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Pharmocophoric Studies of Anti-Telomerase Drugs


 

Human Telomeres are the repetitive DNA sequences of TTAGGG/ AATCCC that protects chromosomes from the loss of essential genes. Telomeres are replicated by telomerase, a special polymerase that has own RNA template. Telomerase is universal marker of human cancer. The cancer cells have neoplastic immortalization rendered by upregulation of telomerase. Rationally, telomerase is an attractive target of cancer therapeutics. Anti-telomerase drugs are the novel enzyme inhibitors. We made a non-computational effort for the basic pharmocophoric design. It is based on the binding functions, , mode of actions, structural resemblances and correlation of reported IC50 values. Pyrimidine nucleosides, non-nucleosides, HIV-RTIs, Cartenoids, Flavonoids, synthetic chrome and phenyl derivatives were pharmocophorically studied. A chemical hybrid structure for anti-telomerase drug was proposed.


Keywords

Human cancer, Binding functions, Telomerase, Pharmocophoric, IC50 values, Planarity, Chemical Hybrid
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  • Pharmocophoric Studies of Anti-Telomerase Drugs

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Abstract


Human Telomeres are the repetitive DNA sequences of TTAGGG/ AATCCC that protects chromosomes from the loss of essential genes. Telomeres are replicated by telomerase, a special polymerase that has own RNA template. Telomerase is universal marker of human cancer. The cancer cells have neoplastic immortalization rendered by upregulation of telomerase. Rationally, telomerase is an attractive target of cancer therapeutics. Anti-telomerase drugs are the novel enzyme inhibitors. We made a non-computational effort for the basic pharmocophoric design. It is based on the binding functions, , mode of actions, structural resemblances and correlation of reported IC50 values. Pyrimidine nucleosides, non-nucleosides, HIV-RTIs, Cartenoids, Flavonoids, synthetic chrome and phenyl derivatives were pharmocophorically studied. A chemical hybrid structure for anti-telomerase drug was proposed.


Keywords


Human cancer, Binding functions, Telomerase, Pharmocophoric, IC50 values, Planarity, Chemical Hybrid