title: Synthesis of 3-phenylpyrazolopyrimidine-1,2,3-triazole conjugates and evaluation of their Src kinase inhibitory and anticancer activities.
abstract: A series of two classes of 3-phenylpyrazolopyrimidine-1,2,3-triazole conjugates were synthesized using click chemistry approach. All compounds were evaluated for inhibition of Src kinase and human ovarian adenocarcinoma (SK-Ov-3), breast carcinoma (MDA-MB-361), and colon adenocarcinoma (HT-29). Hexyl triazolyl-substituted 3-phenylpyrazolopyrimidine exhibited inhibition of Src kinase with an IC(50) value of 5.6 μM. 4-Methoxyphenyl triazolyl-substituted 3-phenylpyrazolopyrimidine inhibited the cell proliferation of HT-29 and SK-Ov-3 by 73% and 58%, respectively, at a concentration of 50 μM.
authors.affiliation: Department of Chemistry, Birla Institute of Technology and Science, Pilani, Rajasthan, India.
authors.forename: Anil
authors.initials: A
authors.lastname: Kumar
authors.forename: Israr
authors.initials: I
authors.lastname: Ahmad
authors.forename: Bhupender S
authors.initials: BS
authors.lastname: Chhikara
authors.forename: Rakesh
authors.initials: R
authors.lastname: Tiwari
authors.forename: Deendayal
authors.initials: D
authors.lastname: Mandal
authors.forename: Keykavous
authors.initials: K
authors.lastname: Parang
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001943:Breast Neoplasms / Q000188:drug therapy; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D003110:Colonic Neoplasms / Q000188:drug therapy; D005260:Female; D006801:Humans; D020128:Inhibitory Concentration 50; D008958:Models, Molecular; D015394:Molecular Structure; D010051:Ovarian Neoplasms / Q000188:drug therapy; D011714:Pyrans / Q000737:chemistry*; D011743:Pyrimidines / Q000737:chemistry*; D014230:Triazoles / Q000737:chemistry*; D019061:src-Family Kinases / Q000037:antagonists & inhibitors / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D011714:Pyrans; D011743:Pyrimidines; D014230:Triazoles; D019061:src-Family Kinases