| Autor: |
Subba Rao AV; Medicinal Chemistry and Pharmacology , India.; Academy of Scientific and Innovative Research (AcSIR) , India., Rao BB; Academy of Scientific and Innovative Research (AcSIR) , India.; Centre for Chemical Biology , CSIR-Indian Institute of Chemical Technology , Hyderabad 500 007 , India . Email: ahmedkamal@iict.res.in., Sunkari S; Medicinal Chemistry and Pharmacology , India.; Academy of Scientific and Innovative Research (AcSIR) , India., Shaik SP; Medicinal Chemistry and Pharmacology , India.; Academy of Scientific and Innovative Research (AcSIR) , India., Shaik B; Medicinal Chemistry and Pharmacology , India., Kamal A; Medicinal Chemistry and Pharmacology , India.; Academy of Scientific and Innovative Research (AcSIR) , India. |
| Abstrakt: |
A new series of 2-arylaminobenzothiazole-arylpropenone conjugates 5 - 6 ( a - r ) was designed, synthesized and investigated for their cytotoxic potency against the various human cancer cell lines. Most of these conjugates exhibited cytotoxic activity and inhibited in vitro tubulin polymerization effectively. Conjugates 5d and 6d cause cell cycle blocks in the G2/M phase in HeLa cells and treatments with 5d and 6d manifested increased mRNA and protein levels of the G2/M marker, cyclin B1. Immunocytochemistry revealed loss of intact microtubule structure in cells treated with 5d and 6d . Western blot analysis revealed that these conjugates accumulate more tubulin in the soluble fraction. Moreover, the triggering of apoptotic cell death after mitotic arrest was investigated by studying their effect on Hoechst staining, mitochondrial membrane potential, ROS generation. |
