Di-substituted Noscapine Analogs as Potent Anticancer Agents

Noscapine is an opium-derived kinder and gentler microtubule affecting drug, currently in clinical trials for cancer chemotherapy. Here, we report the synthesis of four potent di-substituted derivatives of noscapine and their effect on Prostate Cancer and Breast cancer cells. These have higher tubulin binding than noscapine and affect its polymerization.

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The equilibrium dissociation constant between tubulin and new compounds is comparable to parent analog. These noscapine analogs affect cell cycle so that the cells enter a dormant phase and do not divide any further. The biological activity of these analogs was rationalized utilizing molecular modeling Techniques. The analysis of proteins from treated cells revealed the induction of apoptosis and reduction in survivin levels. This result was also supported by increased activity of Caspase enzymes. These compounds have shown great potential for study of microtubule function and as chemotherapeutic agents for managing human cancers.

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