title: Synthesis of imidazothiazole-chalcone derivatives as anticancer and apoptosis inducing agents.
abstract: A new class of imidazo[2,1-b]thiazole chalcone derivatives were synthesized and evaluated for their anticancer activity. These chalcone derivatives show promising activity, with log GI(50) values ranging from -7.51 to -4.00. The detailed biological aspects of these derivatives toward the MCF-7 cell line were studied. Interestingly, these chalcone derivatives induced G(0)/G(1)-phase cell-cycle arrest, down-regulation of G(1)-phase cell-cycle regulatory proteins such as cyclin D1 and cyclin E1, and up-regulation of CDK4. Moreover, these compounds elicit the characteristic features of apoptosis such as enhancement in the levels of p53, p21, and p27, suppression of NF-κB, and up-regulation of caspase-9. One of these chalcone derivatives, 3 d, is potentially well suited for detailed biological studies, either alone or in combination with existing therapies.
authors.affiliation: Chemical Biology Laboratory, Indian Institute of Chemical Technology, Hyderabad 500607, India. ahmedkamal@iict.res.in
authors.forename: Ahmed
authors.initials: A
authors.lastname: Kamal
authors.forename: D
authors.initials: D
authors.lastname: Dastagiri
authors.forename: M Janaki
authors.initials: MJ
authors.lastname: Ramaiah
authors.forename: J Surendranadha
authors.initials: JS
authors.lastname: Reddy
authors.forename: E Vijaya
authors.initials: EV
authors.lastname: Bharathi
authors.forename: Chatla
authors.initials: C
authors.lastname: Srinivas
authors.forename: S N C V L
authors.initials: SN
authors.lastname: Pushpavalli
authors.forename: Dhananjaya
authors.initials: D
authors.lastname: Pal
authors.forename: Manika
authors.initials: M
authors.lastname: Pal-Bhadra
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D053453:Caspase 9 / Q000378:metabolism; D002453:Cell Cycle / Q000187:drug effects*; D045744:Cell Line, Tumor; D002599:Chalcone / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D018844:Cyclin-Dependent Kinases / Q000378:metabolism; D016213:Cyclins / Q000378:metabolism; D005260:Female; D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D016328:NF-kappa B / Q000378:metabolism; D013844:Thiazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D016213:Cyclins; D007093:Imidazoles; D016328:NF-kappa B; D013844:Thiazoles; D002599:Chalcone; D018844:Cyclin-Dependent Kinases; D053453:Caspase 9