title: Synthesis, single crystal and antitumor activities of benzimidazole-quinazoline hybrids.
abstract: A series of novel regioisomeric hybrids of quinazoline/benzimidazole viz. (3-allyl-2-methyl-3H-benzimidazol-5-yl)-(2-substituted-quinazolin-4-yl)-amine and (1-allyl-2-methyl-1H-benzimidazol-5-yl)-(2-substituted-quinazolin-4-yl)-amine of biological interest were synthesized. All the synthesized compounds were well characterized by (1)H and (13)C NMR as well as mass spectroscopy. The newly synthesized compounds were screened for in vitro antitumor activities against 60 tumor cell lines panel assay. A significant inhibition for cancer cells were observed with compound 9 and also more active against known drug 5-fluorouracil (5-FU) in some tumor cell lines. Compound 9 displayed appreciable anticancer activity against leukemia, colon, melanoma, renal and breast cancer cell lines.
authors.affiliation: School of Chemistry and Biochemistry, Thapar University, Patiala 147004, India.
authors.forename: Alka
authors.initials: A
authors.lastname: Sharma
authors.forename: Vijay
authors.initials: V
authors.lastname: Luxami
authors.forename: Kamaldeep
authors.initials: K
authors.lastname: Paul
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D001562:Benzimidazoles / Q000737:chemistry*; D001665:Binding Sites; D020134:Catalytic Domain; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D018360:Crystallography, X-Ray; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D008968:Molecular Conformation; D062105:Molecular Docking Simulation; D057093:Orphan Nuclear Receptors / Q000737:chemistry / Q000378:metabolism; D011799:Quinazolines / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D001562:Benzimidazoles; C403073:NR2E3 protein, human; D057093:Orphan Nuclear Receptors; D011799:Quinazolines; C031000:benzimidazole