Anti-cancer activities of 5-acyl-6-[2-hydroxy/benzyloxy-3-(amino)-propylamino]-1,3-dialkyl-1H-pyrimidin-2,4-diones.
All the nine 1,3-dialkylated-pyrimidin-2,4-diones investigated are active against all the 59 human tumor cell lines. Compounds 2, 3, 4, and 6 show significant anti-cancer activities at some specific cell lines while compounds 7 and 9 exhibit anti-cancer activities against more number of cell lines. The structure-activity relationship studies indicate that the presence of piperidine/pyrrolidine at the end of C-6 chain, benzoyl group at C-5, and benzyl groups at N-1, N-3 of the pyrimidine ring increases the anti-cancer activities of these molecules.
Singh
Palwinder
P
Department of Chemistry, Guru Nanak Dev University, Amritsar-143005, India. palwinder_singh_2000@yahoo.com
Paul
Kamaldeep
K
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy*; D010880:Piperidines / Q000737:chemistry; D011412:Propanolamines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011744:Pyrimidinones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011759:Pyrrolidines / Q000737:chemistry; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D010880:Piperidines; D011412:Propanolamines; D011743:Pyrimidines; D011744:Pyrimidinones; D011759:Pyrrolidines; C032727:piperidine; C030986:pyrimidine; C032519:pyrrolidine