Development of pyridine dicoumarols as potent anti HIV-1 leads, targeting HIV-1 associated topoisomeraseIIβ kinase.

Kurumurthy Kammari, Kiran Devaraya, Akhila Bommakanti, Anand K Kondapi

Future medicinal chemistry 2017 Sep

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A structural study of a series of pyridine dicoumarol derivatives with potential activity against a novel Topoisomerase IIβ kinase which was identified in the HIV-1 viral lysate, compounds were designed and synthesized based on a 3D-QSAR study. Based on QSAR model we have designed and synthesized a series of pyridine dicoumarol derivatives and characterized by spectral studies, all the molecules are biologically evaluated by kinase assay, cytotoxicity assay, ELISA and PCR method. We demonstrated the achievement of water soluble disodium pyridine dicoumarate derivatives showing high anti-HIV-1 activity (IC50 <25 nM) which provides a crucial point for further development of pyridine dicoumarol series as HIV-1-associated topoisomerase IIβ kinase inhibitors for clinical application against AIDS. A new class of anti-HIV-1 lead compounds have been designed and tested. Further studies would result in development of novel and potential drugs.

Citation

Kurumurthy Kammari, Kiran Devaraya, Akhila Bommakanti, Anand K Kondapi. Development of pyridine dicoumarols as potent anti HIV-1 leads, targeting HIV-1 associated topoisomeraseIIβ kinase. Future medicinal chemistry. 2017 Sep;9(14):1597-1609