New class of azaheptapyridine FPT inhibitors as potential cancer therapy agents |
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| Affiliation: | 1. Department of Physics, Linköping University, SE-581 83 Linköping, Sweden;2. Department of Physics, Umeå University, SE-901 87 Umeå, Sweden;1. School of Pure and Applied Physics, Mahatma Gandhi University, Priyadarshini Hills P.O., Kottayam, Kerala, India;2. Department of Physics, Mar Thoma College, Kuttapuzha P.O., Thiruvalla 689103, Kerala, India;3. Department of Physics, N.S.S. Hindu College, Changanacherry 686102, Kerala, India |
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| Abstract: | Tertiary hydroxyl class of C-imidazole bridgehead azaheptapyridine FPT inhibitors were prepared in an attempt to block in vivo oxidation of secondary hydroxyl series. One representative compound 5a exhibited potent enzyme (IC50 = 1.4 nM) and cellular activities (soft agar IC50 = 1.3 nM) with excellent oral pharmacokinetic profiles in rats, mice, monkeys and dogs. The in vivo study in wap-ras TG mouse models showed dose dependent tumor growth inhibition and regression. |
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| Keywords: | FPT inhibitors |
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