2. Academic Validation
  3. Synthesis of pyrazolo[1,5-a]pyrimidine linked aminobenzothiazole conjugates as potential anticancer agents

Synthesis of pyrazolo[1,5-a]pyrimidine linked aminobenzothiazole conjugates as potential anticancer agents

  • Bioorg Med Chem Lett. 2013 Jun 1;23(11):3208-15. doi: 10.1016/j.bmcl.2013.03.129.
Ahmed Kamal 1,  Jaki R Tamboli,  V Lakshma Nayak,  S F Adil,  M V P S Vishnuvardhan,  S Ramakrishna
Affiliations

Affiliation

  • 1 Medicinal Chemistry and Pharmacology, CSIR-Indian Institute of Chemical Technology, Hyderabad 500 007, India. ahmedkamal@iict.res.in
PMID: 23623491 DOI: 10.1016/j.bmcl.2013.03.129
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.

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