronic acid catalyzed by l-proline. This method has the advantages of high yield, high regioselectivity, extensive adaptability, easy operation, and environmental friendliness. These compounds were also investigated in vitro, and some were found to have good anticancer activity.
Shi
Chunling
C
Key Laboratory of Organic Synthesis of Jiangsu Province, College of Chemistry, Chemical Engineering and Materials Science, Soochow University, Suzhou, PR China.
Wang
Juxian
J
Chen
Hui
H
Shi
Daqing
D
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001372:Aza Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002384:Catalysis; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D018360:Crystallography, X-Ray; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008958:Models, Molecular; D015394:Molecular Structure; D011034:Podophyllotoxin / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011392:Proline / Q000737:chemistry*; D013237:Stereoisomerism
D000970:Antineoplastic Agents; D001372:Aza Compounds; D011392:Proline; D011034:Podophyllotoxin