One pot synthesis of thiazolodihydropyrimidinones and evaluation of their anticancer activity.
2-(5-Arylfurfurylidene/5-nitrofurfurylidene)-5-aryl-7-(2,4-dichloro-5-fluorophenyl)-5H-thiazolo[2,3-b]-pyrimidin-2(1H)-ones 5 and 6 are synthesized by a novel three component reaction of 4,6-diarylpyrimidino-2(1H)-thiones 4, monochloroacetic acid, arylfurfuraldehydes and 5-nitro-2-furfuraldenediacetate, respectively. The newly synthesized compounds are characterized by elemental analysis, IR, (1)H NMR and mass spectral studies. These compounds exhibited in vitro antitumour activity with moderate to excellent growth inhibition against a panel of 60 cell lines of leukemia, non-small cell lung cancer melanoma, ovarian cancer, prostate cancer and breast cancer.
Holla
B Shivarama
BS
Department of Post Graduate Studies and Research in Chemistry, Mangalore University, Mangalagangotri 574199, Karnataka, India. hollabs@yahoo.com
Rao
B Sooryanarayana
BS
Sarojini
B K
BK
Akberali
P M
PM
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004353:Drug Evaluation, Preclinical / Q000379:methods; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D015394:Molecular Structure; D011744:Pyrimidinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
D000970:Antineoplastic Agents; D011744:Pyrimidinones; D013844:Thiazoles