title: Synthesis of pyrazolo[1,5-a]pyrimidine linked aminobenzothiazole conjugates as potential anticancer agents.
abstract: A series of pyrazolo[1,5-a]pyrimidine linked 2-aminobenzothizole conjugates (6a-t) were synthesized and evaluated for their anticancer activity against five human cancer cell lines. Among them two compounds 6p and 6m showed significant anticancer activity with IC50 values ranging from 2.01 to 7.07 and 1.94-3.46 μM, respectively. Moreover, cell cycle arrest in G2/M and reduction in Cdk1 expression level were observed upon treatment of these compounds and they also induced caspase-3 dependent apoptosis. This was further confirmed by staining as well as DNA fragmentation analysis.
authors.affiliation: Medicinal Chemistry and Pharmacology, CSIR-Indian Institute of Chemical Technology, Hyderabad 500 007, India. ahmedkamal@iict.res.in
authors.forename: Ahmed
authors.initials: A
authors.lastname: Kamal
authors.forename: Jaki R
authors.initials: JR
authors.lastname: Tamboli
authors.forename: V Lakshma
authors.initials: VL
authors.lastname: Nayak
authors.forename: S F
authors.initials: SF
authors.lastname: Adil
authors.forename: M V P S
authors.initials: MV
authors.lastname: Vishnuvardhan
authors.forename: S
authors.initials: S
authors.lastname: Ramakrishna
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D017209:Apoptosis / Q000187:drug effects; D052160:Benzothiazoles / Q000737:chemistry*; D016203:CDC2 Protein Kinase / Q000378:metabolism; D053148:Caspase 3 / Q000378:metabolism; D045744:Cell Line, Tumor; D053938:DNA Fragmentation / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D059565:G2 Phase Cell Cycle Checkpoints / Q000187:drug effects; D006801:Humans; D059566:M Phase Cell Cycle Checkpoints / Q000187:drug effects; D011720:Pyrazoles / Q000737:chemistry*; D011743:Pyrimidines / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D052160:Benzothiazoles; D011720:Pyrazoles; D011743:Pyrimidines; C523775:aminobenzothiazole compound; C527752:pyrazolo(1,5-a)pyrimidine; D016203:CDC2 Protein Kinase; D053148:Caspase 3